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Patent · US2026102507A1 · A1 · US

Camptothecin derivative for treating or preventing cancer and antibody-drug conjugate thereof

(11) Publication number
US2026102507A1
(21) Application number
19/420,112
(22) Filing date
2025-12-15
(30) Priority date
2023-06-13
(43) Publication date
2026-04-16
(52) CPC
  • A61K Preparations for medical, dental or toiletry purposes: 47/68037, 47/6849, 47/6855, 47/6889
  • A61P Specific therapeutic activity of chemical compounds or medicinal preparations: 35/00
  • C07K Peptides: 16/28, 16/32
(54) Title
Camptothecin derivative for treating or preventing cancer and antibody-drug conjugate thereof
(57) Abstract

The present invention relates to camptothecin derivatives, their linker-payload conjugates, and antibody-drug conjugates, as well as pharmaceutically acceptable salts or esters, solvates, tautomers, stereoisomers, prodrugs, or isotopically labeled forms thereof, for use in the treatment or prevention of cancer. The invention further relates to a pharmaceutical composition comprising the camptothecin derivatives, their linker-payload conjugates, or antibody-drug conjugates; methods for the preparation of the same; and the use thereof.

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Claims (1)

  1. An antibody-drug conjugate of formula (I): or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein: Ab is an antibody or antigen-binding fragment thereof; L 1 is each independently a linker unit; L 2 is each independently a linking unit selected from the group consisting of: - (CR m R n) t -(L M) 0−1 -(CH 2 CH 2 O) s - (CR m R n) t - CO -, - (CR m R n) t -L M -(CR m R n) t -(L M) 0−1 -L N -L M -(CH 2 O) s - (CR m R n) t - CO -, - (CR m R n) t -L M -(CR m R n) t - N(R p) - (CR m R n) t - N(R p) - (CR m R n) t - CO -, and - (CR m R n) t -L M -CH(R p) - CO -, wherein the - CO - terminus of L 2 is connected to L 3, and the other terminus of L 2 is connected to L 1, and wherein, R m and R n are each independently H or C 1-6 alkyl, L M is each independently - NH - CO - or - CO - NH -, L N is each independently - (CH 2 CH 2 O) m - (CH 2) t -, - (CH 2) t - (OCH 2 CH 2) m -, -(3- to 8-membered heteroarylene)-(CH 2) t - (OCH 2 CH 2) m, or - (OCH 2 CH 2) m - (CH 2) t -(3- to 8-membered heteroarylene)-, R p is each independently - CO - (CH 2 CH 2 O) m - CH 3 or - (CH 2) t -L M -(CH 2 CH 2 O) m - CH 3, and s and t are each independently 0, 1, 2, 3, 4, 5, 6, 7, or 8, and m is each independently 2, 3, 4, 5, 6, 7, or 8; L 3 is each independently an amino acid residue, a short peptide chain consisting of 2-10 amino acid residues, or - NH - (CH 2) p - CO -; L 4 is each independently a bond or a spacer unit; D is each independently a small molecule drug moiety derived from a compound of formula (II); wherein, R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 3-8 cycloalkyl) or - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the cycloalkyl and heterocycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH, amino, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - (CH 2) p - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; - NH - (CH 2) p - (CH═CH) - R a; or - COOH; R 2 and R 3 are each independently halogen, cyano, NO 2, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy, - NH - CO - (C 1-6 hydroxyalkyl), or NR a R b; or R 2 and R 3, together with the atoms to which they are attached, form a 4- to 8-membered heterocyclic group; R 4 is H or C 3-8 cycloalkyl, preferably H; R a and R b are each independently H, C 1-6 alkyl, - CO - (C 1-6 alkyl), - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino, and wherein the cycloalkyl is further optionally substituted with one or more substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; and p and q are each independently 0, 1, 2, 3, 4, 5, or 6; wherein D is linked to L 4 via R 1 or R 3, or via the oxygen from the hydroxy shown in formula (II); and n is an integer from 0 to 10, preferably an integer from 0 to 8. 2. The antibody-drug conjugate of formula (I) according to claim 1: or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein: Ab is an antibody or antigen-binding fragment thereof; L 1 is each independently a linker unit; L 2 is each independently a linking unit of the formula - (CH 2 CH 2 O) x - (CR m R n) y - CO -, wherein the - CO - terminus is connected to L 3 and the other terminus is connected to L 1, and wherein R m and R a are each independently H or C 1-6 alkyl, x is an integer from 0 to 5, y is an integer from 1 to 5; and the sum of x and y is ≤6; L 3 is each independently an amino acid residue, a short peptide chain consisting of 2-10 amino acid residues, or - NH - (CH 2) p - CO -; L 4 is each independently a bond or a spacer unit; D is each independently a small molecule drug moiety derived from a compound of formula (II); wherein, R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 3-8 cycloalkyl) or - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the cycloalkyl and heterocycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH, amino, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - (CH 2) p - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; - NH - (CH 2) p - (CH═CH) - R a; or - COOH; R 2 and R 3 are each independently halogen, cyano, NO 2, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy, - NH - CO - (C 1-6 hydroxyalkyl), or NR a R b; or R 2 and R 3, together with the atoms to which they are attached, form a 4- to 8-membered heterocyclic group; R 4 is H or C 3-8 cycloalkyl, preferably H; R a and R b are each independently H, C 1-6 alkyl, - CO - (C 1-6 alkyl), - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino, and wherein the cycloalkyl is further optionally substituted with one or more substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; and p and q are each independently 0, 1, 2, 3, 4, 5, or 6; wherein D is linked to L 4 via R 1 or R 3, or via the oxygen from the hydroxyl shown in formula (II); and n is an integer from 0 to 10, preferably an integer from 0 to 8. 3. The antibody-drug conjugate according to claim 1 or 2, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 cycloalkyl) or - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the cycloalkyl and the heterocycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of OH, SH, C 1-6 alkyl, and C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - (CH 2) p - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; - NH - (CH 2) p - (CH═CH) - R a; or - COOH; wherein R a and R b are each independently H, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 aminoalkyl, - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl optionally substituted with one or more substituents independently selected from the group consisting of hydroxy and C 1-6 hydroxyalkyl); preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH(C 1-6 aminoalkyl); - (CH 2) p - NH - (CH 2) q (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; - (CH 2) p - N(C 1-6 alkyl)(- SO 2 - C 1-6 alkyl); - CH═N(C 1-6 alkyl); - NH - CO - (C 1-6 hydroxyalkyl); - NH - CO - (C 3-8 hydroxycycloalkyl); - NH - CO - (CH 2) p - CH(OH) - (C 1-6 alkyl); - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); - NH - (CH 2) p - (CH═CH) - (C 1-6 hydroxyalkyl); or - COOH; or R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; wherein R a and R b are each independently H, C 1-6 alkyl, - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; preferably, R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 cycloalkyl); - (CH 2) p - (C 3-8 hydroxycycloalkyl); - (CH 2) p - (C 3-8 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; more preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; preferably wherein R a and R b are each independently H, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 aminoalkyl, - SO 2 - (C 1-6 alkyl), - (CH 2) q - (C 3-8 cycloalkyl), or - (CH 2) q - (C 3-8 hydroxycycloalkyl); further more preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH(C 1-6 aminoalkyl); - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl); - (CH 2) p - N(C 1-6 alkyl)(- SO 2 - C 1-6 alkyl); - CH═N(C 1-6 alkyl); - NH - CO - (C 1-6 hydroxyalkyl); - NH - CO - (C 3-8 hydroxycycloalkyl); - NH - CO - (CH 2) p - CH(OH) - (C 1-6 alkyl); - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); or - COOH. 4. The antibody-drug conjugate according to claim 1 or 2, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is H, C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - (CH 2) p - (NH 2), - (CH 2) p - NH(C 1-6 alkyl), - (CH 2) p - NH(C 1-6 hydroxyalkyl), - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); preferably, R 1 is H, C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - NH 2, - (CH 2) p - NH(C 1-6 alkyl), - NH(C 1-6 hydroxyalkyl), - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), or - NH - CO - CH(OH) - (C 3-8 cycloalkyl); more preferably, R 1 is H, C 1-6 alkyl, - CH 2 - (C 1-6 alkylthio), - NH 2, - CH 2 - NH(C 1-6 alkyl), - NH(C 1-6 hydroxyalkyl), - CH 2 - NH - CH 2 - (C 3-8 cycloalkyl), or - NH - CO - CH(OH) - (C 3-8 cycloalkyl). 5. The antibody-drug conjugate according to claim 1 or 2, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - (CH 2) p - NH(C 1-6 alkyl), or - (CH 2) p - NH(C 1-6 hydroxyalkyl); preferably, R 1 is C 1-6 alkyl, - CH 2 - (C 1-6 alkylthio), - NH(C 1-6 alkyl), or - NH(C 1-6 hydroxyalkyl). 6. The antibody-drug conjugate according to claim 1 or 2, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - NH 2, - (CH 2) p - NH(C 1-6 alkyl), - (CH 2) p - NH(C 1-6 hydroxyalkyl), - NH - CO - (C 1-6 hydroxyalkyl), or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); preferably, R 1 is C 1-6 alkyl, - NH 2, - (CH 2) p - NH(C 1-6 alkyl), - (CH 2) p - NH(C 1-6 hydroxyalkyl), or - NH - CO - (C 1-6 hydroxyalkyl). 7. The antibody-drug conjugate according to claim 1 or 2, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is C 1-6 alkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH - (CH 2) q (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; or - NH - (CH 2) p - (CH═CH) - (C 1-6 hydroxyalkyl); or, R 1 is C 1-6 alkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; - NH - CO - (C 1-6 hydroxyalkyl); or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); or, R 1 is C 1-6 alkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; - NH - CO - (C 1-6 hydroxyalkyl); or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); or, R 1 is C 1-6 alkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); or, R 1 is C 1-6 alkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - NH(C 1-6 hydroxyalkyl); or - (CH 2) p - NH - (CH 2) q (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl. 8. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 2 is a halogen, preferably fluorine. 9. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 3 is C 1-6 alkyl, C 1-6 alkoxy, halogen, cyano, - NH 2, - NH - CO - (C 1-6 hydroxyalkyl), or NO 2; preferably, R 3 is C 1-6 alkyl, halogen, - NH 2, - NH - CO - (C 1-6 hydroxyalkyl), or NO 2; or, R 3 is halogen, cyano, NO 2, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy, or NR a R b, wherein R a and R b are each independently H, C 1-6 alkyl, - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; preferably, R 3 is C 1-6 alkyl, C 1-6 alkoxy, halogen, cyano, - NH 2 or NO 2; more preferably, R 3 is C 1-6 alkyl, halogen, - NH 2 or NO 2; or, R 3 is C 1-6 alkyl or NR a R b, wherein R a and R b are each independently H or - CO - (C 1-6 alkyl), wherein the alkyl is optionally substituted with one or more OH groups; or, R 3 is C 1-6 alkyl, - NH 2 or - NH - CO - (CH 2 OH), preferably R 3 is C 1-6 alkyl or - NH - CO - (CH 2 OH); or R 3 is C 1-6 alkyl. 10. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 2 and R 3, together with the atoms to which they are attached, form a 4- to 8-membered heterocyclic group containing N, O or S as a heteroatom, such as dioxolane. 11. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein D is connected to L 4 via a nitrogen or oxygen atom in R 1 or R 3, or via the oxygen atom from hydroxy shown in formula (II), for example, through an amide bond, an aminomethyl ether bond, or a carbamate bond. 12. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein D is a moiety selected from the following: No. Structure 1′ 2′ STI-A-6′ 3′ 4′ STI-A2′ 5′ 6′ STI-E-05′ 7′ 8′ STI-F-8′ 9′ STI-F2′ 10′ STI-F-03c-1′ 11′ STI-G1′ 12′ STI-G03′ 13′ STI-G2-06c′ 14′ STI-G2′ 15′ STI-D′ 16′ STI-F′ 17′ STI-F6′ 18′ STI-F7′ 19′ STI-F13′ 20′ STI-G4′ 21′ SIT-F12R′ 22′ STI-F10′ P1′ STI-F5′ P2′ STI-F8′ P3′ STI-F14′ P4′ STI-F15′ P5′ STI-F17′ P6′ STI-F18′ P7′ STI-G5′ 13. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 1 is each independently: preferably more preferably wherein position 1 is connected to Ab, and position 2 is connected to L 2. 14. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 2 is each independently a linking unit selected from the group consisting of: - (CH 2) t -(L M) 0−1 -(CH 2 CH 2 O) s - (CH 2) t - CO -, - (CH 2) t -L M -(CH 2) t -(L M) 0−1 -L N -L M -(CH 2 O) s - (CH 2) t - CO -, - (CH 2) t -L M -(CH 2) t - N(R p) - (CH 2) t - N(R p) - (CH 2) t - CO -, and (CH 2) t -L M -CH(R p) - CO -, wherein the - CO - terminus of L 2 is connected to L 3, and the other terminus of L 2 is connected to L 1. 15. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 2 is each independently a linking unit selected from the group consisting of: - (CH 2) t - (CH 2 CH 2 O) s - (CH 2) t - CO -, - (CH 2) t - CO - NH - (CH 2 CH 2 O) s - (CH 2) t - CO -, - (CH 2) t - NH - CO - (CH 2 CH 2 O) s - (CH 2) t - CO -, - (CH 2) t - CO - NH - (CH 2) t -(3- to 8-membered heteroarylene)-(CH 2) t - (OCH 2 CH 2) m - NH - CO - (CH 2 O) - (CH 2) t - CO -, - (CH 2) t - CO - NH - (CH 2) t - NH - CO - (CH 2 CH 2 O) m - (CH 2) t - NH - CO - (CH 2 O) - (CH 2) t - CO -, - (CH 2) t - CO - NH - (CH 2) t - NH - CO - (CH 2) t - (OCH 2 CH 2) m - NH - CO - (CH 2 O) - (CH 2) t - CO -, - (CH 2) t - NH - CO - (CH 2) t - N(R p) - (CH 2) t - N(R p) - (CH 2) t - CO -, - (CH 2) t - CO - NH - (CH 2) t - N(R p) - (CH 2) t - N(R p) - (CH 2) t - CO -, or - (CH 2) t - CO - NH - CH(R p) - CO - or - (CH 2) t - NH - CO - CH(R p) - CO -, wherein the - CO - terminus of L 2 is connected to L 3, and the other terminus of L 2 is connected to L 1. 16. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 3 is each independently an amino acid residue, a short peptide chain consisting of 2-6 amino acid residues, or - NH - (CH 2) p - CO -, wherein p is 0, 1, 2, 3, 4, 5, or 6; preferably, the amino acid is selected from the group consisting of glycine (Gly), alanine (Ala), valine (Val), phenylalanine (Phe), citrulline (Cit), lysine (Lys) and asparagine (Asn); for example, L 3 is Gly-Gly-Phe-Gly, Val-Ala, Phe-Lys, or Lys. 17. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 4 is each independently a bond, preferably a bond, more preferably wherein position 1 is connected to L 3 and position 2 is connected to D. 18. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein: L 1 is each independently: preferably more preferably wherein position 1 is connected to Ab, and position 2 is connected to L 2; L 2 is each independently a linking unit of the formula - (CH 2 CH 2 O) x - (CH 2) y - CO -, wherein the - CO - terminus is connected to L 3 and the other terminus is connected to L 1, and wherein x is an integer from 0 to 5, y is an integer from 1 to 5, and x+y≤6; preferably, L 2 is - (CH 2) - CO -, - (CH 2) 2 - CO -, - (CH 2) 3 - CO -, - (CH 2) 4 - CO -, - (CH 2) 5 - CO -, - (CH 2) 6 - CO -, - (CH 2 CH 2 O) - (CH 2) - CO -, - (CH 2 CH 2 O) - (CH 2) 2 - CO -, - (CH 2 CH 2 O) - (CH 2) 3 - CO -, - (CH 2 CH 2 O) - (CH 2) 4 - CO -, - (CH 2 CH 2 O) - (CH 2) 5 - CO -, - (CH 2 CH 2 O) 2 - (CH 2) - CO -, - (CH 2 CH 2 O) 2 - (CH 2) 2 - CO -, - (CH 2 CH 2 O) 2 - (CH 2) 3 - CO -, - (CH 2 CH 2 O) 2 - (CH 2) 4 - CO -, - (CH 2 CH 2 O) 3 - (CH 2) - CO -, - (CH 2 CH 2 O) 3 - (CH 2) 2 - CO -, - (CH 2 CH 2 O) 3 - (CH 2) 3 - CO -; more preferably, L 2 is each independently - (CH 2) 5 - CO - or - (CH 2 CH 2 O) 3 - (CH 2) 2 - CO -; L 3 is each independently an amino acid residue, a short peptide chain consisting of 2-6 amino acid residues, or - NH - (CH 2) p - CO -, wherein p is 0, 1, 2, 3, 4, 5, or 6; preferably, the amino acid is selected from the group consisting of glycine (Gly), alanine (Ala), valine (Val), phenylalanine (Phe), citrulline (Cit), lysine (Lys) and asparagine (Asn); for example, L 3 is Gly-Gly-Phe-Gly, Val-Cit, Val-Ala, Phe-Lys, Val-Lys, Ala-Ala-Ala, Ala-Ala-Asn, or - NH - (CH 2) 2 - CO -; and L 4 is each independently a bond, wherein position 1 is connected to L 3 and position 2 is connected to D. 19. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein the -L 1 -L 2 -L 3 -L 4 - moiety is each independently selected from the group consisting of: wherein position 1 is connected to Ab, and position 2 is connected to D. 20. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein the -L 1 -L 2 -L 3 -L 4 -D moiety is each independently selected from: No. Structure 23′ STI-A3′ 24′ STI-F3′ 25′ STI-F4′ 26′ STI-G′ 27′ STI-G3′ 28′ STI-F1002′ 29′ STI-F1001′ 30′ STI-F1003′ 31′ STI-F1004′ 32′ STI-F1006 33′ STI-F1010 34′ STI-F1011 35′ STI-F1012 36′ STI-F1013 37′ STI-F1014 38′ STI-F1015 39′ STI-F1018 40′ STI-F1019 41′ STI-G1001 42′ STI-F1031 43′ STI-F1034 44′ STI-F1035 45′ STI-F1043 wherein position 1 represents the point of attachment to Ab. 21. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein Ab is an antibody or an antigen-binding fragment thereof that binds to a tumor cell surface antigen; for example, an anti-Her2 antibody or an antigen-binding fragment thereof and/or an anti-FRα antibody or an antigen-binding fragment thereof; in particular, Ab is farletuzumab or an antigen-binding fragment thereof and/or trastuzumab or an antigen-binding fragment thereof. 22. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein the antibody-drug conjugate is selected from the group consisting of: Name Structure Fa-ADC1 Fa-ADC2 Fa-ADC3 Fa-ADC4 Fa-ADC5 Fa-ADC6 Tra-ADC7 Tra-ADC8 Tra-ADC9 Tra-ADC10 Tra-ADC11 Tra-ADC12 Tra-ADC13 Tra-ADC14 Tra-ADC15 Tra-ADC16 Tra-ADC17 Tra-ADC18 Tra-ADC19 Tra-ADC20 wherein, in Fa-ADCs, mAb represents farletuzumab; in Tra-ADCs, mAb represents trastuzumab, and n is 0, 1, 2, 3, 4, 5, 6, 7, or 8. 23. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, which has an average DAR selected from any value within the range from 1.0 to 10.0, preferably has an average DAR selected from any value within the range from 2.0 to 8.0, and more preferably has an average DAR selected from any value within the range from 6.0 to 8.0. 24. A compound of formula (II): or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein, R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 3-8 cycloalkyl) or - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the cycloalkyl and heterocycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH, amino, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - (CH 2) p - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; - NH - (CH 2) p - (CH═CH) - R a; or - COOH; R 2 and R 3 are each independently halogen, cyano, NO 2, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy, - NH - CO - (C 1-6 hydroxyalkyl), or NR a R b; or R 2 and R 3, together with the atoms to which they are attached, form a 4- to 8-membered heterocyclic group; R 4 is H or C 3-8 cycloalkyl, preferably H; R a and R b are each independently H, C 1-6 alkyl, - CO - (C 1-6 alkyl), - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino, and wherein the cycloalkyl is further optionally substituted with one or more substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; and p and q are each independently 0, 1, 2, 3, 4, 5, or 6. 25. The compound according to claim 24, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein: R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 cycloalkyl) or - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the cycloalkyl and the heterocycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of OH, SH, C 1-6 alkyl, and C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - (CH 2) p - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; - NH - (CH 2) p - (CH═CH) - R a; or - COOH; wherein R a and R b are each independently H, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 aminoalkyl, - SO 2 - (C 1-6 alkyl), or - (CH 2) q (C 3-8 cycloalkyl optionally substituted with one or more substituents independently selected from the group consisting of hydroxy and C 1-6 hydroxyalkyl); preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH(C 1-6 aminoalkyl); - (CH 2) p - NH - (CH 2) q (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; - (CH 2) p - N(C 1-6 alkyl)(- SO 2 - C 1-6 alkyl); - CH═N(C 1-6 alkyl); - NH - CO - (C 1-6 hydroxyalkyl); - NH - CO - (C 3-8 hydroxycycloalkyl); - NH - CO - (CH 2) p - CH(OH) - (C 1-6 alkyl); - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); - NH - (CH 2) p - (CH═CH) - (C 1-6 hydroxyalkyl); or - COOH; or R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; wherein R a and R b are each independently H, C 1-6 alkyl, - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; preferably, R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 cycloalkyl); - (CH 2) p - (C 3-8 hydroxycycloalkyl); - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; more preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; preferably wherein R a and R b are each independently H, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 aminoalkyl, - SO 2 - (C 1-6 alkyl), - (CH 2) q - (C 3-8 cycloalkyl), or - (CH 2) q - (C 3-8 hydroxycycloalkyl); further more preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH(C 1-6 aminoalkyl); - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl); - (CH 2) p - N(C 1-6 alkyl)(- SO 2 - C 1-6 alkyl); - CH═N(C 1-6 alkyl); - NH - CO - (C 1-6 hydroxyalkyl); - NH - CO - (C 3-8 hydroxycycloalkyl); - NH - CO - (CH 2) p - CH(OH) - (C 1-6 alkyl); - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); or - COOH. 26. The compound according to claim 24, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is H, C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - (CH 2) p - (NH 2), - (CH 2) p - NH(C 1-6 alkyl), - (CH 2) p - NH(C 1-6 hydroxyalkyl), - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); preferably, R 1 is H, C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - NH 2, - (CH 2) p - NH(C 1-6 alkyl), - NH(C 1-6 hydroxyalkyl), - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), or - NH - CO - CH(OH) - (C 3-8 cycloalkyl); more preferably, R 1 is H, C 1-6 alkyl, - CH 2 - (C 1-6 alkylthio), - NH 2, - CH 2 - NH(C 1-6 alkyl), - NH(C 1-6 hydroxyalkyl), - CH 2 - NH - CH 2 - (C 3-8 cycloalkyl), or - NH - CO - CH(OH) - (C 3-8 cycloalkyl). 27. The compound according to claim 24, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - (CH 2) p - NH(C 1-6 alkyl), or - (CH 2) p - NH(C 1-6 hydroxyalkyl); preferably, R 1 is C 1-6 alkyl, - CH 2 - (C 1-6 alkylthio), - NH(C 1-6 alkyl), or - NH(C 1-6 hydroxyalkyl). 28. The compound according to any one of claims 24-27, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 2 is a halogen, preferably fluorine. 29. The compound according to any one of claims 24-28, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 3 is C 1-6 alkyl, C 1-6 alkoxy, halogen, cyano, - NH 2, - NH - CO - (C 1-6 hydroxyalkyl), or NO 2; preferably, R 3 is C 1-6 alkyl, halogen, - NH 2, - NH - CO - (C 1-6 hydroxyalkyl), or NO 2; or, R 3 is halogen, cyano, NO 2, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy, or NR a R b, wherein R a and R b are each independently H, C 1-6 alkyl, - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; preferably, R 3 is C 1-6 alkyl, C 1-6 alkoxy, halogen, cyano, - NH 2 or NO 2; more preferably, R 3 is C 1-6 alkyl, halogen, - NH 2 or NO 2. 30. The compound according to any one of claims 24-27, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 2 and R 3, together with the atoms to which they are attached, form a 4- to 8-membered heterocyclic group containing an oxygen, nitrogen or sulfur atom as a heteroatom, such as dioxolane. 31. The compound according to claim 24, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein the compound is selected from the group consisting of: No. Structure 1 STI-A-4 2 3 4 5 6 STI-E05 7 8 STI-F-8 9 10 STI-F-03c-1 11 STI-G1 12 STI-G03 13 STI-G2-06c 14 STI-G2 15 STI-D 16 STI-F 17 STI-F6 18 STI-F7 19 STI-F13 20 STI-G4 21 STI-F12R 22 STI-F10 P1 STI-F5 P2 STI-F8 P3 STI-F14 P4 STI-F15 P5 STI-F17 P6 STI-F18 P7 STI-G5 32. A linker-payload conjugate of formula (III): or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 1, L 2, L 3, L 4 and D are as defined in any one of claims 1-20, and wherein when L 1 is Lg and L 1 together form when L 1 is not Lg is a leaving group; preferably, Lg is halogen, sulfonyl (e.g., methanesulfonyl, p-toluenesulfonyl), sulfonyloxy (e.g., methanesulfonyloxy, CF 3 SO 3 -, p-toluenesulfonyloxy), a tertiary-ammonium group (e.g., Me 3 N + or Et 3 N +), or a diazonium group; more preferably, Lg is F, Cl, Br, or methanesulfonyl; especially preferably, Lg is methanesulfonyl. 33. The linker-payload conjugate according to claim 32, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein the linker-payload conjugate is selected from the group consisting of: No. Structure 23 STI-A3 24 STI-F3 25 STI-F4 26 STI-G 27 STI-G3 28 STI-F1002 29 STI-F1001 30 STI-F1003 31 STI-F1004 32 STI-F1006 33 STI-F1010 34 STI-F1011 35 STI-F1012 36 STI-F1013 37 STI-F1014 38 STI-F1015 39 STI-F1018 40 STI-F1019 41 STI-G1001 42 STI-F1031 43 STI-F1034 44 STI-F1035 45 STI-F1043 34. A pharmaceutical composition comprising the antibody-drug conjugate according to any one of claims 1-23, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the compound according to any one of claims 21-31, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the linker-payload conjugate according to any one of claims 32-33, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; together with a pharmaceutically acceptable carrier, diluent or excipient. 35. The antibody-drug conjugate according to any one of claims 1-23, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the compound according to any one of claims 21-31, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the linker-payload conjugate according to any one of claims 32-33, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, for use in the treatment or prevention of cancer. 36. A method for preventing or treating cancer in a patient, comprising administering to the patient a therapeutically effective amount of the antibody-drug conjugate according to any one of claims 1-23, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the compound according to any one of claims 21-31, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the linker-payload conjugate according to any one of claims 32-33, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof. 37. Use of the antibody-drug conjugate according to any one of claims 1-23, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or of the compound according to any one of claims 21-31, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or of the linker-payload conjugate according to any one of claims 32-33, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, in the manufacture of a medicament for the treatment or prevention of cancer. 38. The antibody-drug conjugate or compound or linker-payload conjugate according to claim 35, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, or the method according to claim 36, or the use according to claim 37, wherein the cancer is a solid tumor, particularly lung cancer (e.g., small cell lung cancer, non-small cell lung cancer), liver cancer, digestive system cancers (e.g., intestinal cancer, gastric cancer, cardia cancer, esophageal cancer, appendiceal adenocarcinoma, colon cancer, rectal cancer, colorectal cancer, pancreatic cancer), bladder cancer, melanoma, breast cancer, ovarian cancer, cervical cancer, endometrial cancer, prostate cancer, basal cell carcinoma, cholangiocarcinoma, squamous cell carcinoma, thyroid cancer, brain cancer, head and neck cancer, peritoneal cancer, kidney cancer, urothelial carcinoma, testicular cancer, central nervous system tumors (e.g., glioma, glioblastoma such as glioblastoma multiforme, glioma, or sarcoma), choriocarcinoma, oral epidermoid carcinoma; or hematological malignancies, particularly leukemias (e.g., acute or chronic myeloid leukemia, acute or chronic granulocytic leukemia), lymphomas (e.g., Hodgkin's lymphoma, non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, acute B-cell lymphoma, follicular lymphoma), multiple myeloma; preferably, the cancer is ovarian cancer, colon cancer, lung adenocarcinoma, or oral epidermoid carcinoma.
Record as JSON
{
  "publication_number": "US2026102507A1",
  "country": "US",
  "kind": "A1",
  "title": "Camptothecin derivative for treating or preventing cancer and antibody-drug conjugate thereof",
  "abstract": "The present invention relates to camptothecin derivatives, their linker-payload conjugates, and antibody-drug conjugates, as well as pharmaceutically acceptable salts or esters, solvates, tautomers, stereoisomers, prodrugs, or isotopically labeled forms thereof, for use in the treatment or prevention of cancer. The invention further relates to a pharmaceutical composition comprising the camptothecin derivatives, their linker-payload conjugates, or antibody-drug conjugates; methods for the preparation of the same; and the use thereof.",
  "claims": [
    "1. An antibody-drug conjugate of formula (I): or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein: Ab is an antibody or antigen-binding fragment thereof; L 1 is each independently a linker unit; L 2 is each independently a linking unit selected from the group consisting of: - (CR m R n) t -(L M) 0−1 -(CH 2 CH 2 O) s - (CR m R n) t - CO -, - (CR m R n) t -L M -(CR m R n) t -(L M) 0−1 -L N -L M -(CH 2 O) s - (CR m R n) t - CO -, - (CR m R n) t -L M -(CR m R n) t - N(R p) - (CR m R n) t - N(R p) - (CR m R n) t - CO -, and - (CR m R n) t -L M -CH(R p) - CO -, wherein the - CO - terminus of L 2 is connected to L 3, and the other terminus of L 2 is connected to L 1, and wherein, R m and R n are each independently H or C 1-6 alkyl, L M is each independently - NH - CO - or - CO - NH -, L N is each independently - (CH 2 CH 2 O) m - (CH 2) t -, - (CH 2) t - (OCH 2 CH 2) m -, -(3- to 8-membered heteroarylene)-(CH 2) t - (OCH 2 CH 2) m, or - (OCH 2 CH 2) m - (CH 2) t -(3- to 8-membered heteroarylene)-, R p is each independently - CO - (CH 2 CH 2 O) m - CH 3 or - (CH 2) t -L M -(CH 2 CH 2 O) m - CH 3, and s and t are each independently 0, 1, 2, 3, 4, 5, 6, 7, or 8, and m is each independently 2, 3, 4, 5, 6, 7, or 8; L 3 is each independently an amino acid residue, a short peptide chain consisting of 2-10 amino acid residues, or - NH - (CH 2) p - CO -; L 4 is each independently a bond or a spacer unit; D is each independently a small molecule drug moiety derived from a compound of formula (II); wherein, R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 3-8 cycloalkyl) or - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the cycloalkyl and heterocycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH, amino, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - (CH 2) p - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; - NH - (CH 2) p - (CH═CH) - R a; or - COOH; R 2 and R 3 are each independently halogen, cyano, NO 2, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy, - NH - CO - (C 1-6 hydroxyalkyl), or NR a R b; or R 2 and R 3, together with the atoms to which they are attached, form a 4- to 8-membered heterocyclic group; R 4 is H or C 3-8 cycloalkyl, preferably H; R a and R b are each independently H, C 1-6 alkyl, - CO - (C 1-6 alkyl), - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino, and wherein the cycloalkyl is further optionally substituted with one or more substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; and p and q are each independently 0, 1, 2, 3, 4, 5, or 6; wherein D is linked to L 4 via R 1 or R 3, or via the oxygen from the hydroxy shown in formula (II); and n is an integer from 0 to 10, preferably an integer from 0 to 8. 2. The antibody-drug conjugate of formula (I) according to claim 1: or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein: Ab is an antibody or antigen-binding fragment thereof; L 1 is each independently a linker unit; L 2 is each independently a linking unit of the formula - (CH 2 CH 2 O) x - (CR m R n) y - CO -, wherein the - CO - terminus is connected to L 3 and the other terminus is connected to L 1, and wherein R m and R a are each independently H or C 1-6 alkyl, x is an integer from 0 to 5, y is an integer from 1 to 5; and the sum of x and y is ≤6; L 3 is each independently an amino acid residue, a short peptide chain consisting of 2-10 amino acid residues, or - NH - (CH 2) p - CO -; L 4 is each independently a bond or a spacer unit; D is each independently a small molecule drug moiety derived from a compound of formula (II); wherein, R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 3-8 cycloalkyl) or - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the cycloalkyl and heterocycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH, amino, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - (CH 2) p - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; - NH - (CH 2) p - (CH═CH) - R a; or - COOH; R 2 and R 3 are each independently halogen, cyano, NO 2, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy, - NH - CO - (C 1-6 hydroxyalkyl), or NR a R b; or R 2 and R 3, together with the atoms to which they are attached, form a 4- to 8-membered heterocyclic group; R 4 is H or C 3-8 cycloalkyl, preferably H; R a and R b are each independently H, C 1-6 alkyl, - CO - (C 1-6 alkyl), - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino, and wherein the cycloalkyl is further optionally substituted with one or more substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; and p and q are each independently 0, 1, 2, 3, 4, 5, or 6; wherein D is linked to L 4 via R 1 or R 3, or via the oxygen from the hydroxyl shown in formula (II); and n is an integer from 0 to 10, preferably an integer from 0 to 8. 3. The antibody-drug conjugate according to claim 1 or 2, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 cycloalkyl) or - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the cycloalkyl and the heterocycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of OH, SH, C 1-6 alkyl, and C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - (CH 2) p - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; - NH - (CH 2) p - (CH═CH) - R a; or - COOH; wherein R a and R b are each independently H, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 aminoalkyl, - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl optionally substituted with one or more substituents independently selected from the group consisting of hydroxy and C 1-6 hydroxyalkyl); preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH(C 1-6 aminoalkyl); - (CH 2) p - NH - (CH 2) q (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; - (CH 2) p - N(C 1-6 alkyl)(- SO 2 - C 1-6 alkyl); - CH═N(C 1-6 alkyl); - NH - CO - (C 1-6 hydroxyalkyl); - NH - CO - (C 3-8 hydroxycycloalkyl); - NH - CO - (CH 2) p - CH(OH) - (C 1-6 alkyl); - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); - NH - (CH 2) p - (CH═CH) - (C 1-6 hydroxyalkyl); or - COOH; or R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; wherein R a and R b are each independently H, C 1-6 alkyl, - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; preferably, R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 cycloalkyl); - (CH 2) p - (C 3-8 hydroxycycloalkyl); - (CH 2) p - (C 3-8 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; more preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; preferably wherein R a and R b are each independently H, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 aminoalkyl, - SO 2 - (C 1-6 alkyl), - (CH 2) q - (C 3-8 cycloalkyl), or - (CH 2) q - (C 3-8 hydroxycycloalkyl); further more preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH(C 1-6 aminoalkyl); - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl); - (CH 2) p - N(C 1-6 alkyl)(- SO 2 - C 1-6 alkyl); - CH═N(C 1-6 alkyl); - NH - CO - (C 1-6 hydroxyalkyl); - NH - CO - (C 3-8 hydroxycycloalkyl); - NH - CO - (CH 2) p - CH(OH) - (C 1-6 alkyl); - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); or - COOH. 4. The antibody-drug conjugate according to claim 1 or 2, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is H, C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - (CH 2) p - (NH 2), - (CH 2) p - NH(C 1-6 alkyl), - (CH 2) p - NH(C 1-6 hydroxyalkyl), - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); preferably, R 1 is H, C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - NH 2, - (CH 2) p - NH(C 1-6 alkyl), - NH(C 1-6 hydroxyalkyl), - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), or - NH - CO - CH(OH) - (C 3-8 cycloalkyl); more preferably, R 1 is H, C 1-6 alkyl, - CH 2 - (C 1-6 alkylthio), - NH 2, - CH 2 - NH(C 1-6 alkyl), - NH(C 1-6 hydroxyalkyl), - CH 2 - NH - CH 2 - (C 3-8 cycloalkyl), or - NH - CO - CH(OH) - (C 3-8 cycloalkyl). 5. The antibody-drug conjugate according to claim 1 or 2, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - (CH 2) p - NH(C 1-6 alkyl), or - (CH 2) p - NH(C 1-6 hydroxyalkyl); preferably, R 1 is C 1-6 alkyl, - CH 2 - (C 1-6 alkylthio), - NH(C 1-6 alkyl), or - NH(C 1-6 hydroxyalkyl). 6. The antibody-drug conjugate according to claim 1 or 2, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - NH 2, - (CH 2) p - NH(C 1-6 alkyl), - (CH 2) p - NH(C 1-6 hydroxyalkyl), - NH - CO - (C 1-6 hydroxyalkyl), or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); preferably, R 1 is C 1-6 alkyl, - NH 2, - (CH 2) p - NH(C 1-6 alkyl), - (CH 2) p - NH(C 1-6 hydroxyalkyl), or - NH - CO - (C 1-6 hydroxyalkyl). 7. The antibody-drug conjugate according to claim 1 or 2, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is C 1-6 alkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH - (CH 2) q (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; or - NH - (CH 2) p - (CH═CH) - (C 1-6 hydroxyalkyl); or, R 1 is C 1-6 alkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; - NH - CO - (C 1-6 hydroxyalkyl); or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); or, R 1 is C 1-6 alkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; - NH - CO - (C 1-6 hydroxyalkyl); or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); or, R 1 is C 1-6 alkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); or, R 1 is C 1-6 alkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - NH(C 1-6 hydroxyalkyl); or - (CH 2) p - NH - (CH 2) q (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl. 8. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 2 is a halogen, preferably fluorine. 9. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 3 is C 1-6 alkyl, C 1-6 alkoxy, halogen, cyano, - NH 2, - NH - CO - (C 1-6 hydroxyalkyl), or NO 2; preferably, R 3 is C 1-6 alkyl, halogen, - NH 2, - NH - CO - (C 1-6 hydroxyalkyl), or NO 2; or, R 3 is halogen, cyano, NO 2, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy, or NR a R b, wherein R a and R b are each independently H, C 1-6 alkyl, - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; preferably, R 3 is C 1-6 alkyl, C 1-6 alkoxy, halogen, cyano, - NH 2 or NO 2; more preferably, R 3 is C 1-6 alkyl, halogen, - NH 2 or NO 2; or, R 3 is C 1-6 alkyl or NR a R b, wherein R a and R b are each independently H or - CO - (C 1-6 alkyl), wherein the alkyl is optionally substituted with one or more OH groups; or, R 3 is C 1-6 alkyl, - NH 2 or - NH - CO - (CH 2 OH), preferably R 3 is C 1-6 alkyl or - NH - CO - (CH 2 OH); or R 3 is C 1-6 alkyl. 10. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 2 and R 3, together with the atoms to which they are attached, form a 4- to 8-membered heterocyclic group containing N, O or S as a heteroatom, such as dioxolane. 11. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein D is connected to L 4 via a nitrogen or oxygen atom in R 1 or R 3, or via the oxygen atom from hydroxy shown in formula (II), for example, through an amide bond, an aminomethyl ether bond, or a carbamate bond. 12. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein D is a moiety selected from the following: No. Structure 1′ 2′ STI-A-6′ 3′ 4′ STI-A2′ 5′ 6′ STI-E-05′ 7′ 8′ STI-F-8′ 9′ STI-F2′ 10′ STI-F-03c-1′ 11′ STI-G1′ 12′ STI-G03′ 13′ STI-G2-06c′ 14′ STI-G2′ 15′ STI-D′ 16′ STI-F′ 17′ STI-F6′ 18′ STI-F7′ 19′ STI-F13′ 20′ STI-G4′ 21′ SIT-F12R′ 22′ STI-F10′ P1′ STI-F5′ P2′ STI-F8′ P3′ STI-F14′ P4′ STI-F15′ P5′ STI-F17′ P6′ STI-F18′ P7′ STI-G5′ 13. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 1 is each independently: preferably more preferably wherein position 1 is connected to Ab, and position 2 is connected to L 2. 14. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 2 is each independently a linking unit selected from the group consisting of: - (CH 2) t -(L M) 0−1 -(CH 2 CH 2 O) s - (CH 2) t - CO -, - (CH 2) t -L M -(CH 2) t -(L M) 0−1 -L N -L M -(CH 2 O) s - (CH 2) t - CO -, - (CH 2) t -L M -(CH 2) t - N(R p) - (CH 2) t - N(R p) - (CH 2) t - CO -, and (CH 2) t -L M -CH(R p) - CO -, wherein the - CO - terminus of L 2 is connected to L 3, and the other terminus of L 2 is connected to L 1. 15. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 2 is each independently a linking unit selected from the group consisting of: - (CH 2) t - (CH 2 CH 2 O) s - (CH 2) t - CO -, - (CH 2) t - CO - NH - (CH 2 CH 2 O) s - (CH 2) t - CO -, - (CH 2) t - NH - CO - (CH 2 CH 2 O) s - (CH 2) t - CO -, - (CH 2) t - CO - NH - (CH 2) t -(3- to 8-membered heteroarylene)-(CH 2) t - (OCH 2 CH 2) m - NH - CO - (CH 2 O) - (CH 2) t - CO -, - (CH 2) t - CO - NH - (CH 2) t - NH - CO - (CH 2 CH 2 O) m - (CH 2) t - NH - CO - (CH 2 O) - (CH 2) t - CO -, - (CH 2) t - CO - NH - (CH 2) t - NH - CO - (CH 2) t - (OCH 2 CH 2) m - NH - CO - (CH 2 O) - (CH 2) t - CO -, - (CH 2) t - NH - CO - (CH 2) t - N(R p) - (CH 2) t - N(R p) - (CH 2) t - CO -, - (CH 2) t - CO - NH - (CH 2) t - N(R p) - (CH 2) t - N(R p) - (CH 2) t - CO -, or - (CH 2) t - CO - NH - CH(R p) - CO - or - (CH 2) t - NH - CO - CH(R p) - CO -, wherein the - CO - terminus of L 2 is connected to L 3, and the other terminus of L 2 is connected to L 1. 16. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 3 is each independently an amino acid residue, a short peptide chain consisting of 2-6 amino acid residues, or - NH - (CH 2) p - CO -, wherein p is 0, 1, 2, 3, 4, 5, or 6; preferably, the amino acid is selected from the group consisting of glycine (Gly), alanine (Ala), valine (Val), phenylalanine (Phe), citrulline (Cit), lysine (Lys) and asparagine (Asn); for example, L 3 is Gly-Gly-Phe-Gly, Val-Ala, Phe-Lys, or Lys. 17. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 4 is each independently a bond, preferably a bond, more preferably wherein position 1 is connected to L 3 and position 2 is connected to D. 18. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein: L 1 is each independently: preferably more preferably wherein position 1 is connected to Ab, and position 2 is connected to L 2; L 2 is each independently a linking unit of the formula - (CH 2 CH 2 O) x - (CH 2) y - CO -, wherein the - CO - terminus is connected to L 3 and the other terminus is connected to L 1, and wherein x is an integer from 0 to 5, y is an integer from 1 to 5, and x+y≤6; preferably, L 2 is - (CH 2) - CO -, - (CH 2) 2 - CO -, - (CH 2) 3 - CO -, - (CH 2) 4 - CO -, - (CH 2) 5 - CO -, - (CH 2) 6 - CO -, - (CH 2 CH 2 O) - (CH 2) - CO -, - (CH 2 CH 2 O) - (CH 2) 2 - CO -, - (CH 2 CH 2 O) - (CH 2) 3 - CO -, - (CH 2 CH 2 O) - (CH 2) 4 - CO -, - (CH 2 CH 2 O) - (CH 2) 5 - CO -, - (CH 2 CH 2 O) 2 - (CH 2) - CO -, - (CH 2 CH 2 O) 2 - (CH 2) 2 - CO -, - (CH 2 CH 2 O) 2 - (CH 2) 3 - CO -, - (CH 2 CH 2 O) 2 - (CH 2) 4 - CO -, - (CH 2 CH 2 O) 3 - (CH 2) - CO -, - (CH 2 CH 2 O) 3 - (CH 2) 2 - CO -, - (CH 2 CH 2 O) 3 - (CH 2) 3 - CO -; more preferably, L 2 is each independently - (CH 2) 5 - CO - or - (CH 2 CH 2 O) 3 - (CH 2) 2 - CO -; L 3 is each independently an amino acid residue, a short peptide chain consisting of 2-6 amino acid residues, or - NH - (CH 2) p - CO -, wherein p is 0, 1, 2, 3, 4, 5, or 6; preferably, the amino acid is selected from the group consisting of glycine (Gly), alanine (Ala), valine (Val), phenylalanine (Phe), citrulline (Cit), lysine (Lys) and asparagine (Asn); for example, L 3 is Gly-Gly-Phe-Gly, Val-Cit, Val-Ala, Phe-Lys, Val-Lys, Ala-Ala-Ala, Ala-Ala-Asn, or - NH - (CH 2) 2 - CO -; and L 4 is each independently a bond, wherein position 1 is connected to L 3 and position 2 is connected to D. 19. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein the -L 1 -L 2 -L 3 -L 4 - moiety is each independently selected from the group consisting of: wherein position 1 is connected to Ab, and position 2 is connected to D. 20. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein the -L 1 -L 2 -L 3 -L 4 -D moiety is each independently selected from: No. Structure 23′ STI-A3′ 24′ STI-F3′ 25′ STI-F4′ 26′ STI-G′ 27′ STI-G3′ 28′ STI-F1002′ 29′ STI-F1001′ 30′ STI-F1003′ 31′ STI-F1004′ 32′ STI-F1006 33′ STI-F1010 34′ STI-F1011 35′ STI-F1012 36′ STI-F1013 37′ STI-F1014 38′ STI-F1015 39′ STI-F1018 40′ STI-F1019 41′ STI-G1001 42′ STI-F1031 43′ STI-F1034 44′ STI-F1035 45′ STI-F1043 wherein position 1 represents the point of attachment to Ab. 21. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein Ab is an antibody or an antigen-binding fragment thereof that binds to a tumor cell surface antigen; for example, an anti-Her2 antibody or an antigen-binding fragment thereof and/or an anti-FRα antibody or an antigen-binding fragment thereof; in particular, Ab is farletuzumab or an antigen-binding fragment thereof and/or trastuzumab or an antigen-binding fragment thereof. 22. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein the antibody-drug conjugate is selected from the group consisting of: Name Structure Fa-ADC1 Fa-ADC2 Fa-ADC3 Fa-ADC4 Fa-ADC5 Fa-ADC6 Tra-ADC7 Tra-ADC8 Tra-ADC9 Tra-ADC10 Tra-ADC11 Tra-ADC12 Tra-ADC13 Tra-ADC14 Tra-ADC15 Tra-ADC16 Tra-ADC17 Tra-ADC18 Tra-ADC19 Tra-ADC20 wherein, in Fa-ADCs, mAb represents farletuzumab; in Tra-ADCs, mAb represents trastuzumab, and n is 0, 1, 2, 3, 4, 5, 6, 7, or 8. 23. The antibody-drug conjugate according to any one of the preceding claims, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, which has an average DAR selected from any value within the range from 1.0 to 10.0, preferably has an average DAR selected from any value within the range from 2.0 to 8.0, and more preferably has an average DAR selected from any value within the range from 6.0 to 8.0. 24. A compound of formula (II): or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein, R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 3-8 cycloalkyl) or - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the cycloalkyl and heterocycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH, amino, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - (CH 2) p - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; - NH - (CH 2) p - (CH═CH) - R a; or - COOH; R 2 and R 3 are each independently halogen, cyano, NO 2, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy, - NH - CO - (C 1-6 hydroxyalkyl), or NR a R b; or R 2 and R 3, together with the atoms to which they are attached, form a 4- to 8-membered heterocyclic group; R 4 is H or C 3-8 cycloalkyl, preferably H; R a and R b are each independently H, C 1-6 alkyl, - CO - (C 1-6 alkyl), - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino, and wherein the cycloalkyl is further optionally substituted with one or more substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 cyanoalkyl and C 1-6 aminoalkyl; and p and q are each independently 0, 1, 2, 3, 4, 5, or 6. 25. The compound according to claim 24, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein: R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 cycloalkyl) or - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the cycloalkyl and the heterocycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of OH, SH, C 1-6 alkyl, and C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - (CH 2) p - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; - NH - (CH 2) p - (CH═CH) - R a; or - COOH; wherein R a and R b are each independently H, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 aminoalkyl, - SO 2 - (C 1-6 alkyl), or - (CH 2) q (C 3-8 cycloalkyl optionally substituted with one or more substituents independently selected from the group consisting of hydroxy and C 1-6 hydroxyalkyl); preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 heterocycloalkyl), wherein the heterocycloalkyl is optionally substituted with one or more C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH(C 1-6 aminoalkyl); - (CH 2) p - NH - (CH 2) q (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents selected from C 1-6 hydroxyalkyl; - (CH 2) p - N(C 1-6 alkyl)(- SO 2 - C 1-6 alkyl); - CH═N(C 1-6 alkyl); - NH - CO - (C 1-6 hydroxyalkyl); - NH - CO - (C 3-8 hydroxycycloalkyl); - NH - CO - (CH 2) p - CH(OH) - (C 1-6 alkyl); - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); - NH - (CH 2) p - (CH═CH) - (C 1-6 hydroxyalkyl); or - COOH; or R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 3-8 cycloalkyl), wherein the cycloalkyl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; wherein R a and R b are each independently H, C 1-6 alkyl, - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q - (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; preferably, R 1 is: H; halogen; CN; OH; SH; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 3-8 cycloalkyl); - (CH 2) p - (C 3-8 hydroxycycloalkyl); - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; more preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NR a R b; - CH═NR a; - NH - CO - R a; - NH - CO - (CH 2) p - CH(OH) - R a; or - COOH; preferably wherein R a and R b are each independently H, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 aminoalkyl, - SO 2 - (C 1-6 alkyl), - (CH 2) q - (C 3-8 cycloalkyl), or - (CH 2) q - (C 3-8 hydroxycycloalkyl); further more preferably, R 1 is H; C 1-6 alkyl; C 1-6 haloalkyl; C 1-6 hydroxyalkyl; - (CH 2) p - (C 1-6 alkoxy); - (CH 2) p - (C 1-6 alkylthio); - (CH 2) p - NH 2; - (CH 2) p - NH(C 1-6 alkyl); - (CH 2) p - NH(C 1-6 hydroxyalkyl); - (CH 2) p - NH(C 1-6 aminoalkyl); - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl); - (CH 2) p - N(C 1-6 alkyl)(- SO 2 - C 1-6 alkyl); - CH═N(C 1-6 alkyl); - NH - CO - (C 1-6 hydroxyalkyl); - NH - CO - (C 3-8 hydroxycycloalkyl); - NH - CO - (CH 2) p - CH(OH) - (C 1-6 alkyl); - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); or - COOH. 26. The compound according to claim 24, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is H, C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - (CH 2) p - (NH 2), - (CH 2) p - NH(C 1-6 alkyl), - (CH 2) p - NH(C 1-6 hydroxyalkyl), - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), or - NH - CO - (CH 2) p - CH(OH) - (C 3-8 cycloalkyl); preferably, R 1 is H, C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - NH 2, - (CH 2) p - NH(C 1-6 alkyl), - NH(C 1-6 hydroxyalkyl), - (CH 2) p - NH - (CH 2) q - (C 3-8 cycloalkyl), or - NH - CO - CH(OH) - (C 3-8 cycloalkyl); more preferably, R 1 is H, C 1-6 alkyl, - CH 2 - (C 1-6 alkylthio), - NH 2, - CH 2 - NH(C 1-6 alkyl), - NH(C 1-6 hydroxyalkyl), - CH 2 - NH - CH 2 - (C 3-8 cycloalkyl), or - NH - CO - CH(OH) - (C 3-8 cycloalkyl). 27. The compound according to claim 24, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 1 is C 1-6 alkyl, - (CH 2) p - (C 1-6 alkylthio), - (CH 2) p - NH(C 1-6 alkyl), or - (CH 2) p - NH(C 1-6 hydroxyalkyl); preferably, R 1 is C 1-6 alkyl, - CH 2 - (C 1-6 alkylthio), - NH(C 1-6 alkyl), or - NH(C 1-6 hydroxyalkyl). 28. The compound according to any one of claims 24-27, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 2 is a halogen, preferably fluorine. 29. The compound according to any one of claims 24-28, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 3 is C 1-6 alkyl, C 1-6 alkoxy, halogen, cyano, - NH 2, - NH - CO - (C 1-6 hydroxyalkyl), or NO 2; preferably, R 3 is C 1-6 alkyl, halogen, - NH 2, - NH - CO - (C 1-6 hydroxyalkyl), or NO 2; or, R 3 is halogen, cyano, NO 2, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy, or NR a R b, wherein R a and R b are each independently H, C 1-6 alkyl, - SO - (C 1-6 alkyl), - SO 2 - (C 1-6 alkyl), or - (CH 2) q (C 3-8 cycloalkyl), wherein the alkyl and the cycloalkyl are each optionally substituted with one or more substituents independently selected from the group consisting of halogen, CN, OH, SH and amino; preferably, R 3 is C 1-6 alkyl, C 1-6 alkoxy, halogen, cyano, - NH 2 or NO 2; more preferably, R 3 is C 1-6 alkyl, halogen, - NH 2 or NO 2. 30. The compound according to any one of claims 24-27, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein R 2 and R 3, together with the atoms to which they are attached, form a 4- to 8-membered heterocyclic group containing an oxygen, nitrogen or sulfur atom as a heteroatom, such as dioxolane. 31. The compound according to claim 24, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein the compound is selected from the group consisting of: No. Structure 1 STI-A-4 2 3 4 5 6 STI-E05 7 8 STI-F-8 9 10 STI-F-03c-1 11 STI-G1 12 STI-G03 13 STI-G2-06c 14 STI-G2 15 STI-D 16 STI-F 17 STI-F6 18 STI-F7 19 STI-F13 20 STI-G4 21 STI-F12R 22 STI-F10 P1 STI-F5 P2 STI-F8 P3 STI-F14 P4 STI-F15 P5 STI-F17 P6 STI-F18 P7 STI-G5 32. A linker-payload conjugate of formula (III): or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein L 1, L 2, L 3, L 4 and D are as defined in any one of claims 1-20, and wherein when L 1 is Lg and L 1 together form when L 1 is not Lg is a leaving group; preferably, Lg is halogen, sulfonyl (e.g., methanesulfonyl, p-toluenesulfonyl), sulfonyloxy (e.g., methanesulfonyloxy, CF 3 SO 3 -, p-toluenesulfonyloxy), a tertiary-ammonium group (e.g., Me 3 N + or Et 3 N +), or a diazonium group; more preferably, Lg is F, Cl, Br, or methanesulfonyl; especially preferably, Lg is methanesulfonyl. 33. The linker-payload conjugate according to claim 32, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, wherein the linker-payload conjugate is selected from the group consisting of: No. Structure 23 STI-A3 24 STI-F3 25 STI-F4 26 STI-G 27 STI-G3 28 STI-F1002 29 STI-F1001 30 STI-F1003 31 STI-F1004 32 STI-F1006 33 STI-F1010 34 STI-F1011 35 STI-F1012 36 STI-F1013 37 STI-F1014 38 STI-F1015 39 STI-F1018 40 STI-F1019 41 STI-G1001 42 STI-F1031 43 STI-F1034 44 STI-F1035 45 STI-F1043 34. A pharmaceutical composition comprising the antibody-drug conjugate according to any one of claims 1-23, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the compound according to any one of claims 21-31, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the linker-payload conjugate according to any one of claims 32-33, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; together with a pharmaceutically acceptable carrier, diluent or excipient. 35. The antibody-drug conjugate according to any one of claims 1-23, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the compound according to any one of claims 21-31, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the linker-payload conjugate according to any one of claims 32-33, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, for use in the treatment or prevention of cancer. 36. A method for preventing or treating cancer in a patient, comprising administering to the patient a therapeutically effective amount of the antibody-drug conjugate according to any one of claims 1-23, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the compound according to any one of claims 21-31, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or the linker-payload conjugate according to any one of claims 32-33, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof. 37. Use of the antibody-drug conjugate according to any one of claims 1-23, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or of the compound according to any one of claims 21-31, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof; or of the linker-payload conjugate according to any one of claims 32-33, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, in the manufacture of a medicament for the treatment or prevention of cancer. 38. The antibody-drug conjugate or compound or linker-payload conjugate according to claim 35, or a pharmaceutically acceptable salt or ester, solvate, tautomer, stereoisomer, prodrug, or isotopically labeled form thereof, or the method according to claim 36, or the use according to claim 37, wherein the cancer is a solid tumor, particularly lung cancer (e.g., small cell lung cancer, non-small cell lung cancer), liver cancer, digestive system cancers (e.g., intestinal cancer, gastric cancer, cardia cancer, esophageal cancer, appendiceal adenocarcinoma, colon cancer, rectal cancer, colorectal cancer, pancreatic cancer), bladder cancer, melanoma, breast cancer, ovarian cancer, cervical cancer, endometrial cancer, prostate cancer, basal cell carcinoma, cholangiocarcinoma, squamous cell carcinoma, thyroid cancer, brain cancer, head and neck cancer, peritoneal cancer, kidney cancer, urothelial carcinoma, testicular cancer, central nervous system tumors (e.g., glioma, glioblastoma such as glioblastoma multiforme, glioma, or sarcoma), choriocarcinoma, oral epidermoid carcinoma; or hematological malignancies, particularly leukemias (e.g., acute or chronic myeloid leukemia, acute or chronic granulocytic leukemia), lymphomas (e.g., Hodgkin's lymphoma, non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, acute B-cell lymphoma, follicular lymphoma), multiple myeloma; preferably, the cancer is ovarian cancer, colon cancer, lung adenocarcinoma, or oral epidermoid carcinoma."
  ],
  "cpc": [
    "A61K 47/68037",
    "A61K 47/6849",
    "A61K 47/6855",
    "A61K 47/6889",
    "A61P 35/00",
    "C07K 16/28",
    "C07K 16/32"
  ],
  "filing_date": "2025-12-15",
  "publication_date": "2026-04-16",
  "priority_date": "2023-06-13",
  "application_number": "US-202519420112-A"
}

Record 59 of 5,000 in Patents full text (MLC-0201). Request the full dataset.