Simmitecan hydrochloride
Term · Oncology and biomedicine · MLC-T-ONC-016742
The hydrochloride salt form of simmitecan, an ester prodrug of chimmitecan, a 9-alkyl substituted camptothecin derivative with potential antineoplastc activity. Upon intravenous administration, simmitecan is hydrolyzed by carboxylesterase and the activated form, chimmitecan, is produced. Chimmitecan inhibits topoisomerase I, stabilizes covalent topoisomerase I-DNA complexes, and inhibits the religation of topoisomerase I-mediated single-strand DNA breaks. Futhermore, the covalent topoisomerase I-DNA complexes interfere and block the DNA replication machinery, resulting in the production of potentially lethal double-strand DNA breaks. This leads to an inhibition of DNA replication and the induction of apoptosis. The modification at position 9 yields improved cytotoxicity compared to some other camptothecin analogues.
| Identifier | MLC-T-ONC-016742 |
|---|---|
| Field | Oncology and biomedicine |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-016742",
"term": "Simmitecan hydrochloride",
"field": "Oncology and biomedicine",
"definition": "The hydrochloride salt form of simmitecan, an ester prodrug of chimmitecan, a 9-alkyl substituted camptothecin derivative with potential antineoplastc activity. Upon intravenous administration, simmitecan is hydrolyzed by carboxylesterase and the activated form, chimmitecan, is produced. Chimmitecan inhibits topoisomerase I, stabilizes covalent topoisomerase I-DNA complexes, and inhibits the religation of topoisomerase I-mediated single-strand DNA breaks. Futhermore, the covalent topoisomerase I-DNA complexes interfere and block the DNA replication machinery, resulting in the production of potentially lethal double-strand DNA breaks. This leads to an inhibition of DNA replication and the induction of apoptosis. The modification at position 9 yields improved cytotoxicity compared to some other camptothecin analogues.",
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/simmitecan-hydrochloride/"
}
Record 14,999 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.