Trifluridine and tipiracil hydrochloride

{
  "id": "MLC-T-ONC-008902",
  "term": "Trifluridine and tipiracil hydrochloride",
  "field": "Oncology and biomedicine",
  "definitions": [
    "A combination of two drugs used alone or with bevacizumab to treat adults with certain types of colorectal cancer, stomach cancer, or gastroesophageal junction cancer. It is used in patients whose cancer has spread to other parts of the body and has already been treated with other anticancer treatments. It is also being studied in the treatment of other types of cancer. Trifluridine and tipiracil hydrochloride stops cells from making DNA, which may help keep cancer cells from growing and may kill them. It is a type of antimetabolite and a type of thymidine phosphorylase inhibitor. Also called Lonsurf.",
    "An orally bioavailable combination agent composed of the cytotoxic pyrimidine analog trifluridine (5-trifluoro-2'-deoxythymidine or TFT) and a thymidine phosphorylase inhibitor (TPI) tipiracil hydrochloride, in a molar ratio of 1.0:0.5 (TFT:TPI), with potential antineoplastic activity. After oral administration of TAS-102, TFT is phosphorylated to the active monophosphate form TF-TMP, which binds covalently to the active site of thymidylate synthase, thereby reducing the nucleotide pool levels required for DNA replication. Furthermore, the triphosphate form TF-TTP can be incorporated into DNA, which induces DNA fragmentation and leads to the inhibition of tumor growth. TPI exhibits a dual effect: 1) an anti-angiogenic effect mediated through the inhibition of thymidine phosphorylase, which plays important role in nucleotide metabolism and a variety of development processes, including angiogenesis, 2) increased bioavailability of the normally short-lived antimetabolite TFT by preventing its degradation into the inactive form trifluorothymine (TF-Thy). The synergistic effect of the components in TAS-10 may demonstrate antitumor activity in 5-FU-resistant cancer cells."
  ],
  "synonyms": [
    "Lonsurf",
    "trifluridine and tipiracil",
    "trifluridine/tipiracil hydrochloride",
    "trifluridine/tipiracil hydrochloride combination agent TAS-102",
    "tipiracil hydrochloride mixture with trifluridine",
    "trifluridine/tipiracil"
  ],
  "references": [
    "NCI Dictionary of Cancer Terms",
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/trifluridine-and-tipiracil-hydrochloride/"
}