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- NCIT_C102554 IAO_0000115 "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." @default.
- NCIT_C102554 NCIT_A32 NCIT_C1909 @default.
- NCIT_C102554 NCIT_A7 NCIT_C17199 @default.
- NCIT_C102554 NCIT_A7 NCIT_C26148 @default.
- NCIT_C102554 NCIT_NHC0 "C102554" @default.
- NCIT_C102554 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C102554 NCIT_P107 "Trifluridine and Tipiracil Hydrochloride" @default.
- NCIT_C102554 NCIT_P108 "Trifluridine and Tipiracil Hydrochloride" @default.
- NCIT_C102554 NCIT_P207 "C1451803" @default.
- NCIT_C102554 NCIT_P210 "733030-01-8" @default.
- NCIT_C102554 NCIT_P302 "metastatic colorectal cancer; metastatic gastric or gastroesophageal junction (GEJ) adenocarcinoma" @default.
- NCIT_C102554 NCIT_P322 "CTRP" @default.
- NCIT_C102554 NCIT_P322 "GDC" @default.
- NCIT_C102554 NCIT_P329 "734891" @default.
- NCIT_C102554 NCIT_P330 "734891" @default.
- NCIT_C102554 NCIT_P375 "Trifluridine and Tipiracil Hydrochloride" @default.
- NCIT_C102554 NCIT_P399 "734891" @default.
- NCIT_C102554 normalizedInformationContent "92.730304365937428" @default.
- NCIT_C102554 referenceCount "3" @default.
- NCIT_C102554 hasExactSynonym "Lonsurf" @default.
- NCIT_C102554 hasExactSynonym "TAS 102" @default.
- NCIT_C102554 hasExactSynonym "TAS-102" @default.
- NCIT_C102554 hasExactSynonym "Thymidine, Alpha,alpha,alpha-trifluoro-, Mixt. with 5-Chloro-6-((2-imino-1-pyrrolidinyl)methyl)-2,4(1H,3H)-pyrimidinedione Monohydrochloride" @default.
- NCIT_C102554 hasExactSynonym "Tipiracil Hydrochloride Mixture with Trifluridine" @default.
- NCIT_C102554 hasExactSynonym "Trifluridine and Tipiracil Hydrochloride" @default.
- NCIT_C102554 hasExactSynonym "Trifluridine and Tipiracil" @default.
- NCIT_C102554 hasExactSynonym "Trifluridine/Tipiracil Hydrochloride Combination Agent TAS-102" @default.
- NCIT_C102554 hasExactSynonym "Trifluridine/Tipiracil" @default.
- NCIT_C102554 inSubset NCIT_C116977 @default.
- NCIT_C102554 inSubset NCIT_C116978 @default.
- NCIT_C102554 inSubset NCIT_C128784 @default.
- NCIT_C102554 inSubset NCIT_C157711 @default.
- NCIT_C102554 inSubset NCIT_C157712 @default.
- NCIT_C102554 inSubset NCIT_C176424 @default.
- NCIT_C102554 inSubset NCIT_C177537 @default.
- NCIT_C102554 type Class @default.
- NCIT_C102554 isDefinedBy ncit.owl @default.
- NCIT_C102554 label "Trifluridine and Tipiracil Hydrochloride" @default.
- NCIT_C102554 subClassOf NCIT_C102554 @default.
- NCIT_C102554 subClassOf NCIT_C1557 @default.
- NCIT_C102554 subClassOf NCIT_C1742 @default.
- NCIT_C102554 subClassOf NCIT_C186664 @default.
- NCIT_C102554 subClassOf NCIT_C1908 @default.
- NCIT_C102554 subClassOf NCIT_C1909 @default.
- NCIT_C102554 subClassOf NCIT_C272 @default.
- NCIT_C102554 subClassOf NCIT_C274 @default.