{"meta":{"totalResults":1,"from":0},"results":[{"aliases":[{"type":"USBrandName","name":"Lonsurf"},{"type":"Synonym","name":"trifluridine and tipiracil"},{"type":"Synonym","name":"trifluridine/tipiracil hydrochloride"},{"type":"CodeName","name":"TAS-102"},{"type":"Synonym","name":"trifluridine/tipiracil hydrochloride combination agent TAS-102"},{"type":"CASRegistryName","name":"733030-01-8"},{"type":"CodeName","name":"TAS 102"},{"type":"ChemicalStructureName","name":"thymidine, alpha,alpha,alpha-trifluoro-, mixt. with 5-chloro-6-((2-imino-1-pyrrolidinyl)methyl)-2,4(1H,3H)-pyrimidinedione monohydrochloride"},{"type":"Synonym","name":"tipiracil hydrochloride mixture with trifluridine"},{"type":"Synonym","name":"trifluridine/tipiracil"}],"definition":{"html":"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.","text":"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."},"drugInfoSummaryLink":{"uri":"https://www.cancer.gov/about-cancer/treatment/drugs/trifluridine-tipiracilhydrochloride","text":"Trifluridine and Tipiracil Hydrochloride"},"nciConceptId":"C102554","nciConceptName":"Trifluridine and Tipiracil Hydrochloride","termId":734891,"name":"trifluridine and tipiracil hydrochloride","firstLetter":"t","type":"DrugTerm","termNameType":"PreferredName","prettyUrlName":"trifluridine-and-tipiracil-hydrochloride"}],"links":null}