Trifluridine and Tipiracil Hydrochloride

Preferred Label : Trifluridine and Tipiracil Hydrochloride;

NCIt synonyms : Tipiracil Hydrochloride Mixture with Trifluridine; Thymidine, Alpha,alpha,alpha-trifluoro-, Mixt. with 5-Chloro-6-((2-imino-1-pyrrolidinyl)methyl)-2,4(1H,3H)-pyrimidinedione Monohydrochloride; Trifluridine/Tipiracil Hydrochloride Combination Agent TAS-102; Trifluridine/Tipiracil; FTD-TPI;

NCIt related terms : Trifluridine and tipiracil;

NCIt definition : 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.;

CAS number : 733030-01-8;

Drug name : Lonsurf;

Molecule name : TAS-102; TAS 102;

Codes from synonyms : 516;

Origin ID

C102554;

UMLS CUI

C4682386;

Automatic exact mappings (from CISMeF team)
- trifluridine tipiracil drug combination [MeSH Supplementary Concept]
- trifluridine tipiracil drug combination [MeSH concept]
Semantic type(s)
- Nucleic Acid, Nucleoside, or Nucleotide [UMLS semantic type]
- Pharmacologic Substance [UMLS semantic type]
concept_is_in_subset
- CTRP Agent Terminology [NCIt concept]
- CTRP Terminology [NCIt concept]
- GDC Terminology [NCIt concept]
- GDC Therapeutic Agent Terminology [NCIt concept]
- GDC Value Terminology [NCIt concept]
- HemOnc Agent Terminology [NCIt concept]
- NCI Drug Dictionary Terminology [NCIt concept]
- NCIt Antineoplastic Agent Terminology [NCIt concept]
has_target
- Thymidine Phosphorylase [NCIt concept]
- Thymidylate Synthase [NCIt concept]
is_component_of_chemotherapy_regimen
- Bevacizumab/Tipiracil/Trifluridine Regimen [NCIt concept]
- Tipiracil/Trifluridine Regimen [NCIt concept]

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