Drug intelligence / Profile preview

trifluridine + tipiracil + anlotinib

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

This drug is a combination of three small molecules: trifluridine, tipiracil (together known as TAS-102), and anlotinib. Trifluridine is a nucleoside analog that incorporates into DNA, causing DNA dysfunction and inhibiting tumor cell proliferation. Tipiracil inhibits thymidine phosphorylase, preventing the degradation of trifluridine and increasing its bioavailability and cytotoxicity. Anlotinib is a multi-targeted tyrosine kinase inhibitor that blocks vascular endothelial growth factor receptors (VEGFR 1/2/3), fibroblast growth factor receptors (FGFR 1–4), platelet-derived growth factor receptors (PDGFR α/β), and c-Kit, thereby inhibiting angiogenesis and tumor cell proliferation. This combination has been explored as a third-line treatment for metastatic colorectal cancer after failure of standard therapies[1][3]. Early clinical evidence suggests promising efficacy with manageable toxicity in this setting[1].

Brand names
Lonsurf + Fukanghua
Other names
TAS-102 + anlotinibtrifluridine/tipiracil + anlotinib
02

Targets

FGFR4 (Fibroblast growth factor receptor 4)PDGFRA (Platelet-derived growth factor receptor alpha)TS (Thymidylate synthase)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRB (Platelet-derived growth factor receptor beta)FGFR3 (Fibroblast growth factor receptor 3)TYMP (Thymidine phosphorylase)VEGFR-1 (Vascular endothelial growth factor receptor 1)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)KIT (c-KIT proto-oncogene receptor tyrosine kinase)FGFR1 (Fibroblast growth factor receptor 1)

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