Drug intelligence / Profile preview

anlotinib + tegafur + gimeracil + oteracil

Development stage
Unknown
Lead developer
Chia Tai-Tianqing Pharmaceutical Group
Modality
Small Molecules
Administration
Oral
01

Overview

Anlotinib + tegafur + gimeracil + oteracil is a combination therapy being investigated for the treatment of advanced pancreatic cancer. Anlotinib is a small-molecule multi-targeted tyrosine kinase inhibitor (TKI) that suppresses tumor angiogenesis and proliferation by inhibiting VEGFR1/2/3, FGFR1-4, PDGFRα/β, and c-Kit. The other components—tegafur, gimeracil, and oteracil—constitute the oral fluoropyrimidine S-1. Tegafur is a prodrug of 5-fluorouracil (5-FU); gimeracil inhibits dihydropyrimidine dehydrogenase (DPD) to prevent the degradation of 5-FU; and oteracil inhibits orotate phosphoribosyltransferase (OPRT) to reduce 5-FU-induced gastrointestinal toxicity. This combination aims to provide synergistic antitumor activity by combining anti-angiogenic effects with potent, well-tolerated chemotherapy. It is primarily being developed by the Cancer Hospital Affiliated to Guangxi Medical University for patients who have failed first-line chemotherapy.

Brand names
Focus V
Other names
Anlotinib plus S-1Anlotinib + S-1
02

Targets

DPYD (Dihydropyrimidine dehydrogenase)OPRT (Orotidine 5'-phosphate decarboxylase)TS (Thymidylate synthase)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)

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