Drug intelligence / Profile preview

sorafenib + TS-1

Development stage
Preclinical
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

Sorafenib + TS-1 is a combination therapy consisting of two small molecule drugs used primarily in oncology. Sorafenib is an oral multikinase inhibitor that targets Raf kinase, vascular endothelial growth factor receptors 1, 2, and 3 (VEGFR), and platelet-derived growth factor receptor beta (PDGFRβ). It inhibits tumor cell proliferation and angiogenesis. TS-1 (also known as S-1) is an oral fluoropyrimidine derivative composed of tegafur (a prodrug of 5-fluorouracil), gimeracil (an inhibitor of dihydropyrimidine dehydrogenase to increase 5-FU bioavailability), and oteracil (to reduce gastrointestinal toxicity). The combination has shown synergistic antitumor activity in preclinical studies, with evidence suggesting enhanced cytotoxicity against hepatocellular carcinoma cells compared to either agent alone[1][2]. This regimen has been investigated for advanced or unresectable hepatocellular carcinoma.

Brand names
Nexavar
Other names
sorafenib + S-1sorafenib + tegafur/gimeracil/oteracil
02

Targets

RAF1 (c-Raf-1 (Y340D/Y341D))PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)TS (Thymidylate synthase)OPRT (Orotidine 5'-phosphate decarboxylase)BRAF V600EVEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR2 (Vascular endothelial growth factor receptor 2)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)DPYD (Dihydropyrimidine dehydrogenase)

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