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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
BRAF V600EDPYD (Dihydropyrimidine dehydrogenase)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)OPRT (Orotidine 5'-phosphate decarboxylase)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)TS (Thymidylate synthase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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