Drug intelligence / Profile preview

gemcitabine + S-1 + sorafenib

Development stage
Unknown
Lead developer
Shanghai Sixth People’s Hospital
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Gemcitabine + S-1 + sorafenib is a combination chemotherapy and targeted therapy regimen investigated for the treatment of advanced hilar cholangiocarcinoma (Klatskin tumor). This regimen combines two antimetabolite chemotherapeutic agents, gemcitabine and S-1 (a fixed-dose combination of tegafur, gimeracil, and oteracil), with sorafenib, a multi-kinase inhibitor. Gemcitabine and the active metabolite of S-1 (5-fluorouracil) inhibit DNA synthesis and repair by disrupting nucleotide metabolism, while sorafenib targets tumor angiogenesis and cell signaling pathways by inhibiting VEGFR, PDGFR, and the Raf/MEK/ERK pathway. This triplet combination, primarily studied by researchers at Shanghai Sixth People's Hospital, aims to provide synergistic anti-tumor activity in biliary tract cancers, which are often resistant to standard monotherapies.

Brand names
Nexavar
Other names
GS plus sorafenibGSS regimen
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)DNADPYD (Dihydropyrimidine dehydrogenase)OPRT (Orotidine 5'-phosphate decarboxylase)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RNR (Ribonucleotide reductase)TS (Thymidylate synthase)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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