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

VEGFR2 (Vascular endothelial growth factor receptor 2)RNR (Ribonucleotide reductase)TS (Thymidylate synthase)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))DNAOPRT (Orotidine 5'-phosphate decarboxylase)VEGFR3 (Vascular endothelial growth factor receptor 3)BRAF (B-Raf proto-oncogene, serine/threonine kinase)DPYD (Dihydropyrimidine dehydrogenase)

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