Drug intelligence / Profile preview

gemcitabine + oxaliplatin + tislelizumab + regorafenib

Development stage
Preclinical
Lead developer
BeiGene
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of four drugs: **gemcitabine** (a nucleoside analog chemotherapy), **oxaliplatin** (a platinum-based chemotherapy), **tislelizumab** (a monoclonal antibody targeting PD-1 immune checkpoint), and **regorafenib** (a small molecule multikinase inhibitor). This combination aims to synergistically enhance antitumor efficacy by combining cytotoxic chemotherapy (gemcitabine, oxaliplatin), immune checkpoint blockade (tislelizumab), and angiogenesis/kinase inhibition (regorafenib). Clinical studies have explored similar combinations for aggressive cancers such as advanced or metastatic biliary tract cancer (BTC), aiming to improve response rates and survival outcomes. The regimen has shown promising efficacy and manageable toxicities in studies of related triplet and quadruplet combinations, though data specifically on all four together are emerging.

02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)DNAFGFR1 (Fibroblast growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDCD1 (Programmed cell death protein 1 receptor)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)RNR (Ribonucleotide reductase)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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