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merestinib + cisplatin + gemcitabine
- Development stage
- Phase 2
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Merestinib + cisplatin + gemcitabine is a combination regimen investigated primarily for advanced or metastatic biliary tract cancer. **Merestinib** is an oral small-molecule multikinase inhibitor with antiproliferative and antiangiogenic properties; it inhibits several receptor tyrosine kinases including MET, MST1R, AXL, ROS1, PDGFRA, FLT3, TEK, DDR1, DDR2, MERTK, TYRO3, and the TRK family (TRKA/B/C), as well as serine/threonine kinases MKNK1/2. **Cisplatin** is a platinum-based chemotherapeutic that crosslinks DNA to induce apoptosis, and **gemcitabine** is a nucleoside analog that inhibits DNA synthesis. The combination is being investigated as first-line therapy for patients with advanced or metastatic biliary tract adenocarcinoma. Clinical trials showed a tolerable safety profile but no significant improvement in progression-free survival compared to cisplatin/gemcitabine alone in unselected patients.
- Other names
- merestinib + gemcitabine + cisplatin
02
Targets
AXL (AXL receptor tyrosine kinase)DNADNA polymerase familyMET (Mesenchymal-epithelial transition factor receptor)MST1R (Recepteur d'origine nantais)Trk (Trk receptor family)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)RNR (Ribonucleotide reductase)DDR1 (Discoidin domain receptor 1)DDR2 (Discoidin domain receptor tyrosine kinase 2)FLT3 (Fms related receptor tyrosine kinase 3)MKNK1 (Mitogen‑activated protein kinase‑interacting serine/threonine-protein kinase 1)MKNK2 (MAP kinase-interacting serine/threonine-protein kinase 2)MERTK (MER proto-oncogene, tyrosine kinase)NTRK1 (Tropomyosin-related receptor kinase A)NTRK2 (Tropomyosin-related kinase receptor type B)NTRK3 (Tropomyosin receptor kinase C)PDGFRA (Platelet-derived growth factor receptor alpha)TEK (Tie2)
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