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LY2801653 + cisplatin
- Development stage
- Phase 1
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
**LY2801653 + cisplatin** is an investigational combination therapy involving merestinib (LY2801653), a potent, orally bioavailable, small-molecule multi-kinase inhibitor targeting MET, MST1R (RON), and other receptor tyrosine kinases, and cisplatin, a platinum-based chemotherapy agent. Merestinib inhibits MET signaling, which is implicated in tumor growth, metastasis, and resistance to therapy, and is being evaluated in combination with cisplatin—an agent that induces DNA crosslinks and damage, leading to apoptosis—in various solid tumors, especially advanced or metastatic biliary tract cancer. The combination has shown tolerable safety and anti-tumor activity in early phase clinical studies in advanced cancers[2][5][6].
- Other names
- merestinib + cisplatin
02
Targets
AXL (AXL receptor tyrosine kinase)DDR1 (Discoidin domain receptor 1)DDR2 (Discoidin domain receptor tyrosine kinase 2)FLT3 (Fms related receptor tyrosine kinase 3)MET (Mesenchymal-epithelial transition factor receptor)MKNK1 (Mitogen‑activated protein kinase‑interacting serine/threonine-protein kinase 1)MKNK2 (MAP kinase-interacting serine/threonine-protein kinase 2)PDGFRA (Platelet-derived growth factor receptor alpha)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)TEK (Angiopoietin-1 receptor)DNAMST1R (Recepteur d'origine nantais)
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