Drug intelligence / Profile preview

LY3300054 + merestinib

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

**LY3300054 + merestinib** is a combination therapy of two investigational anticancer agents, studied for advanced, refractory solid tumors. LY3300054 is a monoclonal antibody that inhibits programmed cell death ligand 1 (**PD-L1**), thereby blocking immune evasion by tumor cells and activating T-cell mediated antitumor immunity. Merestinib is a small molecule, oral multikinase inhibitor, primarily targeting the hepatocyte growth factor receptor (**MET**), with additional activity against other kinases such as FGFR, DDR1, and AXL. The combination aims to provide synergistic antitumor effects by both reactivating the immune system (via PD-L1 blockade) and directly inhibiting oncogenic signaling pathways (via MET/other kinase inhibition). Eli Lilly is the developer of both agents. Clinical trials assessed safety, pharmacokinetics, and initial antitumor efficacy in patients with solid tumors, including pancreatic cancer and melanoma[1][3][5].

02

Targets

FGFR1 (Fibroblast growth factor receptor 1)MET (Mesenchymal-epithelial transition factor receptor)AXL (AXL receptor tyrosine kinase)CD274 (Programmed cell death protein 1 ligand 1)DDR1 (Discoidin domain receptor 1)

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