Drug intelligence / Profile preview

lenvatinib + pembrolizumab + pemetrexed + cisplatin

Development stage
Phase 3
Lead developer
Eisai
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral (lenvatinib)
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Overview

A four-drug combination regimen consisting of lenvatinib, pembrolizumab, pemetrexed, and cisplatin, used in the investigational or clinical trial setting for various advanced solid tumors, particularly non-small cell lung cancer (NSCLC). - **Lenvatinib** is a small molecule multi-kinase inhibitor targeting vascular endothelial growth factor receptors (VEGFR1-3), fibroblast growth factor receptors (FGFR1-4), platelet-derived growth factor receptor alpha (PDGFRα), RET, and KIT, thereby inhibiting tumor angiogenesis and proliferation. - **Pembrolizumab** is a monoclonal antibody that blocks the programmed cell death 1 (PD-1) receptor, preventing cancer cells from evading immune detection. - **Pemetrexed** is an antifolate chemotherapy agent that inhibits enzymes involved in purine and pyrimidine synthesis, thus preventing cell replication. - **Cisplatin** is a platinum-based chemotherapy agent that causes DNA crosslinking, leading to apoptosis of rapidly dividing cancer cells. Used together, the regimen combines immunotherapeutic (pembrolizumab), antiangiogenic/targeted (lenvatinib), and cytotoxic (pemetrexed, cisplatin) components to maximize anti-tumor activity.

02

Targets

DNADHFR (Dihydrofolate reductase)GART (GAR transformylase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDCD1 (Programmed cell death protein 1 receptor)PDGFRA (Platelet-derived growth factor receptor alpha)RET (Rearranged during transfection receptor tyrosine kinase)TS (Thymidylate synthase)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)VEGFR-1 (Vascular endothelial growth factor receptor 1)

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