Drug intelligence / Profile preview

pembrolizumab + lenvatinib + gemcitabine + oxaliplatin

Development stage
Phase 2
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of four drugs: - **Pembrolizumab** is a monoclonal antibody that acts as an immune checkpoint inhibitor targeting the programmed cell death protein 1 (PD-1) receptor, thereby enhancing the immune system's ability to detect and destroy cancer cells. - **Lenvatinib** is a small molecule multikinase inhibitor that targets vascular endothelial growth factor receptors (VEGFR1, VEGFR2, VEGFR3), fibroblast growth factor receptors (FGFR1–4), platelet-derived growth factor receptor alpha (PDGFRα), RET proto-oncogene, and KIT proto-oncogene. It inhibits tumor angiogenesis and proliferation. - **Gemcitabine** is a nucleoside analog used as chemotherapy; it inhibits DNA synthesis by incorporation into DNA strands during replication, leading to apoptosis in rapidly dividing cells. - **Oxaliplatin** is a platinum-based chemotherapeutic agent that forms crosslinks in DNA, inhibiting replication and transcription and inducing cell death. This combination brings together immunotherapy (pembrolizumab), targeted therapy (lenvatinib), and cytotoxic chemotherapy agents (gemcitabine and oxaliplatin). The regimen may be under investigation for synergistic effects in various solid tumors where multi-modal mechanisms are desired. While pembrolizumab plus lenvatinib has established approvals for several cancers[1][2][3][5], the specific four-drug combination with gemcitabine and oxaliplatin represents an investigational approach not yet standard or approved for any indication based on current evidence.

02

Targets

DNAFGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)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)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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