Drug intelligence / Profile preview

pembrolizumab + lenvatinib + albumin-bound paclitaxel

Development stage
Unknown
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous, Oral
01

Overview

This drug is an investigational **combination therapy** comprised of pembrolizumab (a monoclonal antibody immune checkpoint inhibitor targeting PD-1), lenvatinib (a small molecule multikinase inhibitor), and albumin-bound paclitaxel (a nanoparticle formulation of the antimitotic agent paclitaxel). Pembrolizumab enhances the immune response against tumor cells by inhibiting the PD-1 pathway, thereby preventing the suppression of T-cell activity. Lenvatinib inhibits multiple tyrosine kinase receptors involved in angiogenesis and tumor proliferation, notably the vascular endothelial growth factor (VEGF) receptors, fibroblast growth factor receptors (FGFRs), and others. Albumin-bound paclitaxel is a cytotoxic agent that interferes with microtubule function, promoting apoptosis in rapidly dividing cells. The combination seeks to leverage the immunomodulatory effect of pembrolizumab, the anti-angiogenic and antiproliferative activities of lenvatinib, and the direct cytotoxic action of paclitaxel. Early clinical investigation is ongoing, principally for gynecologic cancers such as recurrent endometrial cancer.

02

Targets

FGFR1 (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)TUBB (Tubulin (alpha and beta subunits))

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