Drug intelligence / Profile preview

PD-1 antibody + tyrosine kinase inhibitor

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

Overview

This refers to a combination therapy consisting of a programmed cell death protein 1 (PD-1) monoclonal antibody (such as nivolumab, pembrolizumab, or sintilimab) and a tyrosine kinase inhibitor (TKI; such as cabozantinib, pazopanib, axitinib, lenvatinib, sorafenib). The PD-1 antibody blocks the interaction between PD-1 on immune cells and its ligands (PD-L1/PD-L2), thereby enhancing T-cell mediated antitumor immunity. The TKI component inhibits multiple receptor tyrosine kinases involved in tumor angiogenesis and growth—most commonly targeting vascular endothelial growth factor receptors (VEGFRs), but also potentially fibroblast growth factor receptors (FGFRs), platelet-derived growth factor receptors (PDGFRs), RET, KIT and others depending on the specific agent. This combination is used primarily in oncology for synergistic effects against various cancers including metastatic renal cell carcinoma and hepatocellular carcinoma[1][2][3].

Other names
PD-1 inhibitor + TKIanti-PD-1 antibody + TKIimmune checkpoint inhibitor + tyrosine kinase inhibitor
02

Targets

FGFR4 (Fibroblast growth factor receptor 4)PDGFRA (Platelet-derived growth factor receptor alpha)RET (Rearranged during transfection receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)PDCD1 (Programmed cell death protein 1 receptor)VEGFR3 (Vascular endothelial growth factor receptor 3)FGFR3 (Fibroblast growth factor receptor 3)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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