Drug intelligence / Profile preview

cabozantinib + pembrolizumab

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

Overview

Cabozantinib + pembrolizumab is a combination regimen consisting of cabozantinib, a multi-targeted tyrosine kinase inhibitor, and pembrolizumab, an anti–PD-1 monoclonal antibody immune checkpoint inhibitor. Cabozantinib targets multiple tyrosine kinases, including MET, VEGFR-2, RET, AXL, and FLT-3, inhibiting tumor angiogenesis, cell proliferation, and metastasis, and modulating the tumor microenvironment. Pembrolizumab blocks the PD-1 receptor on T-cells, thereby restoring antitumor immune response. Their use in combination is under investigation and has shown promising antitumor activity and manageable safety in several cancer types, including metastatic renal cell carcinoma, ICI-resistant gastroesophageal adenocarcinoma, and advanced sarcomas[1][2][3][4][5][7].

Other names
pembrolizumab + cabozantinib
02

Targets

AXL (AXL receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)PDCD1 (Programmed cell death protein 1 receptor)RET (Rearranged during transfection receptor tyrosine kinase)TEK (Tie2)VEGFR2 (Vascular endothelial growth factor receptor 2)

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