Drug intelligence / Profile preview

izalontamab brengitecan + axitinib + pembrolizumab

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

**Izalontamab brengitecan + axitinib + pembrolizumab** is a combination investigational cancer therapy. It comprises three components:\ - **Izalontamab brengitecan**: an antibody-drug conjugate (ADC, not yet approved; presumed to be an anti-cancer monoclonal antibody conjugated with the cytotoxic topoisomerase I inhibitor brengitecan).\n- **Axitinib**: a small molecule tyrosine kinase inhibitor that selectively inhibits vascular endothelial growth factor receptors (VEGFRs), thereby inhibiting angiogenesis and tumor growth[1][3][7].\n- **Pembrolizumab**: a humanized monoclonal antibody targeting PD-1 (programmed death receptor-1), blocking its interaction with PD-L1 and PD-L2 to promote anti-tumor immune responses[2][4][6][7][8].\ The combination aims to leverage the targeted cytotoxicity of the ADC, the anti-angiogenic effect of axitinib, and the immune checkpoint blockade of pembrolizumab for synergistic anti-tumor activity. The combination is under clinical investigation for advanced solid tumors and possibly renal cell carcinoma; no approvals yet exist for the triple combination.

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Targets

PDCD1 (Programmed cell death protein 1 receptor)ERBB3 (Erb-b2 receptor tyrosine kinase 3)VEGFR2 (Vascular endothelial growth factor receptor 2)TOP1 (DNA Topoisomerase I)VEGFR-1 (Vascular endothelial growth factor receptor 1)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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