Comparative biochemical kinase profiling of VEGFR2 inhibitors


Vascular endothelial growth factor receptor 2 (VEGFR2) is a key regulator of tumor angiogenesis, the formation of new blood vessels from existing vasculature. VEGFR2 has been an attractive target for anti-cancer therapy. However, clinical application of available VEGFR2 inhibitors has been challenged by limited efficacy and a wide range of side effects, potentially due to inadequate selectivity for VEGFR2.

In a study co-authored by scientists from Elevar Therapeutics and Oncolines B.V.  in Cancer Chemotherapy and Pharmacology [1], the biochemical kinase activity profiles of eleven small molecule tyrosine kinase inhibitors are compared on VEGFR2 and 270 kinases representative of the human kinome. Rivoceranib [2], a kinase inhibitor under review at the U.S. Food & Drug Administration (FDA), was identified as a highly selective VEGFR2 inhibitor. The comparative biochemical analysis highlights the potential for rivoceranib to address clinical limitations associated with off-target effects of currently available VEGFR2 inhibitors.

The study highlights the power of combining Oncolines’ ResidenceTimer platform and Carna Bioscience’s kinase activity profiling.

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Figure. Radar plot showing residual activity of 270 kinases in the presence of rivoceranib (160 or 1600 nM) or 1000 nM of 10 FDA-approved reference tyrosine kinase inhibitors.


[1] Jang et al. (2023) Comparative biochemical kinases activity analysis identifies rivoceranib as a highly selective VEGFR2 inhibitor. Cancer Chemotherapy and Pharmacology 91:491-9.

[2] Qin et al. (2023) Camrelizumab plus rivoceranib versus sorafenib as first-line therapy for unresectable hepatocellular carcinoma (CARES-310): a randomised, open-label, international phase 3 study. The Lancet online first 24 July 2023.

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