Lucitanib (hydrochloride)

Lucitanib is a dual inhibitor of VEGFR and FGFR that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC₅₀s = 7, 25, and 10 nM, respectively) and FGFR1 and FGFR2 (IC₅₀s = 17.5 and 82.5 nM, respectively).¹ It is selective for these receptors over FGFR3 and FGFR4 (IC₅₀s = 237.5 and >1,000 nM, respectively), as well as the PDGFR family members c-Kit, PDGFRα, and PDGFRβ (IC₅₀s = 456, 175, and 525 nM, respectively), but does inhibit FMS, also known as CSF-1 receptor tyrosine kinase (IC₅₀ = 5 nM). Lucitanib inhibits the proliferation of human umbilical vein endothelial cells (HUVECs) induced by VEGF or basic FGF (bFGF; IC₅₀s = 40 and 50 nM, respectively) but inhibits the proliferation of A2780 ovarian, A498 renal, and SN12KI renal cancer cells only at higher concentrations (IC₅₀s = 27.7, 19.6, and 12.79 µM, respectively). It reduces tumor growth in HT-29 colon and A2780 ovarian cancer mouse xenograft models, as well as in RXF 393, A498, and SKN12I renal cancer mouse xenograft models in a dose-dependent manner. It also completely inhibits bFGF-induced angiogenesis in a Matrigel™ plug assay in mice when administered at a dose of 20 mg/kg.

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1. Bello, E., Colella, G., Scarlato, V., et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 71(4), 1396-1405 (2011).