Telatinib (BAY 57-9352), a small molecule angiogenesis inhibitor, can potently inhibit VEGFR2, VEGFR3, c-Kit and PDGFRbeta with IC50 of 6 nM, 4 nM, 1 nM and 15 nM. Telatinib (BAY 57-9352) impairs vascular function, induces rarefaction, and causes hypertension. Telatinib can inhibit the autophosphorylation of VEGFR2 autophosphorylation with an IC50 of 19 nM, and telatinib also suppresses VEGF-dependent proliferation of human umbilical vein endothelial cells with an IC50 of 26 nM.
In vivo
The maximum-tolerated dose was not reached up to a dose of 1500 mg BID continuous dosing. Telatinib was rapidly absorbed with median t(max) of 3 hours or less.Telatinib is safe and well tolerated up to a dose of 1500 mg BID continuous dosing. Telatinib (450 mg b.i.d.) combined with bevacizumab (1 mg/kg bi-weekly) shows antitumor activity, but accumulating constitutional toxicity impedes long-term treatment of patients.