Quininib is an antagonist of the cysteinyl leukotriene 1 (CysLT1) and CysLT2 receptors (IC50s = 1.4 and 52 μM, respectively). It inhibits tubule formation in HMEC-1 cells when used at concentrations of 3.16 and 10 μM and inhibits sprout formation in isolated mouse aortic rings in an ex vivo model of angiogenesis when used at 10 μM. Quininib (3 μM) decreases angiogenesis in an oxygen-induced retinopathy mouse model of ocular angiogenesis, preventing revascularization when used at concentrations of 0.5 and 3 μM, as well as increasing neovascularization and vascular density when used at 3 μM. It reduces tumor growth and inhibits angiogenesis in an HT-29 colorectal cancer mouse xenograft model when administered at a dose of 50 mg/kg every three days.
