Quininib

Quininib is an antagonist of the cysteinyl leukotriene 1 (CysLT₁) and CysLT₂ receptors (IC₅₀s = 1.4 and 52 µM, respectively).¹ 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.²

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1. Reynolds, A.L., Alvarez, Y., Sasore, T., et al. Phenotype-based discovery of 2-[(E)-2-(quinolin-2-yl)vinyl]phenol as a novel regulator of ocular angiogenesis. The Journal of Biological Chemisty 291(14), 7242-7255 (2016).

2. Murphy, A.G., Casey, R., Maguire, A., et al. Preclinical validation of the small molecule drug quininib as a novel therapeutic for colorectal cancer. Sci. Rep. 6, 34523 (2016).