Cudetaxestat

Cudetaxestat is an inhibitor of autotaxin (IC₅₀ = ≤0.5 µM), also known as ectonucleotide pyrophosphatase/phosphodiesterase family member 2 (ENPP2).^1,2 It reduces migration of MDA-MB-435 melanoma cells (IC₅₀ = 15 nM).² Cudetaxestat reduces blood glucose levels in a glucose tolerance test, as well as baseline blood glucose levels, in mice fed a high-fat diet when administered at a dose of 15 mg/kg twice per day for two days.¹ It reduces liver fibrosis in mice fed a choline-deficient, L-amino acid-defined, high-fat diet (CDAA/HFD) as a model of liver fibrosis when administered at a dose of 10 mg/kg.² It also reduces colon ulcer area and increases colon length in mouse models of acute and chronic ulcerative colitis, respectively.

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1. Evans, J.F. Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor. (2015).

2. Bain, G., Evans, J.F., Hutchinson, J.H., et al. Autotaxin inhibitors and uses thereof. (2020).