PF-8380 is a potent autotaxin (ATX) inhibitor (IC50 2.8 nM/101 nM purified enzyme/whole blood). Excessive activity of ATX is associated with numerous inflammatory conditions, cancers and other disease. Lysophosphatidic acid (LPA) produced by ATX stimulates cell proliferation through G-protein coupled receptorsLPA1-4. PF-8380 is orally bioavailable and effectively inhibits ATX in vivo reducing LPA levels in serum and at the site of inflammation in a rat arthritis model. Can delivered orally with the “Oral Formulation Vehicle”.
Gierse, J. et al (2010) “A Novel Autotaxin Inhibitor Reduces Lysophosphatidic Acid Levels in Plasma and the Site of Inflammation”> Journal of Pharmacology and Experimental Therapeutics 334(1):310.