PF-8380 (Autotaxin Inhibitor)

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”.

References

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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.