Potent and selective pan-Trk inhibitor (IC50 values are 1, 2 and 6 nM for Trk C, B and A, respectively). Selective for Trk over a panel of ion channels, receptors and other enzymes. Peripherally restricted. Exhibits efficacy in a rodent model of inflammatory pain. Orally bioavailable.
Skerratt et al (2016) The discovery of a potent, selective, and peripherally restricted pan-Trk inhibitor (PF-06273340) for the treatment of pain. J.Med.Chem. 59 10084 PMID:27766865