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Neurotrophic tyrosine kinase receptor 1 (NTRK1; TrkA)

In vitro and rat studies identified small molecule, selective TRKA inhibitors that could help treat pain. In a high throughput screen, four TRKA inhibitors from different molecular classes showed at least 50-fold selectivity over a nonselective receptor tyrosine kinase (RTK). In a rat model of inflammatory pain, one of the inhibitors reversed allodynia with comparable potency to the NSAID naproxen. In a rat model of neuropathic pain, the inhibitor reversed mechanical hypersensitivity with comparable potency to Lyrica pregabalin. Next steps could include testing the inhibitor in additional pain models and testing its safety profile.
Pfizer Inc. markets Lyrica for multiple indications including pain.
Creabilis S.A. has CT327, a topical TRKA inhibitor, in Phase II testing for dermatitis and psoriasis.
Nerviano Medical Sciences s.r.l. has milciclib maleate, an inhibitor of TRKA and cyclin dependent kinases (CDKs), in Phase II testing to treat cancer.
At least four other companies have TRKA inhibitors in Phase I/II or earlier development for various diseases.

SciBX 7(28); doi:10.1038/scibx.2014.834
Published online July 24, 2014

Patent and licensing status undisclosed

Stachel, S.J. et al. J. Med. Chem.; published online June 10, 2014;
Contact: Shawn J. Stachel, Merck Research Laboratories, West Point, Pa.