Thursday, July 24, 2014
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Neurotrophic tyrosine kinase receptor 1 (NTRK1;
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
Next steps could include testing the inhibitor in additional pain models and
testing its safety profile.
Inc. markets Lyrica for multiple indications including
Creabilis S.A. has CT327,
a topical TRKA inhibitor, in Phase II testing for dermatitis and psoriasis.
Nerviano Medical Sciences s.r.l.
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.
Published online July 24, 2014
Patent and licensing status
Stachel, S.J. et al. J.
Med. Chem.; published online June 10, 2014;
Contact: Shawn J. Stachel, Merck Research Laboratories, West
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