Thursday, July 24, 2014
Publication and contact
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
All contents Copyright © 1993-2017 BioCentury Publications, Inc. ALL RIGHTS RESERVED. All use of this Web Site and its contents is governed by the BioCentury User Agreement
. The contents of this Web Site are protected under U.S. and foreign copyright and intellectual property laws, and no part of this Web Site or its contents may be photocopied, reproduced or retransmitted in any form without the written consent of BioCentury, which may be requested from Reprints/Permissions
. BioCentury®; The Bernstein Report on BioBusiness™; The BioCentury 100™; The Clear Route to ROI™; Because Real Intelligence is Hard to Find™; BCIQ™; and BioPharma's Knowledge Center™; are trademarks of BioCentury Publications, Inc., P.O. Box 1246, San Carlos, CA 94070. SciBX® and SciBX: Science-Business eXchange® are trademarks of Nature America, Inc. that are jointly used by BioCentury Publications, Inc. and Nature America, Inc.
Thanks for purchasing this article.
Please bookmark this url for future reference.
We have also sent you a confirming e-mail with a receipt and this same url for your
close [ X ]