Concert, Fast Forward partner to advance new approach to treat spasticity and pain in MS

Mar 5 2012

Concert Pharmaceuticals, Inc. and Fast Forward, LLC, the National Multiple Sclerosis Society's subsidiary devoted to bridging the gap between research and drug development, today announced a new collaboration to fund the preclinical advancement of C-21191, a deuterium-modified subtype-selective GABA_A modulator developed by Concert with the therapeutic potential of treating spasticity and pain in multiple sclerosis (MS). Fast Forward will commit funding to support the program for prospective clinical stage development.

“We are pleased to partner with Concert on this new approach with the potential to treat spasticity and pain, which are so challenging to large numbers of people living with MS”

"We are pleased to partner with Concert on this new approach with the potential to treat spasticity and pain, which are so challenging to large numbers of people living with MS," said Dr. Timothy Coetzee, Chief Research Officer at the National MS Society and Fast Forward. "This collaboration demonstrates Fast Forward's commitment to pursue and fund innovative medicines that can address unmet needs and improve the quality of life for people living with this disease."

"This collaboration with Fast Forward enables us to accelerate development of C-21191 and will provide our team with valuable insight into the management of symptoms associated with multiple sclerosis," said Roger Tung, Ph.D., President and CEO of Concert Pharmaceuticals. "It further validates our novel deuterated chemical entity platform as a highly efficient approach to creating innovative compounds like C-21191 by leveraging previous industry R&D investment."

C-21191, a subtype-selective GABA_A receptor modulator under development by Concert, is a deuterium-modified analog of L-838417. L-838417 was discovered by Merck & Co. and extensively profiled in preclinical testing by Merck and in numerous academic laboratories. L-838417 possesses an attractive pharmacological profile including minimal sedation and ataxia, but has a poor pharmacokinetic profile, which prevented its progression to clinical evaluation. C-21191 has demonstrated significantly improved pharmacokinetic characteristics in preclinical studies compared to L-838417, while maintaining its desired biochemical profile. In side-by-side studies, C-21191 demonstrated a three to four-fold increase in exposure compared to L-838417 in several preclinical species. This superior pharmacokinetic profile resulted in a prolongation of exposure and a corresponding extension of pharmacodynamic effects. C-21191 also demonstrated equivalent efficacy to gabapentin in a neuropathic pain model, with a superior duration of effect, at doses which did not cause sedation or ataxia as assessed by a rotarod model.

Source Concert Pharmaceuticals, Inc. and Fast Forward, LLC,