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Concert Pharmaceuticals, Inc. Message Board

  • beepeeess beepeeess Aug 4, 2014 11:49 PM Flag

    Concert Pharmaceuticals resurrects former Merck & Co. compound from the ashes

    Concert Pharmaceuticals has begun a Phase I trial with CTP-354 to potentially treat spasticity and chronic pain. Previously, the compound had been Merck & Co.’s L-838417 and had demonstrated strong muscle relaxant activity and efficacy against both inflammatory and neuropathic pain. Despite L-838417’s strengths, the compound showed substantial pharmacokinetic limitations and as a consequence, never made it past the lab.The Concert Pharmaceuticals study will evaluate the safety, tolerability, and pharmacokinetics of CTP-354 in healthy volunteers. In addition, the company intends to conduct a Positron Emission Tomography study to assess brain receptor occupancy of CTP-354 in healthy volunteers. Concert expects to report top-line results of the Phase 1 single ascending dose study by the end of the year. “CTP-354 was a compound that was brought to my attention in a conversation that I was having with an expert in another field,” says Concert Pharmaceuticals CEO Roger Tung. “He had worked preclinically with the compound and had mentioned some results that he had with it as a very exciting agent. Based on that, we went back as an organization to review the available data on it, which is vast. There are a lot of publications on the underlying L-838417, which is the Merck compound. We saw this as an opportunity to apply our technology, to improve certain properties such as distribution, metabolism, and secretion to and to enable this compound to be taken into human clinical evaluation and to do what we hope it will be able to, which is be a unique ground breaking medicine.” Merck was not able to fit all of the similar properties into the compound. “What we were able to do then is to essentially start with the huge investment, the time, and the effort that they put into identifying and nearly got there and then used our technology to put us over the finish line,” Tung told R&D Pharma Business Connect. Concert’s selective incorporation of deuterium in CTP-354 significantly improved pharmacokinetic properties in preclinical models while maintaining the desirable pharmacological activity seen with the earlier generation modulators. “We see a lot of applicability to the technology to many different kinds of situations and that has led to the collaboration that we have had in a corporate sense,” says Tung. “We announced our partnership with Celgene and we think that it has the potential to have a very broad and important impact in a wide range of medicines.”

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