– NEO6860 is a promising TRPV1 antagonist designed to avoid on-target side effects
– Target engagement and safety profile established in recently published Phase 1 study1
– Promising preliminary results from Phase 2 Study completed in Q1/2017
Montreal, Quebec – March 28th, 2017 – NEOMED Institute today announced the publication of the Phase 1 data for NEO6860 in the Journal of Pain. The purpose of this study was to assess the safety, pharmacokinetics and pharmacodynamics profile of NEO6860, an oral modality-selective TRPV1 antagonist, predicted to relieve pain without the human safety concerns observed in competitive TRPV1 antagonist clinical trials. Transient Receptor Potential Vanilloid subtype 1 (TRPV1) is a promising peripheral pain target, localized in human sensory neurons, that can be activated in several ways: by capsaicin (the active ingredient in chili peppers), low pH, or heat. Multiple TRPV1 antagonists have been tested in humans and two specific adverse events have been observed leading to the termination of most of these programs. The first is the elevation of body temperature or hyperthermia and the second, and potentially more serious adverse effect, is impaired noxious heat sensation which can lead to severe burning incidents.
The novel profile of NEO6860, as a modality-selective TRPV1 antagonist, is the basis for the hypothesis that NEO6860 should demonstrate an analgesic effect without the undesired side effects on body temperature or heat-pain sensation. As published in the Journal of Pain, the successful Phase 1 study of NEO6860 confirms that NEOMED’s therapeutic agent does not provoke either of these two side effects but does demonstrate clear target engagement and a reduction in secondary hyperalgesia versus placebo.
This promising Phase 1 data was the basis on which NEOMED initiated in 2016 a 50 patient Phase 2 proof-of-concept for NEO6860, treating patients with severe osteoarthritic (OA) pain. This study was successfully completed in Q1/2017 and analysis of the full data set is ongoing for presentation to potential partners. Preliminary data suggests that NEO6860 demonstrates an analgesic effect compared to placebo and that the safety profile is consistent with what was observed in the Phase 1 study.
“These studies are landmarks for the NEOMED Institute, clearly demonstrating our internal capability to develop one of our pipeline therapeutics from preclinical studies through Phase 1 and Phase 2 proof-of-concept clinical trials, fully validating our internal capabilities and semi-virtual operating model.” declared Dr. Philippe Walker, Chief Scientific Officer of NEOMED Institute. “Our Phase 1 and Phase 2 studies of this novel oral small molecule clearly establish the pharmacokinetic, safety and efficacy profile of NEO6860 for the treatment of pain and lead us to believe that NEO6860 has the potential to become an new therapeutic option for the treatment of osteoarthritic pain.” noted Dr. Dan Chiche, Chief Medical Officer of NEOMED Institute
1-Safety, Pharmacokinetic and Pharmacodynamic Study in Healthy Subjects of Oral NEO6860, a Modality Selective TRPV1 Antagonist, The Journal of Pain, 08 Feb 2017
NEO6860, a new drug, under investigation for the treatment of osteoarthritis (OA) pain, shows potent antagonism of human TRPV1 when capsaicin is used as a stimulus in vitro, and has little or no effect against activation by low pH or heat. This profile, described as modality-selective TRPV1 antagonism, is predicted to relieve OA pain without the effects on body temperature or heat-pain threshold reported in the clinic with previous modality-nonselective TRPV1 antagonists.
Osteoarthritis (OA) is a musculoskeletal disorder involving degradation of joints, regularly associated with pain, which is the most debilitating symptom. OA of the knee is very common with approximately 250 million people with the condition globally. While pharmacotherapy is the cornerstone for the medical management of patients OA, there are significant limitations, in terms of efficacy as well as safety. Clinical effects of current drugs are small and limited to the first few weeks after start of treatment. In addition, there are significant risks associated with the use of current therapy, especially cardiovascular and gastrointestinal risks. A potent compound acting through a different mechanism, on a new target, would be desirable to circumvent the pitfalls of existing therapies.
About NEOMED Institute
NEOMED Institute is a not‐for‐profit organization whose mission is to bridge the gap between basic research and the commercialization of new drugs by providing industrial expertise in drug discovery and development, combined with funding and a favorable ecosystem, to transform innovations into solid therapeutic solutions. NEOMED drives drug discovery activities up to the stage of human proof of concept. NEOMED has two fully integrated research and development campuses: one in Ville Saint‐Laurent, specializing in small molecule therapeutics, and the other in Laval, specializing in the development of biologics and vaccines. Both facilities function as open‐access drug discovery hubs housing independent commercial businesses (29 independent companies employing more than 300 people) and providing a dynamic environment that stimulates collaboration, innovation, and creativity. NEOMED’s wholly-owned for-profit subsidiary, NEOMED-LABS, a Contract Research Organization (CRO) providing customized and high-throughput immune-monitoring for clinical vaccine development, is one of these tenants.
NEOMED is jointly funded by the pharmaceutical industry, the Ministère de l’Économie, de la Science et de l’Innovation du Québec, and the Networks of Centres of Excellence (NCE) of Canada.
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