Date: 2015-08-20
Type of information: Results
phase: 2a
Announcement: results
Company: Vernalis (UK)
Product: V158866 (fatty acid amide hydrolase (FAAH) inhibitor)
Action
mechanism: enzyme inhibitor. V15866 is a selective, patent protected, fatty acid amide hydrolase (FAAH) inhibitor which arose from an internal research programme and is now in clinical development. It is being studied in a Phase II proof-of-concept study in neuropathic pain. FAAH is an integral membrane enzyme that hydrolyses the endocannabinoids: AEA (anandamide), and to a lesser extent related signalling lipids such as OEA (ethanolamide) and PEA (palmitoyl ethanolamide). AEA and 2-AG (2-arachidonoyl-glycerol) are the endogenous ligands of CB1 and CB2 receptors. These receptors are also activated by THC (?9-tetrahydrocannabinol), the principal active in cannabis. FAAH inhibition would be expected to augment the endogenous cannabinoid tone by decreasing the metabolic rate of AEA and other endogenous substrates. In contrast to the action of any exogenous CB1 agonists, FAAH inhibition should lead to specifically targeted activation of CB1 receptors only in areas where EC tone is enhanced. It is believed that pain is one of the triggering stimuli, which leads to enhance EC tone, and thus, FAAH inhibition may be able to augment EC-mediated anti-nociception without generating side-effect issues in the non-activated pathways. Finally, the action of FAAH inhibition is controlled by the rate of synthesis of AEA, and hence neural activity. Therefore, the resulting activation of CB1 receptors would be expected to mimic the physiological range, in contrast to those pharmacological responses achieved with CB1 agonists.
Disease: neuropathic pain as a result of spinal cord injury
Therapeutic area: CNS diseases - Neurological diseases
Country: USA
Trial
details: The purpose of this study is to investigate whether V158866 is safe and effective for the treatment of neuropathic pain due to spinal cord injury.(NCT01748695)
Latest
news: * On August 20, 2015, Vernalis announced the results from a Phase II proof-of-concept (POC) study of V158866, its fatty acid amide hydrolase (FAAH) inhibitor, which is being investigated as a treatment for neuropathic pain as a result of spinal cord injury. In the randomised, double-blind, placebo-controlled, two-period cross-over study, although dosing of V158866 resulted in elevated endocannabinoid levels, on an intent-to-treat basis the study failed to meet its pain reduction primary endpoint. Treatment with V158866 did however show a trend towards efficacy on a per protocol basis (p=0.054) and was generally well tolerated.
Consistent with its strategy of becoming a commercial business, Vernalis is not planning to make any further investment in this programme and will seek to realise its potential value through partnering. A previous Phase I study provided encouraging data in evaluating the safety, tolerability and pharmacokinetic and pharmacodynamic effects of the compound.
Ian Garland, CEO of Vernalis commented \"The goal of this study was to identify a therapeutic setting for this programme. Its completion ends the investment in our NCE pipeline and we aim to partner the remaining unpartnered programmes to realise value where possible. The key focus of the organisation remains the transition of Vernalis to a commercial company, with the forthcoming launch of Tuzistra™ XR, our extended release cough cold product for the US prescription market, which is progressing as planned \".
