SAN DIEGO, CA, USA I April 12, 2016 I Arena Pharmaceuticals, Inc. (NASDAQ: ARNA) today announced favorable results from its Phase 1b multiple-ascending dose clinical trial of APD371, a highly selective and potent agonist of the cannabinoid 2 (CB2) receptor with potential utility in the treatment of pain.
This randomized, double-blind, placebo-controlled Phase 1b clinical trial enrolled 36 healthy adults to evaluate the safety, tolerability and pharmacokinetics of multiple-ascending doses of APD371. Cohorts of 12 subjects (9 active, 3 placebo) were administered doses of 50 mg, 100 mg, or 200 mg of APD371 or placebo three times daily for 10 days and, in connection with the pharmacokinetic evaluation, one time on the 11th day. The most common adverse events were headache and nausea. All adverse events were classified as mild, and there were no serious adverse events reported. There was one discontinuation in the high-dose group due to an adverse event of mild thirst and somnolence. Reductions in blood pressure and heart rate were observed, but none were symptomatic or resulted in an adverse event. Drug levels at all doses tested in the trial, including the lowest dose, were well above those believed to be needed to stimulate the CB2 receptor.
“The results of this trial substantiate data from our single-ascending dose trial of APD371. In both trials, we achieved dose-responsive exposure without dose-limiting adverse events across the range studied,” said William R. Shanahan, Jr., M.D., Arena’s Senior Vice President and Chief Medical Officer. “Our scientists designed APD371 as a highly selective, peripherally restricted, full agonist to provide pain relief without psychotropic effects, loss of efficacy over time, or the dependence, abuse potential or adverse event profile associated with other pain treatments.”
About APD371
APD371, an orally available agonist of the CB2 receptor, is Arena’s internally discovered investigational drug candidate intended for the treatment of pain and potentially other indications. With its high level of selectivity for the CB2 receptor versus the CB1 receptor and its high peripheral restriction observed in preclinical studies, APD371 is designed to provide pain relief without psychotropic effects. Targeting the CB2 receptor may also avoid or reduce the potential for the dependence or abuse associated with opioid drugs or the adverse event profile associated with NSAIDs. Preclinical efficacy with APD371 has been shown in animal models of osteoarthritic and neuropathic pain.
About Arena Pharmaceuticals
Arena embraces the challenge of improving health by seeking to bring innovative medicines targeting G protein-coupled receptors to patients. Arena’s focus is discovering, developing and commercializing drugs to address unmet medical needs, and BELVIQ® (lorcaserin HCl) is Arena’s first internally discovered drug approved for marketing. Arena’s US operations are located in San Diego, California, and its operations outside of the United States, including its commercial manufacturing facility, are located in Zofingen, Switzerland. For more information, visit Arena’s website at www.arenapharm.com.
SOURCE: Arena Pharmaceuticals
Post Views: 142
SAN DIEGO, CA, USA I April 12, 2016 I Arena Pharmaceuticals, Inc. (NASDAQ: ARNA) today announced favorable results from its Phase 1b multiple-ascending dose clinical trial of APD371, a highly selective and potent agonist of the cannabinoid 2 (CB2) receptor with potential utility in the treatment of pain.
This randomized, double-blind, placebo-controlled Phase 1b clinical trial enrolled 36 healthy adults to evaluate the safety, tolerability and pharmacokinetics of multiple-ascending doses of APD371. Cohorts of 12 subjects (9 active, 3 placebo) were administered doses of 50 mg, 100 mg, or 200 mg of APD371 or placebo three times daily for 10 days and, in connection with the pharmacokinetic evaluation, one time on the 11th day. The most common adverse events were headache and nausea. All adverse events were classified as mild, and there were no serious adverse events reported. There was one discontinuation in the high-dose group due to an adverse event of mild thirst and somnolence. Reductions in blood pressure and heart rate were observed, but none were symptomatic or resulted in an adverse event. Drug levels at all doses tested in the trial, including the lowest dose, were well above those believed to be needed to stimulate the CB2 receptor.
“The results of this trial substantiate data from our single-ascending dose trial of APD371. In both trials, we achieved dose-responsive exposure without dose-limiting adverse events across the range studied,” said William R. Shanahan, Jr., M.D., Arena’s Senior Vice President and Chief Medical Officer. “Our scientists designed APD371 as a highly selective, peripherally restricted, full agonist to provide pain relief without psychotropic effects, loss of efficacy over time, or the dependence, abuse potential or adverse event profile associated with other pain treatments.”
About APD371
APD371, an orally available agonist of the CB2 receptor, is Arena’s internally discovered investigational drug candidate intended for the treatment of pain and potentially other indications. With its high level of selectivity for the CB2 receptor versus the CB1 receptor and its high peripheral restriction observed in preclinical studies, APD371 is designed to provide pain relief without psychotropic effects. Targeting the CB2 receptor may also avoid or reduce the potential for the dependence or abuse associated with opioid drugs or the adverse event profile associated with NSAIDs. Preclinical efficacy with APD371 has been shown in animal models of osteoarthritic and neuropathic pain.
About Arena Pharmaceuticals
Arena embraces the challenge of improving health by seeking to bring innovative medicines targeting G protein-coupled receptors to patients. Arena’s focus is discovering, developing and commercializing drugs to address unmet medical needs, and BELVIQ® (lorcaserin HCl) is Arena’s first internally discovered drug approved for marketing. Arena’s US operations are located in San Diego, California, and its operations outside of the United States, including its commercial manufacturing facility, are located in Zofingen, Switzerland. For more information, visit Arena’s website at www.arenapharm.com.
SOURCE: Arena Pharmaceuticals
Post Views: 142
