Axsome Therapeutics Announces AXS-06 (MoSEIC™ Meloxicam and Esomeprazole) Meets Primary Endpoint in Phase 1 Clinical Trial
AXS-06 is an oral, rapidly-absorbed, once-daily, non-opioid, COX-2 preferential pain therapeutic with a gastroprotectant
Primary endpoint met with 9 times faster time to maximum plasma concentration (Tmax) of meloxicam versus Mobic® (p<0.0001)
Therapeutic plasma levels of meloxicam achieved within 15 minutes of oral dosing of AXS-06
Gastroprotective concentrations of esomeprazole achieved
Phase 3-ready based on FDA Pre-IND guidance
AXS-06 utilizes Axsome’s MoSEIC™ delivery technology
AXS-06 to complement commercialization of AXS-02 in development for complex regional pain syndrome
The clinical trial results demonstrated, for the first time, rapid achievement of peak plasma levels of meloxicam after oral administration. Meloxicam is a long-acting nonsteroidal anti-inflammatory drug (NSAID) with COX-2 preferential inhibition and potent pain relieving efficacy. However standard meloxicam has an extended time to maximum plasma concentration (Tmax) which delays its onset of action. AXS-06 utilizes Axsome’s proprietary MoSEIC™ (
“AXS-06 provides the benefits of oral administration and demonstrates a more rapid meloxicam Tmax than that reported with intramuscular administration, highlighting the potential for faster pain relief. In addition, AXS-06 maintains the long half-life of meloxicam which enables once-daily dosing and sustained effect,” said
The study compared the pharmacokinetics of meloxicam and esomeprazole after oral administration of AXS-06 tablets (meloxicam 15 mg, esomeprazole 40 mg), and commercially available Mobic® tablets (15 mg meloxicam) and Nexium® capsules (40 mg esomeprazole) in healthy volunteers. The median Tmax for meloxicam, the trial’s primary endpoint, was 9 times faster for AXS-06 as compared to Mobic® (0.5 hour versus 4.5 hours for AXS-06 and Mobic, respectively, p<0.0001). AXS-06 also demonstrated higher mean maximum plasma concentration (Cmax) (p=0.0018), faster time to therapeutic plasma concentration (p<0.0001), and time to half-maximal plasma concentration (p<0.0001) as compared to Mobic®. Terminal half-lives for meloxicam were similar for AXS-06 and Mobic® at approximately 20 and 22 hours, respectively. Plasma concentrations and terminal half-lives of esomeprazole after AXS-06 and Nexium® administration were comparable. AXS-06 was well tolerated with reported adverse events being similar across the three treatment arms. There were no serious adverse events in the study.
“With its differentiated profile and Phase 3-ready status, AXS-06 complements AXS-02 which is currently in Phase 3 trials in complex regional pain syndrome and knee osteoarthritis,” continued Dr. Tabuteau. “The overlapping patient and physician audiences for AXS-02 and AXS-06 should allow Axsome to leverage our commercialization efforts. We look forward to the further development of AXS-06 and to a data readout for AXS-02 in complex regional pain syndrome anticipated in the fourth quarter.”
Phase 1 Trial Design
The study was a randomized, parallel group trial to evaluate the pharmacokinetics and safety of meloxicam and esomeprazole after single and multiple dose administration of AXS-06 in healthy volunteers. A total of 30 subjects were randomly assigned in a 1:1:1 ratio to treatment with AXS-06 tablets (15 mg meloxicam, 40 mg esomeprazole), Mobic® tablets (15 mg meloxicam), or Nexium® capsules (40 mg esomeprazole), once daily for 6 days under fasting conditions. The primary endpoint was the Tmax of meloxicam. Secondary endpoints included Cmax, time to half maximum concentration, and time to therapeutic concentration.
About the NSAID Market
Nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used for the treatment of pain and arthritis. Approximately 120 million prescriptions were written for NSAIDs overall in the U.S. in 2016, of which approximately 25% were written for meloxicam. Chronic use of NSAIDs has been reported to be associated with the development of gastrointestinal ulcers in as many as 25% of patients.
AXS-06 is an oral, non-opioid, fixed-dose combination of MoSEIC™ meloxicam and esomeprazole which is being developed for the treatment of chronic pain. Meloxicam is a long-acting nonsteroidal anti-inflammatory drug (NSAID) with COX-2 preferential inhibition and potent pain-relieving efficacy. AXS-06 utilizes Axsome’s proprietary MoSEIC™ (
Forward Looking Statements
Certain matters discussed in this press release are “forward-looking statements”. We may, in some cases, use terms such as “predicts,” “believes,” “potential,” “continue,” “estimates,” “anticipates,” “expects,” “plans,” “intends,” “may,” “could,” “might,” “will,” “should” or other words that convey uncertainty of future events or outcomes to identify these forward-looking statements. In particular, the Company’s statements regarding trends and potential future results are examples of such forward-looking statements. The forward-looking statements include risks and uncertainties, including, but not limited to, the success, timing and cost of our ongoing clinical trials and anticipated clinical trials for our current product candidates, including statements regarding the timing of initiation and completion of the trials, futility analyses and receipt of interim results; the timing of and our ability to obtain and maintain
Mark JacobsonVice President, Operations Axsome Therapeutics, Inc. 25 Broadway, 9th Floor New York, NY10004 Tel: 212-332-3243 Email: firstname.lastname@example.org www.axsome.com