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In the Pipeline: Pain Management Formulations

November 20, 2017
A number of new pain management formulations promise to positively impact opioid prescribing and usage. Practical Pain Management highlights a few such medications emerging into the market.

Study Shows Pain Relief without Breathing Suppression

Scientists have developed new opioid pain relievers that may reduce pain on par with morphine without impacting a patient’s breathing—the primary cause of  opioid overdose, according to a Scripps Research Institute press release.1 The study, led by Bohn,2   describes a method that may widen the therapeutic window for pain treatment medications and make them safer for patients facing chronic pain.

The six-year study built on two decades of research by Bohn et al examining the G protein pathway and its link to the breathing suppression pathway (beta-arrestin pathway). Researchers tweaked the chemical structures of six specific compounds currently in drug development to systematically vary the “bias” between these two pathways. Animal studies (mice) demonstrated that the new compounds could enter the brain with the potency equal to or greater than that of morphine without respiratory impact. These compounds’ G protein signaling may allow for antinociception in the absence of respiratory suppression, said Bohn in the release.

Of note, the team also examined βarrestin–biased compounds such as fentanyl, which have known links to respiratory depression. Findings showed that the compounds preferred receptor-βarrestin2 associations with a more narrow safety margin.

Extended Release Version of MorphaBond Enters US Market

Morphine sulfate (MorphaBond) is now available in the United States in extended-release formulation, according to  November 2017 release from  Daiichi Sankyo and Inspirion Delivery Sciences.3 The abuse-deterrent opioid agonist is indicated for severe pain in patients in which previous treatments have been ineffective. MorphaBond ER is available in four dosage strengths: 15, 30, 60, and 100 mg.

“We are pleased to provide a treatment option that allows healthcare professionals to manage their patients’ chronic pain in a form that is expected to reduce the potential for intranasal and intravenous abuse,” said Ken Keller, president, administrative and commercial, at Daiichi Sankyo, in the release.

The extended-release formulation, which uses multiple overlapping abuse-deterrent barriers (SentryBond technology), is the only FDA approved single-agent ER morphine sulfate whose label includes its potential to deter abuse by both intranasal and intravenous administration, according to the release. The drug’s properties are designed to resist being cut, crushed, or broken; when combined with liquid, the medication forms a viscous material that resists passage through a needle, according to Daiichi Sankyo. MorphaBond does, however still have potential risk for abuse by intranasal, intravenous, or oral routes. The company’s 3-year labeling exclusivity (set to expire in October 2018) prevents other drug developers from submitting an NDA for another single-entity extended release morphine product labeled as an intranasal abuse deterrent.

A similar product, Arymo ER by Egalet US, was approved by FDA in January 2017 to treat severe pain and touts a formulation that makes abuse by injection difficult. Both products fall under the agency’s Opioid Action Plan and the increased focus among pharmaceutical developers to craft abuse- deterrent products. 

Investigational Opioid Use Disorder Drugs Move toward Final FDA Approvals

A buprenorphine depot injection in development for the treatment of adults with opioid use disorder has been approved by FDA’s Psychopharmacologic Drugs Advisory Committee, and its Drug Safety and Risk Management Advisory Committee, according to a press release from Braeburn Pharmaceuticals.4 Known as CAM2038, the once-monthly and once-weekly depot subcutaneous injection, to be administered in a healthcare setting, provides an opportunity for individualized treatment, said Braeburn President and CEO Mike Derkacz in the release.

The fast-tracked drug recently completed seven Phase 1-3 clinical trials in patients with opioid use disorder, including a pivotal Phase 3 efficacy and a long-term safety study. FDA set a Prescription Drug User Fee Act (PDUFA) target date of Jan. 19, 2018.

FDA review committees also approved Invidior’s investigational, once-monthly injectable buprenorphine medication aimed at OUD.5 Known as RBP-6000, this fast-tracked product uses the trademarked Artigel delivery system. Its Phase 3 study met the primary efficacy endpoint, with tested doses demonstrating significantly higher abstinence rates vs placebo (P< .0001), and delivered a well-tolerated safety profile consistent with that of transmucosal buprenorphine, except for injection site reactions. RBP-6000 has a PDUFA date of Nov. 30, 2017.

According to the American Psychiatric Association, medications designed to treat opioid abuse are vastly underused, with approximately 1 in 5 patients continuing opioid use after discharge from inpatient treatment.6 These new weekly and monthly OUD formulations may assist with patient compliance, which is often deterred by daily administration.

Last updated on: March 5, 2019
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Abuse-Deterrent Formulations
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