FEBRUARY 16, 2024
LAS VEGAS—As America remains gripped by the opioid crisis, with 106,000 opioid-related deaths in 2022, drug companies look for new agents designed to deter abuse while effectively managing pain.
To this end, Ensysce Biosciences Inc., a clinical-stage pharmaceutical company in La Jolla, Calif., presented two studies examining the safety and effectiveness of two “next-generation” analgesics, PF614 and PF614-MPAR (multi-pill abuse resistance), at the 2023 annual PAINWeek
LAS VEGAS—As America remains gripped by the opioid crisis, with 106,000 opioid-related deaths in 2022, drug companies look for new agents designed to deter abuse while effectively managing pain.
To this end, Ensysce Biosciences Inc., a clinical-stage pharmaceutical company in La Jolla, Calif., presented two studies examining the safety and effectiveness of two “next-generation” analgesics, PF614 and PF614-MPAR (multi-pill abuse resistance), at the 2023 annual PAINWeek conference.
Ensysce chief medical officer William Schmidt, MD, presented one of the papers on an extended-release oxycodone prodrug. “Ensysce next-generation opioids use a chemical approach to reduce abuse called trypsin-activated abuse protection [TAAP],” said Schmidt, adding that “trypsin exists in the ‘gut’ only and is chemically designed to create a release timing of one to six hours.” Ensysce says its technology will reduce opioid abuse.
Ensysce is using its TAAP and MPAR platforms to develop unique, tamper-proof treatment options for pain that minimize the risk for drug abuse and overdose, according to the company. Ensysce’s products are anticipated to provide safer options to treat patients with severe pain and assist in preventing deaths caused by medication abuse.
The data presented build a picture of unique safety combined with powerful pain relief, charting the progress of these drugs in development from animal models to compelling human clinical data, according to Ensysce CEO Lynn Kirkpatrick.
“The medication has to be swallowed, and you cannot get around or circumvent it; it is not what addicts or SUD [substance use disorder] patients are seeking,” Kirkpatrick said. “We call it ‘clever chemistry’ because the trypsin inhibitor in the MPAR recognizes and controls the release of the opioids.
“The issue of opioid abuse has led to major problems for some people who live in chronic severe pain and who need an opioid medication,” she said. “Many have found reduced access to their life-changing medication due to the restrictions that have been put on opioid prescribing.”
“There are few true innovations in the treatment of severe pain. I see the Ensysce approach as a potential game changer when opioids are needed for the treatment of pain,” said Jeff Gudin, MD, a faculty member in the Department of Anesthesiology and Pain Management at the University of Miami, and a Pain Medicine News editorial advisory board member, who also presented Ensysce data at PAINWeek. “Clinicians need treatment options, and patients in severe pain need the best and safest approaches available. I support any new products that provide effective analgesia with added safety features and especially overdose protection.
“All ADFs [abuse-deterrent formulations] are also not the same,” he said. “ADF properties deter but do not prevent abuse. There are ways an ADF can be abused. You have to look at the claim. How has the drug earned its abuse-deterrent credentials, if you will?”
According to the results of a Substance Abuse and Mental Health Services Administration 2019 National Survey on Drug Use and Health, which included 1,000 chronic pain patients, 10% will crush, chew or grind up the pill form of the opioid delivery system. This is not a nefarious matter in all cases. “They may have trouble swallowing the pill,” said Lynn Webster, MD, a senior fellow at the Center for U.S. Policy, in Washington, D.C., and a Pain Medicine News editorial advisory board member. “Sixty-five percent did not know there was a problem doing it this way. They are making it easier to swallow and not attempting to [misuse] or abusing long-acting opioids. Often, the patient just doesn’t know they are doing it wrong.
“An opioid abuser often tries to take opioids orally, chew, crush and dissolve them. They are also trying to get a faster onset of action. People break pills in half splitting them, such as an ER [extended-release] tablet. This changes the pharmacokinetic action of the medicine,” Webster said.
“PF614-MPAR could be the first opioid product with the abuse resistance and the opioid overdose protection already built in,” Schmidt said. “It’s pain relief with overdose protection.”
—Mike Smith
Kirkpatrick and Schmidt are employees of Ensysce. Webster is on the Ensysce scientific advisory board.
