Ensysce Biosciences initiates final stage of Phase 1 study of PF614-MPAR

Ensysce Biosciences announced the initiation of the final stage of the Phase 1 study of PF614-MPAR. PF614-MPAR is the overdose protection version of its lead product, PF614, and this key study is being conducted in healthy subjects by Dr. Maria Bermudez MD, at Quotient Sciences, Miami, Florida. PF614, a TAAP prodrug of oxycodone, has a number of safety features designed to reduce abuse, including its extended-release profile that has been shown to reduce ‘drug liking’ in recreational drug users. Additionally, its requirement for exposure to the enzyme trypsin to release oxycodone reduces the ability of recreational users to chew, crush and snort, or manipulate and inject to change the opioid release profile. The combination product PF614-MPAR has another layer of safety, with an added trypsin inhibitor to prevent overdose. PF614-MPAR is designed to provide optimal pain relief at prescribed doses. Accidental or intentional overdose is designed to be limited by the overdose protection built into each capsule with the addition of Ensysce’s formulated trypsin inhibitor, nafamostat. With MPAR technology, the target dose of one or two prescribed PF614-MPAR capsules will release the expected concentration of oxycodone required to provide pain relief as intended. However, when three or more capsules are taken, exceeding the target dose, the increased exposure to nafamostat progressively inhibits the release of oxycodone from the excess PF614 ingested. This allows the inactive drug to pass through the body, thus averting an overdose. The recently completed initial stage of the trial sought to optimize PF614-MPAR for both release rate and ratio of the combination. Data from the trialdemonstrated that PF614-MPAR could deliver oxycodone similarly toPF614, which was the goal of the study. In line with expectations, the results of the study demonstrated that an overdose of PF614-MPAR would result in diminished oxycodone release and uptake as compared to an equivalent amount of PF614. In the final stage of the study, the selected PF614-MPAR formulation will be evaluated by measuring oxycodone release from increasing dose units delivered to a group of healthy subjects.