Addictionisadisease.AccordingtotheNationalInstituteonDrugAbuse,addictioncanbehereditary,andcan be triggered by environmental conditions and behavior. One key environmental factor involves the ready accesstounusedprescriptionopioidsbypotentialabusers,especiallyteens. Elysiumhasdiscoveredanovelmoleculardeactivation(XpiRx?or?expiringpill?)technologythatisdesigned toeffectivelycurbthewidespreadstockpiling,diversion,abuse,andoverdoseofunusedprescriptionopioids, even by the most common route of abuse, oral ingestion. Current opioid pills lose only <1% of their potency per year, resulting in a 70-year potency half-life. Using Elysium?s XpiRx technology, prescription opioids will provide effective analgesia to pain patients, then safely and irreversibly lose their potency after their prescribed-use period lapses, rendering them (i) unattractive to recreational and chronic abusers, and (ii) significantlylesslikelytoelicitpotentiallylethalrespiratorydepressioneffectswhenoverdosed.Broadusedof Elysium?s XpiRx technology would substantially decrease the pool of opioid drugs currently available to abusersandaddicts,andreducetheriskofoverdose. Keystakeholdershaveexpressedstronginterestintechnologiestocurtaildiversionofprescriptionopioids: TheOfficeforNationalDrugControlPolicy(ONDCP)andTheNationalInstituteonDrugAbuse(NIDA) haveidentifieddiversionasahighpriorityissuebecauseitfuelstheprescriptiondrugabuseepidemic. Pharmaceutical company leaders believe that XpiRx could become a standard safety requirement for opioiddrugs(likeairbagsforautomobiles). Experts have indicated that they are not aware of any technologies in development or on the market that addressprescriptionopioiddiversion. Under our initial SBIR Fast-Track Grant (1R44DA037908), we achieved several key milestones: (i) identified lead and backup development candidates;? (ii) discovered two proprietary strategies to achieve targeted product profiles;? (iii) demonstrated proof of concept for two potential target product profiles with life-saving potential;? (iv) generated significant commercial interest;? and (v) obtained critical feedback from the FDA. We intendtobuildonthesuccessfulprogressunderourinitialFastTrackGrantwiththisproposedSBIRPhaseIIB Continuation Grant. The overall objective of this grant proposal is to qualify a lead XpiRx immediate-release productcandidateforhumanclinicalstudiesbycompletingrequisiteIND-enablingstudies.Theseactivitieswill have a meaningful impact on advancing our lead XpiRx product candidate toward FDA approval and a commercializationdealwithalargerpharmaceuticalcompany.
The significance of the proposed research plan is based on the contention that the initial step along the pathwayfrominitialexperimentationwithopioidstoopioidaddiction,ofteninvolvesexposureandreadyaccess to prescription opioids. The established medical paradigms involving (i) the increasing use of opioids for the treatment of pain, (ii) the often excessive number of pills prescribed to patients, and (iii) the fact that many patients retain a significant number of their unused opioids, all contribute in a significant way to the current opioid abuse and addiction epidemics. Elysium has discovered a novel molecular deactivation technology (XpiRx?or?expiringpill?)thatsafelyandirreversiblyforcesopioidstolosetheirpotencyaftertheprescribed- use period in order to effectively curb the widespread stockpiling, diversion, abuse, and overdose of unused prescriptionopioids,evenbythemostcommonrouteofabuse,oralingestion.