Novel Opioid Prodrugs with Oral Overdose Protection: Minimizing Cost-of-Goods

Project SummaryAbstract The abuse of prescription drugs is the fastest growing drug problem in the United Statesand reducing such abuse is a national priorityWhile the most prevalent route of abuse for opioid medicines is the oral routecurrent formulationand molecular based technologies are primarily designed to resist abuse via non oral routese ginhalation and injectionConsequentlythese approaches fail to address oral abuse and overdosei eco ingestion of multiple pillsand can be easily thwarted by straightforward extraction techniquesTo address the nation s opioid abuse epidemicnovel and effective technologies need to be developed andideallyapplied widely to all prescription opioids to make them saferElysium s O P technology was designed to provide a balanced solution that takes advantage of the well established efficacy of existing opioidswhile protecting against abuse and fatal overdoseBy using a novel chemistry approachwe have created a new class of immediate release oral opioids that offer an attractive alternative to the widelyprescribed VicodinPercocetLortabNorcoetcThis novel technology couldiprotect thousands of lives each year from fatal overdoseiiprevent the primary route of misuse and abuse of prescription opioidsand disrupt the heartbreaking and often lethal progression to illicit opioide gheroinfentanyluse and addictionandiiiprovide safe and highly effective pain relief to patientsTo that endwe have successfully completed the key aims of our previously awarded Phase II Fast Track grantRDAand have identified clinical candidates that meet our target product profile and are ready to progress to IND enabling activitiesThe strategic importance of this SBIR Phase I grant is to ensure that the cost of goodsCOGsassociated with O P opioids will facilitate their development and widespread useIn additionwe intend to deliver a cost effectivescalablesafe and robust API manufacturing process for the active pharmaceutical ingredients contained in both hydrocodone and oxycodone O P drug products at kilogram scaleFurtherit is anticipated that the successful completion of the proposed Aims will significantly reduce the timecosts and risks associated with the GMP manufacturing of APIs required for IND enabling and Phasehuman clinical studiesand provide critical information to potential commercialization partners Project Narrative Prescription opioids causedoverdose deaths in the United States inaccording to the American Society of Addiction MedicineElysium s O Poral overdose protectiontechnology uniquely addresses a significant need of national importance by offering an innovative solution to reduce the risk of the oral and non oral abuse of prescription opioids byipreventing the primary route of misuse and abuse of prescription opioidsiidisrupting the heartbreaking and often lethal progression to illicit opioid usee gfentanyl and heroinand addictionandiiioffering unprecedented protection from lethal oral overdoses of prescription opioidsThe overall goal of this SBIR Phase I grant is to optimize chemistry processes and analytical methods to minimize the cost of goodsCOGsof our O P opioids to facilitate their development and widespread commercial use