LAS VEGAS, NV — Opioids play an important role in the treatment of moderate-to-severe pain, but with an increasing market for pain therapies, diversion and abuse have escalated as well, reported Travis Mickle, PhD, of KemPharm, North Liberty, IA , at PAINWeek 2012. Physicians and payors have expressed a need for pain medication with less potential for abuse.

Dr. Mickle and colleagues described a novel opioid derivative, KP511, which has anti-abuse properties, is tamper-resistant, and thus could potentially reduce tampering and opioid-induced constipation (OIC), while possibly protecting against oral overdose. KP511 is a prodrug composed of hydromorphone and a nontoxic ligand. When taken as directed, the prodrug is metabolized after oral administration to release the active opioid.

Preclinical studies by Dr. Mickle and colleagues suggest that KP511 exhibits unique abuse-deterrent properties by significantly limiting the narcotic exposure upon intranasal and intravenous administration and is resistant to chemical and physical extraction. Additionally, studies in rats have indicated that KP511 limits the exposure to the active opioid at high doses and may thus be the first opioid derivative with oral-abuse prevention and overdose protection. Another benefit of KP511 is its potential to prevent or reduce OIC, a troublesome side effect that afflicts many patients. KP511 appears not to cause OIC because it is biologically inactive and does not interfere with the enteric μ-opoid receptors in the gut. This theory, noted Dr. Mickle,  was confirmed by a motility study in rats.