KemPharm, Inc. announced positive results from a phase I clinical trial of its most advanced opioid-based drug candidate, KP201, a novel hydrocodone prodrug for treating pain. KP201 is a New Chemical Entity (NCE) composed of hydrocodone chemically bound to a ligand.

The data confirmed that KP201 is cleaved in man as predicted, releasing the active pharmaceutical compound hydrocodone into the bloodstream at amounts equivalent to the Reference Listed Drug (RLD), Norco. Importantly, intact KP201 could not be detected in systemic circulation, indicating that minimal additional studies are warranted to determine the impact of KP201 exposure in the body.

“Our findings from this first clinical trial of KP201 are as good as we could have hoped,” stated Sven Guenther, PhD, vice president of Research at KemPharm. “The human pharmacokinetic profile of KP201 indicates that the prodrug releases hydrocodone efficiently and is bioequivalent to the comparator drug, supporting a 505(b)(2) regulatory pathway for KP201 in combination with acetaminophen. KP201 has unique physiochemical and pharmacological attributes that deliver additional patient benefits, including reduced potential for abuse as well as reduction or elimination of opioid-induced constipation.”

The phase I study was a single dose, three-treatment, three-period, six-sequence, cross-over PK study in which twenty-four healthy volunteers received oral doses of 5 mg KP201, 10 mg KP201, or 10/325 mg tablet of hydrocodone bitartrate and acetaminophen (Norco, RLD). The objectives of the study included evaluation of the serum concentrations of hydrocodone, certain metabolites, and intact KP201, as well as safety and tolerability.

“We believe KP201 has the potential to assume sizeable market share, given the opportunity for extended market exclusivity in acute and chronic pain, as well as the potential to minimize opioidinduced constipation,” commented Travis Mickle, PhD, president and chief executive officer at KemPharm. “We expect to be in a position to file an NDA for KP201 within the next 18 to 24 months, allowing us to position the product in full compliance with the FDA’s recent decision to limit acetaminophen in prescription products.”

KP201, KemPharm’s lead clinical prodrug candidate for the treatment of pain, is composed of hydrocodone attached to a ligand. Preclinical studies suggest that KP201 may exhibit unique abuse deterrent properties and lower incidence of constipation based on its physicochemical and pharmacological characteristics as compared with currently approved narcotic analgesics.

KemPharm, Inc. is focused on the discovery and development of NCEs to treat serious medical conditions through its proprietary and broadly applicable LAT prodrug approach.