Nektar Therapeutics (Nasdaq: NKTR) presented clinical study data today demonstrating that the oral tablet formulation of NKTR-118 has favorable systemic bioavailability and a low risk for mediating significant drug-drug interactions. NKTR-118, an oral peripherally-acting opioid antagonist, is in clinical development for the treatment of opioid-induced constipation. These findings were presented today at the 38th Annual American College of Clinical Pharmacology (ACCP) Meeting in San Antonio, Texas.
Oral NKTR-118 combines Nektar's advanced small molecule polymer conjugate technology platform with naloxol, a derivative of the opioid-antagonist drug, naloxone. Nektar's proprietary advanced polymer conjugate technology increases the bioavailability and half-life of naloxol, enabling NKTR-118 to act selectively in the periphery while preserving centrally-mediated opioid analgesic clinical benefits.
"The data reported today, in combination with our strong Phase 2 clinical results, support advancing the oral tablet formulation of NKTR-118 into pivotal Phase 3 studies. NKTR-118 is an excellent example of how our novel advanced polymer conjugate platform improves oral bioavailability and enables preferential distribution of a drug within the body," said Lorianne Masuoka, M.D., Chief Medical Officer of Nektar. "By significantly improving the pharmacological activity of small molecule drugs, we are building an impressive portfolio of innovative treatments for diseases with high unmet needs."
A human pharmacokinetic study conducted in 20 healthy subjects demonstrated the comparative bioavailability of NKTR-118 in tablets and solution, confirming the drug's rapid absorption profile in both formulations and demonstrating the bioequivalence of the oral tablet formulation to solution. In vitro studies demonstrated the high metabolic stability of NKTR-118 compared to naloxone. Results of in vitro testing indicate that NKTR-118 has a low potential for clinically important drug-drug interactions, thereby facilitating the combination of NKTR-118 with a wide range of drugs in clinical development.
NKTR-118 Phase 2 Clinical Trial Data to be presented in Oral Plenary Session at ACG 2009