Nektar Data Shows NKTR-118 Favorable Oral Bioavailability, Drug-Drug Interaction Profile

Nektar Therapeutics’ clinical study data demonstrated that the oral tablet formulation of NKTR-118 has favorable systemic bioavailability and a low risk for mediating significant drug-drug interactions. NKTR-118 is in clinical development for the treatment of opioid-induced constipation.

According to Nektar, Oral NKTR-118 combines Nektar’s small molecule polymer conjugate technology platform with naloxol. Nektar’s 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.

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 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 range of drugs in clinical development.

Lorianne Masuoka, chief medical officer of Nektar, said: “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. 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.”