NKTR-118 Shows Substantial Oral Bioavailability and Extended Half-Life in Phase 1 Clinical Data Presented at American Pain Socie...(as evidenced by a steep increase of plas...),Health

Date:5/7/2008

as evidenced by a steep increase of plasma NKTR-118 concentration. Plasma concentrations of NKTR-118-glucuronide were approximately 100-fold less than plasma NKTR-118 concentrations. Studies have shown that the bioavailability of oral naloxone is limited by first-pass metabolism of naloxone.(1)

"The prevalence and impact of opioid-bowel dysfunction among chronic pain patients are underestimated today," said Sunil J. Panchal, M.D., President of the National Institute of Pain and the Coalition for Pain Education (COPE) Foundation. "The condition can have a serious deleterious impact on a patient's quality of life and can also limit chronic pain management treatments. There is a clear need for an oral therapy that targets the underlying cause of OBD while preserving the desired analgesic effects of opioid treatment."

About the Phase 1 Clinical Trial

The primary objective of this Phase 1 multi-dose, double-blind, randomized, placebo-controlled study was to evaluate the safety and tolerability of multiple doses of oral NKTR-118 in healthy human subjects not receiving opioid therapy. A total of 32 subjects enrolled in the trial. The secondary objective of the trial was to evaluate the pharmacokinetics of oral NKTR-118 and its metabolite (NKTR-118 glucuronide) following twice-daily oral administration for seven days. Escalating doses up to 250 mg twice daily were studied. Subjects were randomized 3:1 to NKTR-118 or placebo twice daily (every 12 hours) for seven days, with a single dose on the eighth day.

Prior Clinical Study Results for NKTR-118

Nektar previously presented results from a proof-of-principle, single-dose Phase 1 study at the American College of Clinical Pharmacology Meeting (ACCP) conference in September of 2007. In this proof-of-principle study, single oral doses of NKTR-118 antagonized morphine-induced delay in gastrointestinal transit time demonstrating the potential of the drug to relieve constipation. Further, no dimi
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