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NKTR-118 Shows Substantial Oral Bioavailability and Extended Half-Life in Phase 1 Clinical Data Presented at American Pain Society Meeting
Date:5/7/2008

nution of morphine-induced miosis, a CNS effect, was observed at single oral doses of NKTR-118 of 125 mg or less. In addition, NKTR-118 at single doses up to 1,000 mg was well-tolerated. The drug was rapidly absorbed with dose-proportional pharmacokinetics over the 8-1,000 mg dose range.

Data Presentations for NKTR-118

The poster presentation made this week at the APS Meeting, as well previous data presentations for NKTR-118, can be found on Nektar's website at http://www.nektar.com/wt/page/nktr118_media

APS Poster #210: "Results from a Phase 1, Double-Blind, Randomized, Placebo-Controlled, Multiple-Dose Study Evaluating the Safety, Tolerability and Pharmacokinetics of Oral Doses of NKTR-118 (PEG-Naloxol)"

About NKTR-118

Oral NKTR-118 is currently in a Phase 2 study to evaluate the efficacy, safety and tolerability of once-daily doses in patients with opioid-induced constipation (OIC). The investigational drug combines Nektar's advanced small molecule PEGylation technology platform with naloxol, a derivative of the opioid-antagonist drug, naloxone. In a Phase 1 clinical study, Nektar's PEGylation technology has been shown to reduce penetration of oral NKTR-118 across the blood-brain barrier, an important potential advance for this and possibly many other small molecule therapies.

The antagonist NKTR-118 targets mu-opioid receptors within the enteric nervous system, which mediate OBD, a symptom complex resulting from opioid use that encompasses constipation, bloating, abdominal cramping, and gastroesophageal reflux. Constipation is the hallmark of this syndrome, and is generally its most prominent component. Many studies indicate that a high percentage of patients receiving opioids are likely to experience significant constipation and other symptoms of OBD. According to IMS Health, about 230 million prescriptions were written for opioids in 2007 in the Un
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SOURCE Nektar Therapeutics
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