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Nektar Presents Positive Proof-of-Concept Clinical Data for Its New Opioid Molecule, NKTR-181, at American Academy of Pain Medicine's 28th Annual Meeting
Date:2/27/2012

SAN FRANCISCO, Feb. 27, 2012 /PRNewswire/ -- Nektar Therapeutics (Nasdaq: NKTR) today announced a presentation of positive clinical data for NKTR-181, its new oral opioid analgesic molecule, at the 2012 American Academy of Pain Medicine's 28th Annual Meeting (AAPM). NKTR-181 is a novel mu-opioid agonist molecule, which was designed to have a slow rate of entry into the brain to reduce the attractiveness of the molecule as a target of abuse and to reduce its CNS-mediated side effects. NKTR-181 was created using Nektar's proprietary polymer conjugate technology and its differentiating properties are inherent to the design of the new molecule.  As a new molecular structure, NKTR-181 is unique in that it does not rely on a formulation approach to prevent its conversion into a more abusable form of an opioid.

Clinical results were presented at AAPM from a human Phase 1 study which evaluated the pharmacokinetics, pharmacodynamics, and safety of oral doses of NKTR-181 as compared to placebo over an 8-day treatment period in healthy subjects.  Using pupil constriction as a measure of the onset of central opioid effect, the study showed that NKTR-181 enters the brain slowly and produces centrally-mediated opioid effects that are dose-dependent and statistically meaningful (P<0.001) following twice daily oral doses of 200-400 mg.  Further, NKTR-181 enters the CNS from the plasma at a rate approximately ten-times slower than historical published rates for oxycodone.(1)  NKTR-181's slow rate of entry into the CNS may reduce the euphoria and other CNS side effects that are associated with rapid CNS uptake of current standard opioid therapies. 

"NKTR-181 is an exciting new approach to opioid analgesia," said Lynn R. Webster, MD, Medical Director of Lifetree Clinical Research. "The human data now show us that NKTR-181 crosses into the brain slowly across
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SOURCE Nektar Therapeutics
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2. Positive Data for Nektars New Mu-Opioid Analgesic Molecule to Treat Acute Pain Highlighted at Neuroscience 2011
3. Nektar Therapeutics Reports Third Quarter 2011 Financial Results
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5. Nektar Therapeutics President and CEO, Howard W. Robin, to Present at the UBS 2011 Global Life Sciences Conference in New York City
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10. Nektar Announces New Phase 2 Data for NKTR-102 to Be Presented at 2011 ASCO Annual Meeting
11. FDA Grants Orphan Drug Designation for Nektars Investigational Drug, NKTR-102, for Treatment of Women with Ovarian Cancer
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