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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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1. Nektar to Announce Financial Results for the Fourth Quarter and Year-End of 2011 on Wednesday, February 29, 2012, After Close of U.S.-Based Financial Markets
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
4. Nektar to Announce Financial Results for the Third Quarter of 2011 on Wednesday, November 2, 2011, After Close of U.S.-Based Financial Markets
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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8. Nektar to Announce Financial Results for the Second Quarter of 2011 on Thursday, August 4, 2011, After Close of U.S.-Based Financial Markets
9. Nektar Therapeutics President and CEO Howard W. Robin to Present at the Jefferies 2011 Global Healthcare Conference in New York
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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