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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

to this new mu-opioid analgesic molecule is that it does not rely on a formulation to decrease its abuse liability. With a ten-fold slower entry into the brain as compared to oxycodone, NKTR-181 avoids the rush into the brain associated with euphoria.  Adding to our excitement is the data that shows the peripheral analgesic and anti-hyperalgesic effects of NKTR-181 in multiple pain models. We will seek to capitalize on the properties of this unique molecule as we advance NKTR-181 into Phase 2 development this year."

In a separate presentation of preclinical data at the AAPM Meeting, NKTR-181 resulted in less sedation and abuse liability as compared to oxycodone in multiple animal models across a wide range of doses.  As predicted from its molecular design, NKTR-181 has a reduced rate of entry into the brain in rodents.  This feature contributed to a 30-fold shift in the dose-response for abuse liability and a 10-fold shift in the dose response for sedation relative to oxycodone.

Chronic pain conditions, such as osteoarthritis, back pain and cancer pain, affect at least 126 million adults in the U.S. annually and contribute to over $100 billion a year in lost productivity.(2) 

About the NKTR-181 Phase 1 Multiple Ascending Dose Study

This Phase 1, double-blind, randomized, placebo-controlled, ascending multiple dose study of NKTR-181 was conducted in the U.S. at Lifetree Clinical Research. The study enrolled a total of 60 healthy subjects over an eight-day treatment period.  Four dose cohorts were evaluated with 15 subjects in each dose cohort (100 mg, 200 mg, 300 mg, 400 mg).  Subjects in each cohort received oral twice-daily doses of NKTR-181 (n=12) in aqueous solution or placebo (n=3) following an overnight fast.  Pharmacokinetics were determined through serial blood samples. Serial opioid pharmacodynamic tests included the cold-pressor test (CPT) and a UVB injury model to assess both central
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SOURCE Nektar Therapeutics
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Related medicine technology :

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
6. Nektar Initiates Second Phase 1 Clinical Study Evaluating NKTR-181, A Novel Opioid Molecule, for Treatment of Chronic Pain
7. Nektar Therapeutics Reports Second Quarter 2011 Financial Results
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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