Nektar (NKTR) Reports 'Statistically Meaningful' Data for NKTR-181
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Nektar Therapeutics (Nasdaq: NKTR) 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.
Data presented at AAPM show the positive analgesic properties of NKTR-181 in humans. NKTR-181 produced dose-dependent analgesic responses in two separate models of pain used to measure central and peripheral analgesic activity in healthy subjects. In a cold-pressor test pain model measuring latency-to-hand-removal (LHR), the 200 mg dose of NKTR-181 given twice-daily over the 8-day dosing period demonstrated the extent and duration of analgesic effect of NKTR-181 administration. Results show a significant analgesic effect as compared to placebo (P<0.01, n=12) over the entire dosing period. In addition, a model of induced UVB injury was also used to demonstrate the extent and duration of analgesic effect produced by NKTR-181. Results show that NKTR-181 has both centrally-mediated and peripherally-mediated analgesic effects. In this model, data was presented on NKTR-181 at doses of 300 mg and 400 mg demonstrating its significant analgesic and anti-hyperalgesic effect (measured as change from baseline) following mechanical and thermal stimulation, with p-values of P<0.009 and P<0.03, respectively (n=12).
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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.
Data presented at AAPM show the positive analgesic properties of NKTR-181 in humans. NKTR-181 produced dose-dependent analgesic responses in two separate models of pain used to measure central and peripheral analgesic activity in healthy subjects. In a cold-pressor test pain model measuring latency-to-hand-removal (LHR), the 200 mg dose of NKTR-181 given twice-daily over the 8-day dosing period demonstrated the extent and duration of analgesic effect of NKTR-181 administration. Results show a significant analgesic effect as compared to placebo (P<0.01, n=12) over the entire dosing period. In addition, a model of induced UVB injury was also used to demonstrate the extent and duration of analgesic effect produced by NKTR-181. Results show that NKTR-181 has both centrally-mediated and peripherally-mediated analgesic effects. In this model, data was presented on NKTR-181 at doses of 300 mg and 400 mg demonstrating its significant analgesic and anti-hyperalgesic effect (measured as change from baseline) following mechanical and thermal stimulation, with p-values of P<0.009 and P<0.03, respectively (n=12).
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