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First Subjects Dosed in Phase 1 Clinical Study of NKTR-171, A New Peripherally-Restricted Sodium Channel Blocker to Treat Neuropathic Pain
Date:1/14/2014

lerable for many patients.  A peripherally-restricted sodium channel blocker with good efficacy and low CNS side effects would be an important advance in the treatment of patients with debilitating neuropathic pain."

About NKTR-171In preclinical studies, NKTR-171 demonstrated an improved efficacy and CNS side effect profile when compared to pregabalin (Lyrica®), the most highly prescribed therapy in the treatment of neuropathic pain. 2,3
NKTR-171 also exhibited significantly reduced CNS penetration versus currently-approved sodium channel blockers.2  NKTR-171 did not significantly impair motor coordination at doses demonstrating analgesia, suggesting that the therapeutic index, or the ability to provide analgesia at doses that do not cause significant CNS side effects, may be greater for NKTR-171 than for currently available therapies.2,3 In pre-clinical in vitro data, NKTR-171 was shown to produce frequency-dependent blockade of inactivated sodium channels, meaning NKTR-171 preferentially blocks the abnormal, rapidly-firing neurons associated with neuropathic pain and spares normal nerve function in unaffected tissues.2,3About Neuropathic PainNeuropathic pain, also known as nerve pain or peripheral neuropathy, is the result of nerve damage and can be caused by such diverse conditions as diabetes, shingles, cancer, HIV, multiple sclerosis and fibromyalgia, as well as injury or trauma to the nerves.  According to the Neuropathy Association, an estimated 1 in 15 Americans suffer from peripheral neuropathy4.  Its prevalence is particularly high among diabetes patients and incidence increases with age4.  Though neuropathic pain is a very common condition, the symptoms of it can be highly variable, including numbness, tingling, and pricking sensations, sensitivity to touch, or burning sensations, making diagnosis difficult.  If left untreated, peripheral
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SOURCE Nektar Therapeutics
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