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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

SAN FRANCISCO, Jan. 14, 2014 /PRNewswire/ -- Nektar Therapeutics (Nasdaq: NKTR) today announced that the first subjects were dosed in a Phase 1 clinical study for NKTR-171, a new sodium channel blocker being developed as an oral therapy for the treatment of peripheral neuropathic pain.  The single-ascending dose Phase 1 clinical study of NKTR-171 will assess its pharmacokinetics, tolerability, and safety in up to 50 healthy subjects.  NKTR-171 is a new molecular entity that is specifically designed to treat neuropathic pain by blocking hyperactive neuronal sodium channels associated with damaged nerves in the peripheral nervous system.Chronic neuropathic pain arises from nerves injured or damaged by systemic disease, infection, toxins, or physical trauma that are in a continuous state of hyper-excitability, often due to aberrant sodium channel firing. This hyper-excitability results in transmission of abnormal pain signals from the periphery to the central nervous system (CNS).1 Existing therapies that block sodium channels have been shown to provide effective pain relief but are typically associated with significant unwanted CNS side effects, including dizziness, ataxia and somnolence.  NKTR-171 is designed to be a peripherally-restricted molecule which selectively blocks hyper-excitable sodium channels without causing the CNS side effects that limit usage of existing therapies.

"Neuropathic pain is estimated to affect more than 20 million people in the US alone and is characterized by symptoms of burning pain and painful hypersensitivity," said Robert Medve, MD, Nektar's Chief Medical Officer.  "While conventional sodium channel blockers have demonstrated efficacy in addressing peripheral nerve pain, the CNS-mediated side effects associated with these medicines make the treatment into
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