First Subjects Dosed in Phase 1 Clinical Study of NKTR-171, A New Peripherally-Restricted Sodium Channel Blocker to Treat

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

PR Newswire

SAN FRANCISCO, Jan. 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).^1Existing 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 intolerable 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-171

In 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.^2,3

About Neuropathic Pain

Neuropathic 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 neuropathy^4. Its
prevalence is particularly high among diabetes patients and incidence
increases with age^4. 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 neuropathy can lead to
permanent nerve damage^5 and significant disability.

Today, medicines that act by blocking sodium or calcium channels such as the
gabapentinoids and anti-epileptic medications, are used in the treatment of
neuropathic pain but are known to cause significant CNS-related side effects,
such as sedation and dizziness. The sodium channel blocker lidocaine is known
to be effective in addressing peripheral nerve pain, however it is not
selective and blocks both normal and abnormal nerve conduction. The lack of an
oral form further limits its utility^5. In spite of the shortcomings of
medications currently prescribed for neuropathic pain, total U.S. sales in
2011 were $2.5 billion^6.

About Nektar

Nektar Therapeutics (NASDAQ: NKTR) is a biopharmaceutical company developing
novel therapeutics based on its PEGylation and advanced polymer conjugation
technology platforms. Nektar has a robust R&D pipeline of potentially
high-value therapeutics in oncology, pain and other therapeutic areas. In the
area of pain, Nektar has an exclusive worldwide license agreement with
AstraZeneca for naloxegol (NKTR-118), an investigational drug candidate, which
has been filed in the U.S., Europe and Canada as a once-daily, oral tablet for
the treatment of opioid-induced constipation. This agreement also includes
NKTR-119, an earlier stage development program that is a co-formulation of
fixed doses of naloxegol and opioids. NKTR-181, a novel mu-opioid analgesic
candidate for chronic pain conditions, has completed Phase 2 development in
osteoarthritis patients with chronic knee pain. NKTR-192, a novel mu-opioid
analgesic in development to treat acute pain is in Phase 1 clinical
development. In oncology, etirinotecan pegol (NKTR-102) is being evaluated in
a Phase 3 clinical study (the BEACON study) for the treatment of metastatic
breast cancer and is also in Phase 2 studies for the treatment of ovarian,
colorectal, lung and brain cancers. In anti-infectives, Amikacin Inhale is in
Phase 3 studies being conducted by Bayer Healthcare to treat patients with
Gram-negative pneumonia. Additional development-stage products that leverage
Nektar's proprietary technology platform include Baxter's BAX 855, a
longer-acting PEGylated rFVIII therapy, which is in Phase 3 clinical
development.

Nektar's technology has enabled eight approved products in the U.S. or Europe
through partnerships with leading biopharmaceutical companies, including UCB's
Cimzia^® for Crohn's disease and rheumatoid arthritis, Roche's PEGASYS^® for
hepatitis C and Amgen's Neulasta^® for neutropenia.

Nektar is headquartered in San Francisco, California, with additional
operations in Huntsville, Alabama and Hyderabad, India. Further information
about the company and its drug development programs and capabilities may be
found online at http://www.nektar.com

Cautionary Note Regarding Forward-Looking Statements

This press release contains "forward-looking statements" within the meaning of
the Private Securities Litigation Reform Act of 1995. Forward-looking
statements can be identified by words such as: "anticipate," "intend," "plan,"
"expect," "believe," "should," "could," "potential," "may" and similar
references to future periods. Examples of forward-looking statements include
our current views as to the potential of NKTR-171 to be new treatment of
peripheral neuropathic pain; the potential of NKTR-171 to exhibit reduced
CNS-related side effects that are associated with existing sodium channel
blocker therapies; the value of our pegylation and polymer conjugate
technology platform; and the potential of certain of our other drug candidates
and those of our collaboration partners. Forward-looking statements are
neither historical facts nor assurances of future performance. Instead, they
are based only on our current beliefs, expectations, observations and
assumptions regarding the potential of our business, drug candidates, and our
technology. Because forward-looking statements relate to the future, they are
subject to inherent uncertainties, risks and changes in circumstances that are
difficult to predict and many of which are outside of our control. Our actual
results may differ materially from those indicated in the forward-looking
statements. Therefore, you should not rely on any of these forward-looking
statements. Important factors that could cause our actual results to differ
materially from those indicated in the forward-looking statements include,
among others: (i) the statements regarding the therapeutic potential of
NKTR-171 are based on preclinical data only and data from clinical studies may
not confirm these potential therapeutic benefits; (ii) NKTR-171 is in early
stage clinical development and could fail at any time due to numerous
unpredictable and significant risks related to safety, efficacy and other
important findings that can negatively impact clinical development; (iii)
scientific discovery of new medical breakthroughs is an inherently uncertain
process and the future success of the application of Nektar's technology
platform to potential new drug candidates such as NKTR-171 is therefore very
uncertain and unpredictable and could unexpectedly fail at any time; (iv)
patents may not issue from our patent applications for NKTR-171 or additional
intellectual property licenses from third parties may be required; and (v) the
outcome of any potential intellectual property or other litigation related to
our proprietary drug candidates. Other important risks and uncertainties are
detailed in our filings with the Securities and Exchange Commission ("SEC"),
including without limitation, those risks and uncertainties set forth in our
Form 10-Q filed with the SEC on November 7, 2013. We undertake no obligation
to update any forward-looking statement, whether written or oral, that may be
made from time to time, whether as a result of new information, future
developments or otherwise.

Nektar Investor Inquiries:
Jennifer Ruddock/Nektar Therapeutics        (415) 482-5585
Susan Noonan/SA Noonan Communications, LLC (212) 966-3650
Nektar Media Inquiries:
Brianne Cannon                              415-512-0770

1) Devor et. al., The Journal of Pain, Vol 7, No 1S (January), Supplement 1,
2006: pp S3-S12
2) Gursahani et. al., 2013 American Pain Society 32nd Annual Meeting
3) Gursahani et. al., 2013 Fourth International Congress on Neuropathic Pain
4) Neuropathy Association; Facts
(http://www.neuropathy.org/site/PageServer?pagename=About_Facts)
5) NINDS Peripheral Neuropathy Fact Sheet
(http://www.ninds.nih.gov/disorders/peripheralneuropathy/detail_peripheralneuropathy.htm)
6) IMS Health 2011

SOURCE Nektar Therapeutics

Website: http://www.nektar.com
 
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