SAN FRANCISCO, Sept. 19, 2014 /PRNewswire/ -- Nektar
Therapeutics (NASDAQ:NKTR) today announced results from preclinical
studies characterizing the analgesic profiles of a series of the
company's internally-discovered oral, peripherally-acting kappa
opioid receptor agonist molecules. The preclinical research
candidates were created using Nektar's small molecule polymer
medicinal chemistry platform.
The analgesic properties of kappa receptor agonism are well
described in the medical literature.1,2 Kappa opioid
receptors are expressed in the peripheral nervous system as well as
in the central nervous system (CNS), and activation of these
receptors at both sites has been shown to result in a reduction in
pain and inflammation in a wide range of preclinical
models.1,4 However, the therapeutic use of kappa
receptor agonists has been limited because activation of these
receptors in the CNS is associated with significant dysphoria and
other unwanted side effects (i.e., anxiety, restlessness and
fidgeting).3
"We are encouraged by the results of our research, which shows
that we can achieve efficacy through the peripheral activation of
the kappa opioid receptor, while at the same time reducing the side
effects observed with centrally-acting kappa agonist molecules,"
said Stephen K. Doberstein, Ph.D.,
senior vice president and chief scientific officer of Nektar
Therapeutics. "With this research, we are continuing to capitalize
on the ability of our small molecule polymer medicinal chemistry
platform to create new peripherally-acting molecules that could
address different pain conditions."
Results presented showed that a series of novel, oral,
peripherally-acting kappa agonist molecules demonstrated a 15-fold
improved therapeutic index (separation between efficacy and
CNS-mediated side effects) compared with kappa agonist molecules
that were not peripherally selective. The preclinical data is being
presented today at the American Academy of Pain Management Annual
Meeting (Choi IY, et al. Characterization of novel, oral
peripherally-acting kappa agonists in preclinical models).
About Nektar
Nektar Therapeutics has a robust R&D
pipeline of potentially high-value therapeutics in pain, oncology,
hemophilia and other therapeutic areas. In the area of pain, Nektar
has an exclusive worldwide license agreement with AstraZeneca for
MOVANTIKTM, the first FDA-approved once-daily oral
peripherally-acting mu-opioid receptor antagonist (PAMORA)
medication for the treatment of opioid-induced constipation (OIC),
in adult patients with chronic, non-cancer pain. The AstraZeneca
agreement also includes NKTR-119, an earlier stage development
program that is a co-formulation of MOVANTIK and an opioid.
NKTR-181, a wholly-owned mu-opioid analgesic molecule for chronic
pain conditions, has completed Phase 2 development. NKTR-171, a
wholly-owned new sodium channel blocker being developed as an oral
therapy for the treatment of peripheral neuropathic 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. In
hemophilia, BAX 855, a longer-acting PEGylated Factor VIII
therapeutic is in Phase 3 development conducted by partner
Baxter. In anti-infectives,
Amikacin Inhale is in Phase 3 studies conducted by Bayer Healthcare
as an adjunctive treatment for intubated and mechanically
ventilated patients with Gram-negative pneumonia.
Nektar's technology has enabled nine approved products in the
U.S. or Europe through
partnerships with leading biopharmaceutical companies, including
AstraZeneca's MOVANTIK, 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.
MOVANTIK is a trademark of the AstraZeneca group of
companies.
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," "may," "will" and similar references to future periods.
Examples of forward-looking statements include, among others,
statements regarding the potential of our polymer medicinal
chemistry platform and drug candidates such as our proprietary
kappa opioid receptor agonist molecules. Forward-looking statements
are neither historical facts nor assurances of future performance.
Instead, they are based only on our current beliefs, expectations
and assumptions regarding the future of our business, future plans
and strategies, anticipated events and trends, the economy and
other future conditions. 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) positive preclinical
findings, such as those for our proprietary kappa opioid receptor
agonist molecules, are subject to inherent scientific and medical
uncertainties typical for this early stage of drug development and
may not be confirmed in subsequent preclinical studies or in
clinical trials; (ii) our drug candidates and those of our
collaboration partners are in various stages of clinical
development and the risk of failure is high and can unexpectedly
occur at any stage prior to regulatory approval for numerous
reasons including safety and efficacy findings even after positive
findings in previous preclinical and clinical studies; (iii)
scientific discovery of new medical breakthroughs is an inherently
uncertain process and the future success of applying our technology
platform to potential new drug candidates (such as our kappa opioid
receptor agonist molecules) is therefore highly uncertain and
unpredictable and one or more research and development programs
could fail; (iv) patents may not issue from our patent
applications, patents that have issued may not be enforceable, or
additional intellectual property licenses from third parties may be
required; and (v) certain other important risks and uncertainties
set forth in our Quarterly Report on Form 10-Q filed with the
Securities and Exchange Commission on August
1, 2014. Any forward-looking statement made by us in
this press release is based only on information currently available
to us and speaks only as of the date on which it is made. 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.
1. Machelska H, et al. Peripheral effects of the kappa-opioid
agonist EMD 61753 on pain and inflammation in rats and humans. J
Pharmacol Exp Ther. 1999;290(1): 354-61.
2. Hope PJ, Fleetwood-Walker SM, Mitchell R. Distinct
antinociceptive actions mediated by different opioid receptors in
the region of lamina I and laminae III-V of the dorsal horn of the
rat. Br J Pharmacol. 1990101(2): 477-83.
3. Vanderah TW, et al. Novel D-amino acid tetrapeptides produce
potent antinociception by selectively acting at peripheral
kappa-opioid receptors. Eur J Pharmacol. 2008.
583(1):62-72.
4. Millan MJ, et al. Inflammation of the hind limb as a model of
unilateral, localized pain: influence on multiple opioid systems in
the spinal cord of the rat. Pain. 1988;35(3):299-312.
Contact:
Investors
Jennifer Ruddock of Nektar
Therapeutics
415-482-5585
Media
Nadia Hasan of WCG
212-257-6738
SOURCE Nektar Therapeutics