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
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
About Nektar
Nektar's technology has enabled nine approved products in the U.S. or
Nektar is headquartered in
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
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
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.
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