NKTR-192 is Nektar Therapeutics' product candidate for the treatment of moderate to severe acute pain. NKTR-192 is a novel mu-opioid analgesic created using Nektar's advanced polymer conjugation technology to slow drug entry into the central nervous system (CNS). By dramatically slowing the rate of drug entry into the CNS, NKTR-192 is intended to maintain opioid-like efficacy without the abuse potential associated with rapid-acting opioids.
About Opioids and Pain Management
Opioid drugs are widely prescribed in pain management and are highly effective for treatment of moderate-to-severe pain. Each year, there are over 250 million prescriptions written for these opioid painkillers in the US alone including 140 million prescriptions for acute pain indications, such as muscle injuries, post-operative pain, and kidney stones.1,2 Sales of opioids to treat acute pain conditions are over $3 billion in the US annually.1 Although prescription opioids are considered the most effective treatment for moderate-to-severe pain, their abuse has been identified by the U.S. Food and Drug Administration (FDA) and the Centers for Disease Control (CDC) as a significant public health issue. The abuse of these drugs has led to extremely high societal costs estimated in the tens of billions of dollars annually in the U.S.3
Rapid-acting opioids enter the brain quickly, frequently causing a euphoric effect, or "high" which results in high potential for drug abuse, addiction and diversion. In addition to their potential to be abused, opioids can also cause drowsiness, impacting a patient's ability to function normally. The pharmaceutical industry has invested heavily in the development of new formulations of these drugs in order to combat the abuse and diversion of these painkillers. However, these reformulations have been primarily focused on physical means of deterrence, and abusers have found ways to overcome these formulation barriers.
NKTR-192 was created using Nektar's advanced polymer conjugation technology and is designed to minimize the unwanted side effects of opioids and reduce abuse potential by slowing the rate of drug entry into the brain. In preclinical testing, NKTR-192 demonstrates a rapid onset of analgesia and relatively short half-life, without exhibiting sedative or abuse potential at analgesic doses. The unique molecular structure of the polymer drug conjugate is designed to prevent conversion of NKTR-192 into rapidly-acting, more abusable opioid.
NKTR-192 is currently in Phase 1 clinical studies to assess the pharmacokinetics and safety of NKTR-192 in healthy subjects.
|November 13, 2011
||Neuroscience 2011: Society for Neuroscience Annual Meeting
DATE: November 13, 2011
TIME: 8:00 AM - 12:00 PM Eastern Time
ABSTRACT TITLE: "Pharmacological characterization of an orally active opioid analgesic with rapid onset of activity and low abuse liability." Harrison, S., et al.
ABSTRACT POSTER NUMBER: #178.10/NN20
SESSION TITLE/TRACK: "Pharmacology Relevant to Pain, Addiction, and Development"
1 IMS Health, 2010.
2 Defined Health Research
3 Birnbaum et al. (2011) Pain Medicine 12(4): 657-667.