Nektar Therapeutics (Nasdaq: NKTR) announced today that positive data from the first single-ascending dose Phase 1a clinical study of NKTR-192, the company's novel short-acting mu-opioid analgesic candidate, demonstrate that the drug candidate achieved its target pharmacokinetic profile. These data support its continued development as a new analgesic for the treatment of acute pain. The company also announced that dosing has commenced in a second single-ascending dose Phase 1a clinical study of NKTR-192, which will explore the pharmacodynamic profile of this new drug candidate in healthy subjects.
NKTR-192 is a new mu-opioid agonist molecule designed to have a short-acting profile and onset of pain relief suitable for the treatment of acute pain, but with a reduced rate of entry into the CNS as compared to other fast-acting opioids used to treat acute pain, such as Vicodin® and Percocet®.
"With prescription opioid abuse at epidemic levels in the United States, we need new thinking, new approaches and new molecules to address this serious problem," said Robert Medve, M.D., Chief Medical Officer of Nektar Therapeutics. "With NKTR-192, we set out to build a new molecule that behaves differently than other opioids, preserving the powerful pain relief but changing the way it enters the brain and how it targets receptors throughout the body. The way we have engineered NKTR-192 may allow us to reduce the euphoria, or rush, that can drive opioid abuse and dependence, while at the same time reducing other unwanted CNS side effects, such as sedation. These potential unique characteristics of NKTR-192 are built into the molecular design – this is designed to be different."
The second Phase 1a clinical study will assess the pharmacodynamic profile and tolerability of single ascending doses of NKTR-192 in up to 48 healthy subjects. The Phase 1 clinical development program is being conducted in the United States at Lifetree Clinical Research.
"Results from our first clinical study of NKTR-192 demonstrated that this new mu-opioid molecule achieved a short-acting pharmacokinetic profile which is ideal for the treatment of acute pain," continued Dr. Medve. "In our second clinical study, we will measure multiple pharmacodynamic endpoints, including indicators of CNS entry and models of analgesia in healthy volunteers. NKTR-192 is an excellent addition to Nektar's pain portfolio and we look forward to the continued development of this new mu-opioid analgesic molecule in the clinic."
In preclinical studies, NKTR-192 has demonstrated a reduced rate of entry into the central nervous system, demonstrating the potential to greatly reduce the euphoria that underlies opioid abuse and dependence, as well as other unwanted CNS side effects, such as sedation. The unique characteristics of NKTR-192 are physically engineered into its new molecular design so its potential differentiating properties are inherent to the molecule.