First Participants Enrolled in Phase I Clinical Trial for Nociceptin Receptor Agonist by Grünenthal
Today, Grünenthal, a global leader in pain management and related diseases, announced that the first participants have been enrolled in a first-in-human Phase I clinical trial for a nociceptin (NOP) receptor agonist. The trial, which will include 90 healthy volunteers, aims to demonstrate a favourable safety and tolerability profile and confirm the pharmacokinetic characteristics of the compound after single and multiple ascending doses. The results of the trial are expected in Q3 2025.
According to Gillian Burgess, Head of Research at Grünenthal, this development is a significant step towards delivering a unique and transformative first-in-class therapy option to millions of patients suffering from chronic pain. “With a unique mechanism of action for treating chronic pain, these molecules have the potential to deliver robust pain relief combined with an improved safety profile compared to the available standard of care,” said Burgess.
Grünenthal’s research into NOP receptor agonists has shown promising results in pre-clinical studies, indicating the potential for the compounds to act as potent analgesics without abuse liability. Leveraging the clinical data obtained during the development of its NOP receptor programme, Grünenthal has now identified a candidate that shows best-in-class potency and selectivity for the NOP receptor. These properties are predicted to provide robust pain relief in a broad range of chronic pain indications without the serious central nervous system related side effects associated with available opioids.
This development is a part of Grünenthal’s commitment to delivering innovative treatment options for patients suffering from pain and related diseases. Currently, the company has multiple programmes across different stages, targets, modalities, and mechanisms of action in its R&D pipeline. Recently, Grünenthal completed a Phase I clinical trial with a Glucocorticoid Receptor Modulator (GRM) for chronic inflammatory diseases. In addition, the company is running a Phase III clinical trial with Qutenza® (capsaicin) 8% topical system in post-surgical neuropathic pain, with the aim of expanding its label in the United States. A global Phase III programme investigating the efficacy, safety and tolerability of Resiniferatoxin in patients with painful osteoarthritis of the knee is also currently ongoing.
The nociceptin (NOP) receptor is a G protein-coupled receptor whose natural ligand is the 17 amino acid neuropeptide known as nociceptin (N/OFQ). NOP receptor agonists have been shown to act as potent analgesics without abuse liability in pre-clinical models. Although the NOP receptor shares some sequence identity with opioid receptors, it possesses little or no affinity for opioid peptides or morphine-like compounds.
Grünenthal is a science-based, fully integrated pharmaceutical company with a long track record of bringing innovative treatments and state-of-the-art technologies to patients worldwide. The company’s purpose is to change lives for the better, and innovation is its passion. Headquartered in Aachen, Germany, Grünenthal has affiliates in 27 countries across Europe, Latin America, and the U.S. Its products are available in approximately 100 countries, and in 2023, the company employed around 4,400 people and achieved revenues of €1.8 billion.
For further information, please contact:
Florian Dieckmann, Head Global Corporate Affairs & Communication
Florian.Dieckmann@grunenthal.com
Christopher Jansen, Global Communication
Christopher.Jansen@grunenthal.com
References:
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