Grünenthal Announces Enrollment of First Participants in Phase I Clinical Trial for NOP Receptor Agonist
Aachen, Germany, 22 October 2024 – Grünenthal, a global leader in pain management and related diseases, has announced the enrollment of the first participants in a first-in-human Phase I clinical trial for a nociceptin (NOP) receptor agonist. The trial, which aims to demonstrate a favorable safety and tolerability profile and confirm the pharmacokinetic characteristics of the compound, will include 90 healthy volunteers. The results of the trial are expected in Q3 2025.
According to Gillian Burgess, Head of Research at Grünenthal, the company is pioneering the research into NOP receptor agonists to provide a unique and transformative first-in-class therapy option for the millions of patients suffering from chronic pain. These molecules have a unique mechanism of action that has shown potential to deliver robust pain relief with an improved safety profile compared to current standard of care.
Pre-clinical data has shown that NOP receptor agonists have the potential to act as potent analgesics without abuse liability. Leveraging the clinical data obtained during the development of its NOP receptor program, Grünenthal has brought forward a candidate that demonstrates 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.
Grünenthal has a diverse R&D pipeline that includes multiple programs across different stages, targets, modalities, and mechanisms of action aimed at providing innovative treatment options for patients suffering from pain and related diseases. Recently, the company completed a Phase I clinical trial with a Glucocorticoid Receptor Modulator (GRM), which is being developed to provide patients with a therapy option for chronic inflammatory diseases. Grünenthal is also currently running a Phase III clinical trial with Qutenza® (capsaicin) 8% topical system in post-surgical neuropathic pain, with the goal of expanding its label in the United States. Additionally, a global Phase III program investigating the efficacy, safety and tolerability of Resiniferatoxin in patients with painful osteoarthritis of the knee is currently ongoing.
The 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, there is little or no affinity for opioid peptides or morphine-like compounds. Likewise, opioid receptors possess little affinity towards NOP’s endogenous ligand nociceptin.
Grünenthal is a science-based, fully integrated pharmaceutical company headquartered in Aachen, Germany. With affiliates in 27 countries across Europe, Latin America, and the U.S., their products are available in approximately 100 countries. In 2023, Grünenthal employed around 4,400 people and achieved revenues of €1.8 billion. The company’s purpose is to change lives for the better through its passion for innovation and dedication to providing effective pain management and related disease treatments.
For more information, please visit https://www.grunenthal.com. Follow Grünenthal on LinkedIn at Grunenthal Group and on Instagram at grunenthal.
For further information, please contact:
Florian Dieckmann, Head Global Corporate Affairs & Communication
Florian.Dieckmann@grunenthal.com
Christopher Jansen, Global Communication
Christopher.Jansen@grunenthal.com
Reference:
[1] Lin AP, Ko MC. The therapeutic potential of nociceptin/orphanin FQ receptor agonists as analgesics without abuse liability. ACS Chem Neurosci. 2013 Feb 20;4(2):214-24. doi: 10.1021/cn300124f. Epub 2012 Nov 6. PMID: 23421672; PMCID: PMC3582300.
[2] Henderson G, McKnight AT (August 1997). “The orphan opioid receptor and its endogenous ligand– nociceptin/orphanin FQ”. Trends in Pharmacological Sciences. 18 (8): 293–300. doi:10.1016/S0165- 6147(97)90645-3. PMID 9277133.
[3] Butour JL, Moisand C, Mazarguil H, Mollereau C, Meunier JC (February 1997). “Recognition and activation of the opioid receptor-like ORL 1 receptor by nociceptin, nociceptin analogs and opioids”. European Journal of Pharmacology. 321 (1): 97–103. doi:10.
