First subjects enrolled in Phase I trial of NOP receptor agonist

AACHEN, Germany, October 22, 2024 – Grünenthal has commenced a groundbreaking clinical trial by enrolling the first participants in a Phase I study for a nociceptin (NOP) receptor agonist. This initial trial will involve 90 healthy volunteers and aims to verify the safety and tolerability of the compound, as well as its pharmacokinetic properties when administered in both single and multiple escalating doses. The results from this study are anticipated by the third quarter of 2025.

Gillian Burgess, Head of Research at Grünenthal, highlighted the significance of their work on NOP receptor agonists, which has the potential to offer a novel and transformative treatment option for chronic pain sufferers. According to Burgess, these molecules, with their unique mode of action, promise substantial pain relief while potentially offering a better safety profile compared to existing treatments.

Pre-clinical data has indicated that NOP receptor agonists may serve as powerful pain relievers without the risk of abuse. Building on the clinical data acquired through its NOP receptor program, Grünenthal is advancing a candidate that exhibits superior potency and selectivity for the NOP receptor. This is expected to provide substantial pain relief across various chronic pain conditions without the severe central nervous system side effects often linked with current opioid treatments.

Grünenthal’s research and development pipeline is robust, encompassing multiple programs at different stages, targeting various mechanisms and modalities to develop innovative treatments for pain and related disorders. Recently, Grünenthal completed a Phase I clinical trial for a Glucocorticoid Receptor Modulator (GRM) aimed at treating chronic inflammatory diseases. In parallel, a Phase III clinical trial is underway for Qutenza® (capsaicin) 8% topical system to address post-surgical neuropathic pain, with the goal of expanding its label in the United States. Additionally, a global Phase III program is investigating Resiniferatoxin’s efficacy, safety, and tolerability in patients with painful osteoarthritis of the knee.

The nociceptin (NOP) receptor is a G protein-coupled receptor, naturally binding with the neuropeptide nociceptin (N/OFQ). Pre-clinical studies have demonstrated that NOP receptor agonists can act as effective analgesics without the potential for abuse. Despite sharing some sequence identity with the opioid receptors μ-OP (MOP), κ-OP (KOP), and δ-OP (DOP), NOP receptors do not exhibit significant affinity for opioid peptides or morphine-like compounds, and vice versa.

Grünenthal is a leading global entity in pain management and related conditions. As an integrated pharmaceutical company grounded in scientific research, Grünenthal has a history of delivering innovative treatments and advanced technologies to patients globally. The company’s mission is to improve lives through innovation, with a vision of a world free of pain. Headquartered in Aachen, Germany, Grünenthal operates in 27 countries across Europe, Latin America, and the U.S., with its products available in approximately 100 countries. In 2023, Grünenthal employed around 4,400 people and reported revenues of €1.8 billion.