AACHEN, Germany, Oct. 22, 2024 . Today, Grünenthal 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 will include 90 healthy volunteers and aims to demonstrate a favourable safety and tolerability profile and to confirm the pharmacokinetic characteristics of the compound after single and multiple ascending doses.

2024年10月22日，德国亚琛。今天，Grünenthal宣布，首批参与者已经参加了伤害感受蛋白（NOP）受体激动剂的首次人体I期临床试验。该试验将包括90名健康志愿者，旨在证明良好的安全性和耐受性，并确认单次和多次递增剂量后该化合物的药代动力学特征。

The results of the trial are expected in Q3 2025.'Grünenthal pioneered the research into NOP receptor agonists to deliver a unique and transformative first-in-class therapy option to millions of patients suffering from chronic pain,' says Gillian Burgess, Head of Research, Grünenthal. '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.'Pre-clinical data show that NOP receptor agonists have the potential to act as potent analgesics without abuse liability.1 Leveraging the clinical data Grünenthal obtained during the development of its NOP receptor programme, Grünenthal now brings forward a candidate that shows best-in-class potency and selectivity for the NOP receptor.

该试验的结果预计将于2025年第三季度公布。“Grünenthal开创了NOP受体激动剂的研究，为数百万患有慢性疼痛的患者提供了独特且具有变革性的一流治疗选择，”Grünenthal研究负责人吉莉安·伯吉斯（GillianBurgess）说与现有的护理标准相比，这些分子具有治疗慢性疼痛的独特作用机制，有可能提供强大的疼痛缓解，并改善安全性。”临床前数据显示，NOP受体激动剂有可能成为有效的镇痛药，而不会产生滥用责任。利用Grünenthal在其NOP受体计划开发过程中获得的临床数据，Grünenthal现在提出了一种候选者，该候选者显示出最佳的NOP受体效力和选择性。

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's R&D pipeline includes multiple programmes across different stages, targets, modalities, and mechanisms of action to deliver innovative treatment options for patients suffering from pain and related diseases.

预计这些特性将在广泛的慢性疼痛适应症中提供强大的疼痛缓解，而不会产生与可用阿片类药物相关的严重中枢神经系统相关副作用。Grünenthal的研发管道包括跨越不同阶段，目标，模式和行动机制的多个计划，为患有疼痛和相关疾病的患者提供创新的治疗选择。

Recently, a Phase I clinical trial with a Glucocorticoid Receptor Modulator (GRM) has been completed. The compound is deve.

最近，使用糖皮质激素受体调节剂（GRM）的I期临床试验已经完成。该化合物是开发的。