Aachen, Germany, 27 July 2021 – Grünenthal announced today that the first volunteers have been enrolled in a Phase I trial of its Glucocorticoid Receptor Modulator (GRM). The oral investigational medicine aims to provide a therapy option with broad anti-inflammatory efficacy and a more favourable benefit-risk profile compared to current glucocorticoid-based therapies like prednisolone.
The Phase I trial includes 80 healthy volunteers and is designed as a head to head comparison between the GRM and prednisolone, the most frequently used glucocorticoid 1. Observing several biomarkers, the trial will assess the influence of the investigational medicine on bone metabolism and glucose levels. Reduced bone formation leading to osteoporosis as well as increased blood glucose levels leading to an increased risk of diabetes are among the most common side-effects of glucocorticoids, which are a strong limitation for their long-term use at highly effective doses.2,3,4 The results of the study are expected to be available in the first quarter of 2022.
“Millions of patients rely on glucocorticoid-based therapies to manage their condition and are therefore at risk to experience severe side effects”, says Jan Adams, M.D., Chief Scientific Officer, Grünenthal. “We strive to increase the quality of life for these patients during long-term treatments by providing a therapy option that delivers a broad anti-inflammatory efficacy with significantly fewer side effects.”
The investigational medicine is a Grünenthal proprietary development and is currently the most advanced compound of the company’s Glucocorticoid Receptor Modulator programme. Preclinically, the compound has shown anti-inflammatory properties comparable to prednisolone with a lower risk of glucocorticoid receptor mediated side effects.
This Phase I trial is Grünenthal’s latest milestone in progressing its research pipeline. Recently, the company announced another Phase I trial with its Nociceptin/Orphanin Peptid Receptor (NOP)-agonist for the treatment of chronic neuropathic pain. In addition, Grünenthal announced several Phase III studies investigating the efficacy, safety and tolerability of Qutenza® (capsaicin) 8% topical system in post-surgical neuropathic pain (PSNP) and the efficacy, safety and tolerability of Resiniferatoxin in patients with pain associated with osteoarthritis of the knee. Both programmes are expected to start in 2021.
1 Robert A. Overman, Jun-Yen Yeh, and Chad L. Deal; Prevalence of Oral Glucocorticoid Usage in the United States: A General Population Perspective; Arthritis Care & Research, Vol. 65, No. 2; February 2013; pp 294 –29. DOI 10.1002/acr.21796
2 Liu X, Zhu X, Miao Q, Ye H, Zhang Z, Li Y; Hyperglycemia Induced by Glucocorticoids in Nondiabetic Patients: A Meta-Analysis; Ann Nutr Metab 2014; 65: 324-332. doi: 10.1159/000365892
3 Singh JA, Saag KG, Bridges SL Jr, Akl EA, Bannuru RR, Sullivan MC, Vaysbrot E, McNaughton C, Osani M, Shmerling RH, Curtis JR, Furst DE, Parks D, Kavanaugh A, O'Dell J, King C, Leong A, Matteson EL, Schousboe JT, Drevlow B, Ginsberg S, Grober J, St Clair EW, Tindall E, Miller AS, McAlindon T; American College of Rheumatology. 2015 American College of Rheumatology Guideline for the Treatment of Rheumatoid Arthritis. Arthritis Care Res (Hoboken). 2016 Jan;68(1):1-25. doi: 10.1002/acr.22783. Epub 2015 Nov 6. PMID: 26545825.
4 Price DB, Trudo F, Voorham J, Xu X, Kerkhof M, Ling Zhi Jie J, Tran TN; Adverse outcomes from initiation of systemic corticosteroids for asthma: long-term observational study. J Asthma Allergy. 2018; 11: 193-204 https://doi.org/10.2147/JAA.S176026
Glucocorticoids are a class of corticosteroids derived from the steroid hormone cortisol. Glucocorticoids are potent anti-inflammatory agents regardless of the cause of the inflammation and thus are used to suppress various allergic, inflammatory, and autoimmune disorders and to treat diseases caused by an overactive immune system. Long-term administration of Glucocorticoids can lead to a number of side effects, including osteoporosis and diabetes.
Grünenthal is a global leader in pain management and related diseases. As a science-based, privately-owned pharmaceutical company, we have a long track record of bringing innovative treatments and state-of-the-art technologies to patients worldwide. Our purpose is to change lives for the better – and innovation is our passion. We are focusing all of our activities and efforts on working towards our vision of a world free of pain.
Grünenthal is headquartered in Aachen, Germany, and has affiliates in 29 countries across Europe, Latin America and the US. Our products are available in around 100 countries. In 2020, Grünenthal employed around 4,500 people and achieved sales of € 1.3 bn.
More information: www.grunenthal.com
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