ABSTRACT
Introduction: The beneficial effects of glucocorticoids are highly regarded in the treatment of inflammatory diseases. In rheumatoid arthritis, these drugs are widely used because they effectively reduce signs and symptoms of the disease, and exert disease-modifying effects. However, both patients and physicians frequently associate glucocorticoids with a variety of adverse effects which hamper adherence. Due to this ambivalent nature of these drugs, several new glucocorticoids or glucocorticoid receptor ligands are being developed, aiming at improving their benefit-risk balance.
Areas covered: Focussing on rheumatoid arthritis, we discuss current approaches to achieve this goal, including an optimized application of conventional glucocorticoids and the development of novel formulations aiming at minimizing adverse effects while keeping or even enhancing the anti-inflammatory efficacy.
Expert opinion: Glucocorticoids – be it conventional or modified/delayed-release formulations – have so far been convincing in clinical practice, and their widespread use will therefore continue. They are not likely to be replaced by novel drugs in the near future although some investigational preparations are promising, and results obtained from currently ongoing clinical trials in humans are eagerly awaited. As a result of these developmental activities, a further improvement of the benefits-risk balance of glucocorticoids or glucocorticoid receptor ligands is expected.
Article highlights
Conventional GCs have been successfully in use for more than 65 years.
Adverse effects of GCs remain a matter of concern.
The modification of conventional GCs enables an improved benefit-risk balance.
Novel formulations aim at avoiding adverse effects by specifically targeting transrepression.
Clinical data on novel GC preparations and new drug delivery systems are pending.
This box summarizes key points contained in the article.
Declaration of interest
J. W. J. Bijlsma has received consultancy fees from Horizon Pharma, Mundipharma, Enceladus and SUN. F. Buttgereit has received consultancy fees, honoraria and travel expenses from Merck Serono, Horizon Pharma (formerly Nitec), Mundipharma International and Roche. F. Buttgereit has also received grant support from Merck Serono and Horizon Pharma. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.