GSK870086 inhalation / GSK - LARVOL DELTA

Biased regulation of glucocorticoid receptors signaling. (PubMed, Biomed Pharmacother) - "Based on the bias regulation of GR, selective GR agonists and modulators (SEGRAMs) were developed to bias therapeutic outcomes toward expected outcomes (e.g., anti-inflammation and immunoregulation) by influencing GR-mediated gene expression. This paper provides a review of the bias regulation and mechanism of GR and the research progress of drugs."

Journal • Review • Immune Modulation • Inflammation

Dimerization of glucocorticoid receptors and its role in inflammation and immune responses. (PubMed, Pharmacol Res) - "Furthermore, some studies have shown that some selective glucocorticoid receptor agonists and modulators (SEGRAMs) have good separation characteristics (i.e., preferentially mediate the transrepression of proinflammatory genes or preferentially activate anti-inflammatory target genes). This article reviewed the formation of GR dimers, the role of GR dimers in the inflammation and immune responses, and the progress of SEGRAMs to provide novel ideas for further understanding the anti-inflammatory mechanism of GR and the development of SEGRAMs."

Journal • Review • Allergic Rhinitis • Asthma • Immunology • Inflammation • Inflammatory Arthritis • Respiratory Diseases • Rheumatoid Arthritis • Rheumatology

Experimental Glucocorticoid Receptor Agonists for the Treatment of Asthma: A Systematic Review. (PubMed, J Exp Pharmacol) - "Several compounds are currently under pre-clinical development, but only three novel experimental GR agonists (GW870086X, AZD5423, AZD7594) seem to have some potential therapeutic relevance and have entered clinical trials for the treatment of asthma. Since data from pre-clinical studies have not always been confirmed in clinical investigations, well-designed randomized controlled trials are needed in asthmatic patients to confirm the potentially positive benefit/risk ratio of each specific SEGRA and to optimize the development strategy of these agents in respiratory medicine."

Journal • Review • Asthma • Immune Modulation • Inflammation • Respiratory Diseases