History
Synthetic steroids with SEGRA-like properties were already discovered in the late 1990s. During the 2000s, many potential SEGRAs were synthesized, most of them having non-steroidal structures. Compounds were investigated in cellular models, which established that these molecules bind to the glucocorticoid receptor with an affinity similar to dexamethasone, a potent glucocorticoid, and that they are able to repress the production of inflammatory mediators such as interleukin 6 and prostaglandin E2. Studies in mice showed that a topically administered SEGRA inhibited peroxidase activity and formation of oedema, both indicators of anti-inflammatory activity, comparably to prednisolone. Skin atrophy in rats was significantly less pronounced than under prednisolone in the same study, and metabolic effects like weight gain or increase of blood glucose were practically inexistent.
Phase II clinical trials with one of the candidate compounds, mapracorat (code names BOL-303242-X and ZK 245186), started in summer 2009. One was a double blind dose finding study for an ointment against atopic dermatitis conducted by Intendis, a part of Bayer HealthCare Pharmaceuticals specialized on dermatology. A Phase III trial started in November 2010, evaluating an ophthalmic suspension for the treatment of inflammation following cataract surgery, conducted by Bausch & Lomb.
Read more about this topic: Selective Glucocorticoid Receptor Agonist
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