Selective glucocorticoid receptor modulator
Class of experimental drugs / From Wikipedia, the free encyclopedia
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Selective glucocorticoid receptor modulators (SEGRMs) and selective glucocorticoid receptor agonists (SEGRAs) formerly known as dissociated glucocorticoid receptor agonists (DIGRAs) are a class of experimental drugs designed to share many of the desirable anti-inflammatory, immunosuppressive, or anticancer properties of classical glucocorticoid drugs but with fewer side effects such as skin atrophy. Although preclinical evidence on SEGRAMs’ anti-inflammatory effects are culminating,[2] currently, the efficacy of these SEGRAMs on cancer are largely unknown.
Selective glucocorticoid receptor modulator | |
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Drug class | |
Class identifiers | |
Synonyms | SEGRM; SEGRA; SEGRAM; DIGRA |
Use | Potentially atopic dermatitis, glaucoma, cataract, eye infections, and others |
Biological target | Glucocorticoid receptor |
Chemical class | Steroidal; nonsteroidal |
Legal status | |
In Wikidata |
Selective glucocorticoid receptor agonists (SEGRAs) are historically and typically steroidal in structure while selective glucocorticoid receptor modulators (SEGRMs) are typically nonsteroidal. The combined abbreviation of selective glucocorticoid receptor agonist and modulator is SEGRAM.[2] A number of such ligands have been developed and are being evaluated in preclinical and clinical testing.
SEGRAMs achieve their selectivity by triggering only a subset the glucocorticoid receptor mechanisms of action.[3][4]