Selective glucocorticoid receptor modulator

"DIGRA" redirects here. For the research association also known as DiGRA, see Digital Games Research Association. For other uses, see Digra.
"SEGRAM" redirects here. Not to be confused with Seagram.
Selective glucocorticoid receptor modulator
Drug class
Chemical structure of mapracorat, one of the furthest developed SEGRAs.[1]
Class identifiers
SynonymsSEGRM; SEGRA; SEGRAM; DIGRA
UsePotentially atopic dermatitis, glaucoma, cataract, eye infections, and others
Biological targetGlucocorticoid receptor
Chemical classSteroidal; nonsteroidal
Legal status
In Wikidata

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 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]

  1. ^ Cite error: The named reference Prous was invoked but never defined (see the help page).
  2. ^ a b Cite error: The named reference Sundahl P&T 2015 was invoked but never defined (see the help page).
  3. ^ Cite error: The named reference Robinson was invoked but never defined (see the help page).
  4. ^ Cite error: The named reference Biggadike was invoked but never defined (see the help page).