BI 653048

BI 653048 is a selective, orally active, nonsteroidal glucocorticoid receptor agonist developed by Boehringer Ingelheim as a "dissociated" GR agonist, meaning it displays different regulatory profiles between gene transrepression and transactivation. It was designed to provide anti-inflammatory efficacy similar to traditional glucocorticoids but with reduced side effects. In clinical studies, BI 653048 demonstrated comparable anti-inflammatory effects to prednisolone but did not fully separate the desired efficacy from the typical side-effect profile of glucocorticoid steroids. The compound also inhibits several cytochrome P450 isoforms (CYP1A2, CYP2D6, CYP2C9, CYP2C19, and CYP3A4) and has low affinity for the hERG ion channel. It has been evaluated in Phase I clinical trials for its safety and pharmacodynamics in healthy subjects.

Other names

(R)-2-(4-((5-(Ethylsulfonyl)-1H-pyrrolo[2,3-c]pyridin-2-yl)methyl)-5,5,5-trifluoro-4-hydroxy-2-methylpentan-2-yl)-5-fluorobenzamideUNII-KQ33EVH4KUUNII-KQ-33EVH4KUUNII-KQ 33EVH4KUCHEMBL3358954CHEMBL-3358954CHEMBL 33589541198784-72-3KQ33EVH4KUKQ-33EVH4KUKQ 33EVH4KU