Novel selective glucocorticoid receptor modulator GRM-01 demonstrates dissociation of anti-inflammatory effects from adverse effects on glucose and bone metabolism.

ABSTRACT:

Introduction

The development of selective GR agonist and modulators (SEGRAMs) aimed to minimize the adverse effects of chronic glucocorticoid treatment (e.g., hyperglycemia and osteoporosis) by separating the transactivation and transrepression activities of the glucocorticoid receptor (GR). Herein we report the pharmacologic profile of clinical candidate GRM-01, a novel, orally available, non-steroidal SEGRAM.

Methods

In vitro GR, progesterone receptor (PR), and mineralocorticoid receptor (MR) binding and reporter gene assays were conducted to determine GRM-01 potency and selectivity. Anti-inflammatory effects were investigated in vitro using functional assays in rat and human whole blood, human lung cells, and primary fibroblast-like synoviocytes from human d

SUBMITTER: Jakob F 

PROVIDER: S-EPMC11920646 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature