Treatment of inflammation is often accomplished through the use of glucocorticoids. However, their use is limited by side effects. We have examined the activity of a novel glucocorticoid receptor ligand that binds the receptor efficiently and strongly represses inflammatory gene expression. This compound has potent anti-inflammatory activity in vivo and represses the transcription of the inflammatory cytokine Monocyte Chemoattractant protein -1 (MCP-1) and induces the anti-inflammatory cytokine Interleukin 10 (IL-10). The compound demonstrates differential gene regulation compared to commonly prescribed glucocorticoids, effectively inducing some genes and repressing others in a manner different from the glucocorticoid prednisolone. The separation between the anti-inflammatory effects of LGD5552 and the side effects commonly associated with glucocorticoid treatment suggest that this molecule differs significantly from prednisolone and other steroids and may provide a safer therapeutic for inflammatory conditions now commonly treated with steroidal glucocorticoids.