LEO 134310 (LP 0155) is a non-steroidal, potent and selective glucocorticoid receptor (GR) agonist (EC50=2 nM, hPBMC).
LEO 134310 is rapidly deactivated in the blood resulting in low systemic exposure and a higher therapeutic index in the TPA-induced skin inflammation mouse model compared with betamethasone valerate (BMV) and clobetasol propionate (CP).
LEO 134310 displays high selectivity for GR in a panel of nuclear receptors, including the mineralocorticoid receptor (MR).
LEO 134310 exhibits full efficacy on GR transactivation and transrepression.
LEO 134310 may be suitable for long-term topical treatment of inflammatory skin diseases.
