Drug intelligence / Profile preview

relacorilant + itraconazole

Development stage
Unknown
Lead developer
Corcept Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

**relacorilant + itraconazole** is an investigational combination of two small molecule drugs: relacorilant, a highly selective glucocorticoid receptor modulator (SGRM), and itraconazole, a triazole antifungal agent. Relacorilant acts by antagonizing the glucocorticoid receptor, reducing the effects of excess cortisol without significant activity at the progesterone receptor[2][3][4][6]. Itraconazole is primarily a potent inhibitor of fungal lanosterol 14α-demethylase (CYP51A1), but in this combination, its role is chiefly as a strong CYP3A4 inhibitor to alter the pharmacokinetics of relacorilant[5]. This combination has been studied mainly in pharmacokinetic and hepatic safety studies, demonstrating that co-administration of itraconazole does not notably alter the adverse event profile of relacorilant or cause clinically significant increases in liver enzymes in healthy volunteers or special populations[1][3][5].

02

Targets

GR (Glucocorticoid receptor)CYP3A4 (Cytochrome P450 3A4)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)

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