Pharmacokinetics of the Selective Glucocorticoid Receptor Modulator Miricorilant in Healthy Volunteers and Patients with Presumed Metabolic Dysfunction-Associated Steatohepatitis (MASH)

Summary & Conclusions 

  • The presented studies characterize the PK/ADME of miricorilant Administration of [14C]-miricorilant to mice resulted in high concentrations of radioactivity in the liver 
    • The primary route of miricorilant elimination is hepatic 
    • Miricorilant systemic concentrations increased with repeated daily dosing, with accumulation ratios of 1.42 for Cmax and 1.92 for AUC(0-24) and steady state exposures achieved by Day 7 
    • Miricorilant is a strong inhibitor of CYP2C8 in vivo 
    • Miricorilant is a moderate inhibitor of BCRP in vivo 
    • Miricorilant does not affect the activity of UGT1A1, CYP3A4, or CYP2C9 in vivo 
    • Miricorilant is a moderately sensitive substrate of CYP2C19 in vivo 
    • In patients with presumed MASH, miricorilant plasma PK behaved in an approximately dose proportional manner 
    • Miricorilant was well tolerated in patients and healthy volunteers 
    • A phase 2b study (MONARCH, NCT06108219) of miricorilant in patients with MASH is currently enrolling 

AUC(0-24), area under the curve from time 0 to 24 hours; 14C, carbon-14; ADME, absorption, distribution, metabolism, and excretion; BCRP, breast cancer resistance protein; Cmax, maximum measured concentration; CYP, cytochrome P450; MASH, metabolic dysfunction-associated steatohepatitis; PK, pharmacokinetics; UGT1A1, UDP-glucuronyltransferase 1A1. 


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