A mifepristone-based steroidal glucocorticoid receptor (GR) antagonist with potential antineoplastic activity. Upon oral administration, ORIC-101 selectively binds to GRs, thereby inhibiting the activation of GR-mediated proliferative and anti-apoptotic gene expression pathways. The GR, a member of the nuclear receptor superfamily of ligand-dependent transcription factors, is overexpressed in certain tumor types and may be associated with tumor cell proliferation and treatment resistance. Inhibition of GR activity may potentially slow tumor cell growth and disease progression in certain cancers. Due to its reduced androgen receptor (AR) agonistic activity and improved cytochrome P450 2C8 (CYP2C8) and 2C9 (CYP2C9) inhibition profile, ORIC-101 may be useful in the treatment of AR-positive tumors with reduced potential for drug-drug interactions.