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rinzimetostat + darolutamide

Development stage: Phase 3
Lead developer: ORIC Pharmaceuticals
Modality: Small Molecules
Administration: Oral

Overview

Rinzimetostat plus darolutamide is an investigational combination therapy being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). The combination consists of rinzimetostat (ORIC-944), an orally bioavailable, potent, and selective allosteric inhibitor of the polycomb repressive complex 2 (PRC2) that acts via the embryonic ectoderm development (EED) subunit, and darolutamide (Nubeqa), an androgen receptor (AR) antagonist. By combining PRC2 inhibition with AR pathway inhibition, the regimen aims to overcome lineage plasticity and tumor cell adaptation, thereby restoring sensitivity to androgen receptor pathway inhibitors (ARPIs) and delaying resistance. The combination is currently being evaluated in the global Phase 3 Himalayas-1 registrational trial (NCT07723248) in patients with mCRPC who have previously progressed on abiraterone acetate.

Other names: Nubeqa + rinzimetostatODM-201 + ORIC-944ORIC-944 + ODM-201ORIC-944 + darolutamideORIC-944 + NubeqaORIC-944 and darolutamideORIC944 and darolutamideORIC 944 and darolutamideORIC-944 plus darolutamideORIC944 plus darolutamideORIC 944 plus darolutamidedarolutamide + ORIC-944darolutamide + rinzimetostatdarolutamide and rinzimetostatdarolutamide plus rinzimetostatrinzimetostat + Nubeqarinzimetostat and darolutamiderinzimetostat plus darolutamide

Targets

AR (Adrenergic receptors)EED (Embryonic ectoderm development protein)EZH1EZH2 (Histone-lysine N-methyltransferase EZH2)SUZ12 (Polycomb protein SUZ12)

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