MRT-2359 + apalutamide

MRT-2359 + apalutamide is an investigational combination therapy being evaluated for the treatment of patients with androgen receptor (AR) mutation-positive metastatic castration-resistant prostate cancer (mCRPC). MRT-2359 is an orally bioavailable, selective molecular glue degrader (MGD) of GSPT1 (G1 to S phase transition protein 1), a translation termination factor. By inducing the degradation of GSPT1 via the cereblon (CRBN) E3 ubiquitin ligase pathway, MRT-2359 disrupts the protein translation machinery, particularly affecting MYC-driven cancer cells that depend on high translation rates. Apalutamide is an FDA-approved, second-generation oral androgen receptor inhibitor that binds directly to the ligand-binding domain of the androgen receptor, preventing nuclear translocation and DNA binding. The combination of these two agents is designed to target both the androgen receptor pathway and the translational dependencies of MYC-driven prostate cancer cells, potentially overcoming resistance to standard hormone therapies. The combination is being developed by Monte Rosa Therapeutics and is currently in Phase 2 clinical development.

Other names

apalutamide + MRT-2359apalutamide and MRT-2359Erleada + MRT-2359MRT-2359 + apalutamideMRT-2359 + ErleadaMRT-2359 and apalutamideMRT2359 and apalutamideMRT 2359 and apalutamide