Drug intelligence / Profile preview

MRT-2359 + enzalutamide

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

Overview

MRT-2359 + enzalutamide is a combination investigational therapy studied for its activity in patients with castration-resistant prostate cancer (CRPC). MRT-2359 is an orally bioavailable, potent, and selective molecular glue degrader that induces the degradation of the translation termination factor GSPT1 by promoting its interaction with the E3 ubiquitin ligase cereblon, leading to proteasomal degradation. This disrupts protein synthesis, especially in MYC-driven tumor cells, potentially inhibiting cancer cell proliferation. Enzalutamide is an androgen receptor inhibitor approved for the treatment of prostate cancer, acting by inhibiting androgen receptor signaling critical for prostate cancer cell survival and proliferation. The combination targets vulnerabilities in prostate cancer, particularly in the subset of patients who have progressed despite hormonal manipulation. This combination is currently being evaluated in Phase 1/2 clinical trials for non-neuroendocrine, castration-resistant prostate cancer.

Other names
enzalutamide
02

Targets

CRBN (Cereblon)GSPT1 (G1 to S phase transition 1)AR (Adrenergic receptors)

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