galeterone

Galeterone is a first-in-class, multi-targeted small molecule developed for the treatment of metastatic castration-resistant prostate cancer (CRPC). It acts through three primary mechanisms of action: - Androgen receptor antagonist - CYP17 lyase inhibitor (while conserving CYP17 hydroxylase function) - Inducer of androgen receptor degradation via proteasomal pathways Galeterone disrupts androgen signaling by blocking the androgen receptor (AR), inhibiting androgen synthesis through CYP17 lyase inhibition, and promoting AR protein degradation—including both full-length AR and the AR-V7 splice variant—by enhancing ubiquitin-mediated proteasomal degradation. This multi-modal approach aims to overcome resistance mechanisms seen with other antiandrogens. The drug was developed as an oral therapy primarily for advanced prostate cancer but has not received FDA approval[1][2][3][5][6].

Brand names

galeterone

Other names

galeteroneTOK-001TOK001TOK 001VN/124-1