About Galeterone

Tokai’s lead product candidate is galeterone, an oral small molecule that utilizes the mechanistic pathways of current second-generation hormonal therapies, including abiraterone and enzalutamide, while also introducing a unique third mechanism – androgen receptor degradation – that impairs the function of androgen receptors, decreasing their sensitivity to androgen activity and reducing tumor growth. Tokai is developing galeterone for the treatment of patients with metastatic castration-resistant prostate cancer. Enrollment in the ARMOR2 and ARMOR3-SV clinical trials of galeterone has been closed. Assessment of future plans for galeterone are underway at this time.

Galeterone has been studied in over 250 subjects in Phase 1 and Phase 2 clinical trials, including in CRPC patients with and without the AR-V7 splice variant. In these trials, galeterone demonstrated good tolerability and showed clinically meaningful reductions in levels of prostate specific antigen, or PSA, a biochemical marker used to evaluate prostate cancer patients for signs of response to therapy.

We have worldwide development and commercialization rights to galeterone.

Androgen receptor degradation, which reduces the amount of androgen receptor protein in the tumor cells.

Androgen receptor antagonism, which blocks the binding of testosterone or DHT with the androgen receptor.

Inhibition of the enzyme CYP17, which blocks the synthesis of testosterone.