Ralaniten acetate

Ralaniten acetate (also known as EPI-506) is an androgen receptor antagonist which is under development by ESSA Pharma for the treatment of prostate cancer. It is a prodrug of ralaniten (EPI-002).

Mechanism of action

Ralaniten acetate acts by binding to the N-terminal domain of the androgen receptor (AR). This is in contrast to other AR antagonists like bicalutamide and enzalutamide, which bind to the C-terminal ligand-binding domain of the AR. The N-terminal domain is where the AR is activated by coactivator proteins. By binding to this site, ralaniten acetate prevents the AR from being activated by these coactivators.

Clinical trials

Ralaniten acetate has been studied in a phase I/II clinical trial for prostate cancer. The results of this trial have not yet been published.

See also

• Androgen receptor antagonist
• Prostate cancer

References

Ralaniten acetate Resources
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