ralaniten

Ralaniten (EPI-002) is a potent, specific, and orally active antagonist of the androgen receptor N-terminal structural domain (AR-NTD).Ralaniten inhibits AR transcriptional activity with an IC50 value of 7.4 μM.Ralanites have anticancer activity and can be used to study desmoplasia-resistant prostate cancer (CRPC).

Ralaniten triacetate (EPI-506), a precursor of Ralaniten, is a first-of-its-kind, orally active androgen receptor N-terminal structural domain (AR-NTD) inhibitor with anticancer activity and can be used to study prostate and breast cancer.

EPI-7170 is a ralaniten analogue and a potent antagonist of the androgen receptor N-terminal structural domain, blocking the transcriptional activity of the full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 exhibits antitumor activity against enzalutamide resistant debulking resistant prostate cancer (CRPC).