Masofaniten, also known by its developmental code name EPI-7386, is an N-terminal domain antiandrogen, or antagonist of the N-terminal domain (NTD) of the androgen receptor (AR), which was under development for the treatment of prostate cancer. The development of masofaniten has been discontinuted.
Development history
The compound was developed as a successor of previous drugs in the EPI series such as EPI-001, ralaniten (EPI-002), and ralaniten acetate (EPI-506). Masofaniten showed a 20-fold improved potency than ralaniten in vitro ( = 535 nM vs. 9,580 nM, respectively), as well as greater stability in human hepatocytes.
It entered phase I clinical trials in 2020. Preliminary results of a phase I/II clinical trial were published in 2023. A combination of masofaniten and enzalutamide (ClinicalTrials.gov Identifier: NCT06312670) was tested in clinical trials for treatment-naïve metastatic hormone-sensitive prostate cancer and showed efficacy with an acceptable safety profile suggesting that further investigation was warranted.
The development of masofaniten was discontinued by ESSA Pharma Inc in 2024 .
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