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DRUG:

EPI-8207

i
Other names: EPI-8207, Androgen receptor (AR) N-Terminal Domain degrader, ANITAC degrader
Associations
Trials
Company:
ESSA Pharma
Drug class:
Androgen receptor degrader
Associations
Trials
almost3years
Androgen receptor (AR) N-terminal domain degraders can degrade AR full length and AR splice variants in CRPC preclinical models (AACR 2022)
However, we recently demonstrated that EPI-7386, an AR NTD small molecule inhibitor, inhibits AR activity by binding to Tau5 region of the NTD. In summary, we report preclinical data on the first generation of ANITAC molecules, that can be orally bioavailable and show activity against forms of AR expressed in late stage CRPC patients.
Preclinical
|
AR (Androgen receptor)
|
AR expression • AR splice variant 7
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masofaniten (EPI-7386) • EPI-8207