<unk>  is the first inhibitor of the androgen receptor amino-terminal domain. The single stereoisomer of<unk> ,<unk> , is a first-in-class drug that the USAN council assigned a new stem class "-aniten" and the generic name "ralaniten". This distinguishes the anitens novel molecular mechanism from anti androgens that bind the C-terminus ligand-binding domain and have the stem class "lutamide" (such as flutamide, nilutamide, bicalutamide, enzalutamide, etc.).<unk>  and its stereoisomers and analogues were discovered by Dr. Marianne Sadar and Dr. Raymond Andersen who co-founded the pharmaceutical company ESSA Pharma Inc (Vancouver, Canada) for the clinical development of anitens for the treatment of castration-resistant prostate cancer (CRPC).<unk>  is an antagonist of the androgen receptor (AR) that acts by binding covalently to the N-terminal domain (NTD) of the AR and blocking protein-protein interactions required for transcriptional activity of the AR and its splice variants (IC50 for inhibition of AR NTD transactivation ≈ 6 μM). This is different from all currently-used antiandrogens, which, conversely, bind to the C-terminal ligand-binding domain (LBD) of the AR and competitively block binding and activation of the receptor by androgens. Due to its unique mechanism of action,<unk>  type compounds may prove to be effective in the treatment of advanced prostate cancer resistant to conventional antiandrogens such as enzalutamide.<unk> 's successor, ralaniten acetate <unk> -506), a prodrug of ralaniten <unk> , one of the four stereoisomers of<unk> , was under clinical investigation in a phase I study.<unk> -506 was the first drug that directly binds to an intrinsically disordered region to be tested in humans and marks a leap in drug development from folded drug targets.
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