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Clinical data | |
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Routes of administration | By mouth |
Drug class | Nonsteroidal antiandrogen |
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Formula | C22H16F4N4O2S |
Molar mass | 476.45 g·mol−1 |
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RD-162 is asecond-generationnonsteroidal antiandrogen (NSAA) which was developed for the treatment ofprostate cancer but was never marketed.[1] It acts as apotent andselectivesilent antagonist of theandrogen receptor (AR).[1] The drug is a diarylthiohydantoinderivative.[1] It is closely related toenzalutamide andapalutamide.[1] Both RD-162 and enzalutamide show 5- to 8-fold higheraffinity for the AR than the first-generation NSAAbicalutamide, and only 2- to 3-fold lower affinity thandihydrotestosterone (DHT), the majorendogenousligand of the receptor in theprostate gland.[1]
RD-162 and enzalutamide were developed together and were derived from thenonsteroidal androgenRU-59063, which itself was derived from thefirst-generation NSAAnilutamide.[2] RD-162 and enzalutamide were selected as thelead compounds from a group of over 200 compounds that weresynthesized andassayed forantiandrogenic activity.[1] Enzalutamide was ultimately selected from the two for furtherclinical development and was eventually marketed.[1] RD-162 is also very closely related to apalutamide, with the two compounds differing only by the replacement of a single atom (acarbon atom in one of thephenyl rings of RD-162 swapped with anitrogen atom in apalutamide). Apalutamide was approved for the treatment of prostate cancer in 2018.[3]
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