RD-162
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| Routes of administration | By mouth |
| Drug class | Nonsteroidal antiandrogen |
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| Chemical and physical data | |
| Formula | C22H16F4N4O2S |
| Molar mass | 476.45g·mol−1 |
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RD-162is asecond-generationnonsteroidal antiandrogen(NSAA) which was developed for the treatment ofprostate cancerbut was never marketed.[1]It acts as apotentandselectivesilent antagonistof theandrogen receptor(AR).[1]The drug is a diarylthiohydantoinderivative.[1]It is closely related toenzalutamideandapalutamide.[1]Both RD-162 and enzalutamide show 5- to 8-fold higheraffinityfor the AR than the first-generation NSAAbicalutamide,and only 2- to 3-fold lower affinity thandihydrotestosterone(DHT), the majorendogenousligandof 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-generationNSAAnilutamide.[2]RD-162 and enzalutamide were selected as thelead compoundsfrom a group of over 200 compounds that weresynthesizedandassayedforantiandrogenicactivity.[1]Enzalutamide was ultimately selected from the two for furtherclinical developmentand 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 (acarbonatom in one of thephenyl ringsof RD-162 swapped with anitrogenatom in apalutamide). Apalutamide was approved for the treatment of prostate cancer in 2018.[3]
References
[edit]- ^abcdefgTran C, Ouk S, Clegg NJ, Chen Y, Watson PA, Arora V, Wongvipat J, Smith-Jones PM, Yoo D, Kwon A, Wasielewska T, Welsbie D, Chen CD, Higano CS, Beer TM, Hung DT, Scher HI, Jung ME, Sawyers CL (2009)."Development of a second-generation antiandrogen for treatment of advanced prostate cancer".Science.324(5928): 787–90.Bibcode:2009Sci...324..787T.doi:10.1126/science.1168175.PMC2981508.PMID19359544.
- ^Liu B, Su L, Geng J, Liu J, Zhao G (2010). "Developments in nonsteroidal antiandrogens targeting the androgen receptor".ChemMedChem.5(10): 1651–61.doi:10.1002/cmdc.201000259.PMID20853390.S2CID23228778.
- ^"Apalutamide - Janssen Research and Development - AdisInsight".
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