RD162

RD162

RD162 is a nonsteroidal antiandrogen (NSAA) that was never marketed. It is a selective antagonist of the androgen receptor (AR) and was developed by the pharmaceutical company Roussel Uclaf for the potential treatment of prostate cancer. RD162 is closely related to enzalutamide (MDV3100), which was also developed by Roussel Uclaf and is now marketed for the treatment of prostate cancer.

Pharmacology

RD162, like enzalutamide, works by binding to the androgen receptor and preventing its activation and subsequent upregulation of androgen-responsive genes by androgens like testosterone and dihydrotestosterone (DHT). It has been found to possess greater affinity for the androgen receptor and to be a stronger antagonist of the receptor than the earlier NSAA bicalutamide.

Chemistry

RD162 is a anilide and a tetrahydroquinoline. It is structurally very similar to enzalutamide, with the difference between the two drugs being that RD162 has a 2-cyanoethyl group at the 5-position of its tetrahydroquinoline ring whereas enzalutamide has a 2-fluoroethyl group at this position.

History

RD162 was developed by the French pharmaceutical company Roussel Uclaf in the 2000s. It was not further developed beyond preclinical studies, but its development led to the discovery and development of enzalutamide, which was approved for the treatment of prostate cancer in 2012.

See also

• List of investigational hormonal agents