OPK-88004 explained
OPK-88004 (formerly known as LY-2452473 or TT-701) is a non-steroidal indole derivative which acts as a selective androgen receptor modulator (SARM). It has been investigated by OPKO Health for the treatment of erectile dysfunction and symptoms associated with benign prostate hyperplasia.[1] [2] [3]
Research
The compound advanced to a phase II trial in benign prostatic hyperplasia, but it was terminated due to difficulty in measuring prostate size, the trial's primary endpoint.[4]
It was also tried in a study to improve quality of life in patients with prostate cancer. Although it did not cause progression of the disease and increased lean body mass, the drug did not improve sexual function.[3]
See also
Notes and References
- Yi P, Rehmel JF, Cassidy K, Hadden C, Campanale K, Patel N, Johnson J . Disposition and metabolism of LY2452473, a selective androgen receptor modulator, in humans . Drug Metabolism and Disposition . 40 . 12 . 2354–2364 . December 2012 . 22961682 . 10.1124/dmd.112.047613 . 6942291 .
- Noey EL, Yang Z, Li Y, Yu H, Richey RN, Merritt JM, Kjell DP, Houk KN . 6 . Origins of Regioselectivity in the Fischer Indole Synthesis of a Selective Androgen Receptor Modulator . The Journal of Organic Chemistry . 82 . 11 . 5904–5909 . June 2017 . 28467062 . 10.1021/acs.joc.7b00878 .
- Pencina KM, Burnett AL, Storer TW, Guo W, Li Z, Kibel AS, Huang G, Blouin M, Berry DL, Basaria S, Bhasin S . 6 . A Selective Androgen Receptor Modulator (OPK-88004) in Prostate Cancer Survivors: A Randomized Trial . The Journal of Clinical Endocrinology and Metabolism . 106 . 8 . 2171–2186 . July 2021 . 34019661 . 10.1210/clinem/dgab361 . 8277210 .
- Christiansen AR, Lipshultz LI, Hotaling JM, Pastuszak AW . Selective androgen receptor modulators: the future of androgen therapy? . Translational Andrology and Urology . 9 . Suppl 2 . S135–S148 . March 2020 . 32257854 . 7108998 . 10.21037/tau.2019.11.02 . free .
