A Review on Steroidal 5α-Reductase Inhibitors for Treatment of Benign Prostatic Hyperplasia
August 2011
in “
Current Medicinal Chemistry
”
TLDR New treatments for enlarged prostate are being developed, some of which may be more effective than current medications.
The document reviewed the effectiveness of steroidal 5α-reductase inhibitors, particularly finasteride and dutasteride, in treating benign prostatic hyperplasia (BPH). It detailed the role of the enzyme 5α-reductase in converting testosterone to dihydrotestosterone (DHT), a key factor in BPH development, and the significance of targeting the enzyme's two isozymes. The review highlighted dutasteride as a potent dual inhibitor, reducing DHT levels by over 90%, compared to finasteride's 65-80% reduction. It also discussed the importance of structural modifications, such as the C17-substituent, in enhancing inhibitory activity, with new compounds showing up to five times the potency of finasteride. The document concluded by mentioning the synthesis of new inhibitors, like compound 66, with comparable potency to finasteride, indicating ongoing efforts to improve treatment options for BPH.
