An Overview on 5α-Reductase Inhibitors

The document provided an overview of 5α-reductase inhibitors, which were developed to inhibit the enzyme converting testosterone to dihydrotestosterone (DHT). It discussed the challenges in designing these inhibitors due to the unknown crystal structure of the enzyme. Various azasteroids, particularly 4-azasteroids, were extensively studied and used clinically, while non-steroidal inhibitors like benzo[f]quinolinones and pyridones were developed to minimize interactions with other steroidal systems. Finasteride and Dutasteride were the only steroidal drugs in clinical use at the time, with Epristeride in clinical trials. The document also noted the success of combining 5α-reductase inhibitors with α-blockers in managing benign prostatic hyperplasia.