MK-386

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MK-386

MK-386 is a 5α-reductase inhibitor that was under development by Merck & Co. for the treatment of androgenic alopecia (male-pattern baldness) and benign prostatic hyperplasia (BPH). It is a selective inhibitor of the 5α-reductase type I isoform of the enzyme, and was the first such inhibitor to be developed. However, it was not marketed due to the discovery of more effective treatments.

History

Merck & Co. began the development of MK-386 in the 1990s as a potential treatment for androgenic alopecia and benign prostatic hyperplasia. The drug was designed to inhibit the 5α-reductase type I isoform of the enzyme, which is primarily found in the skin and scalp. This was a novel approach, as previous treatments had focused on inhibiting the 5α-reductase type II isoform, which is found in the prostate.

Mechanism of Action

MK-386 works by inhibiting the 5α-reductase type I isoform of the enzyme. This enzyme is responsible for converting testosterone into dihydrotestosterone (DHT), a more potent androgen. By inhibiting this conversion, MK-386 reduces the levels of DHT in the body, which can help to slow or stop the progression of conditions like androgenic alopecia and benign prostatic hyperplasia.

Clinical Trials

Several clinical trials were conducted to assess the efficacy and safety of MK-386. These trials found that the drug was effective at reducing levels of DHT in the body, and that it was generally well-tolerated by patients. However, the trials also found that MK-386 was less effective than other treatments at slowing the progression of androgenic alopecia and benign prostatic hyperplasia.

Conclusion

Despite the initial promise of MK-386, the drug was never marketed. This was due to the discovery of more effective treatments, such as finasteride and dutasteride, which inhibit both the type I and type II isoforms of the 5α-reductase enzyme. However, the development of MK-386 represented a significant step forward in our understanding of the role of the 5α-reductase type I isoform in conditions like androgenic alopecia and benign prostatic hyperplasia.