5α-Reductase inhibitor

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Incomplete map of testosterone metabolites

5α-Reductase (5-AR) is the enzyme in the cytosol of cells that converts Testosterone into Dihydrotestosterone (DHT), which is ~100x more potent. However, this isn't 5-AR's only job - it also metabolizes neurosteroids in the brain, and in general reduces (replaces Oxygen with Hydrogen) on the 5α position on any steroid.

5-AR exists in three isozymes, i.e. there are three different genes that produce the three different forms of the 5-AR enzyme: SRD5A1 (Type I), SRD5A2 (Type II) and SRD5A3 (Type III). Each of these enzymes behaves subtly differently, and not all drugs target all three isozymes equally.

Uses

Safety Concerns

  • 5-AR inhibition may cause a form of androgen deficiency. [1]

Inhibitors

Finasteride

Finasteride is the most common 5-AR inhibitor. Officially marketed for androgenic alopecia ("male-pattern baldness"), it's inexpensive, easy to obtain and generally trusted by clinicians.

Pros

  • Long track record of clinical use.

Cons