Target intelligence / Profile preview

5α-Reductase enzyme (5α-Reductase)

Target
5α-Reductase
Molecular classification
Enzyme, Oxidoreductase (EC 1.3.1), Steroidogenic enzyme
01

Overview

The 5α-reductase enzyme is a family of enzymes responsible for catalyzing the irreversible reduction of testosterone into dihydrotestosterone (DHT), a more potent androgen that plays a critical role in male sexual differentiation and development as well as in several androgen-dependent conditions. There are three known isoforms—type 1, type 2, and type 3—encoded by SRD5A genes. The enzyme is expressed in various tissues including reproductive organs, skin, liver, and nervous system. Inhibition or deficiency of this enzyme leads to significant clinical consequences related to androgen action such as ambiguous genitalia or reduced secondary male characteristics at birth.

Other names
3-oxo-5α-steroid 4-dehydrogenaseSteroid 5α-reductaseSRD5A (refers to gene family)Five alpha reductaseTestosterone reductase (less common)
02

Mechanism of action

Finasteride and dutasteride are competitive inhibitors of the 5α-reductase enzyme, blocking the conversion of testosterone to DHT, thereby reducing DHT levels in tissues.

03

Biological functions

Steroid metabolismConversion of testosterone to dihydrotestosterone (DHT)Regulation of androgen and estrogen activity
04

Disease associations

Benign prostatic hyperplasiaAndrogenic alopecia (male pattern baldness)Acne vulgarisHirsutismPolycystic ovarian syndrome
05

Safety considerations

Sexual dysfunctionDecreased libidoErectile dysfunctionGynecomastiaPossible mood changesOngoing debate about long-term effects on prostate cancer risk
06

Interacting drugs

Finasteride

1 more in the full profile.

07

Biomarkers

There are no widely used direct biomarkers for patient selection specific to this enzymeSerum DHT levels can be monitored as a pharmacodynamic marker during therapy

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