Target intelligence / Profile preview

Steroid 5-alpha-reductase (SRD5A) (5α-reductase)

Target
5α-reductase
Molecular classification
Enzyme, Oxidoreductase, Membrane-bound protein
01

Overview

Steroid 5-alpha-reductase (5α-reductase) is a membrane-bound enzyme that catalyzes the NADPH-dependent conversion of testosterone into the more potent androgen, dihydrotestosterone (DHT) (UniProt P18405, P31213). It exists in two major isoforms: Type 1 (SRD5A1), found primarily in the skin, liver, and sebaceous glands, and Type 2 (SRD5A2), which predominates in the prostate and hair follicles (StatPearls, 5-Alpha Reductase Inhibitors). This enzyme plays a critical role in male sexual development and the pathophysiology of androgen-dependent conditions. Excessive DHT production is a primary driver of benign prostatic hyperplasia (BPH) and androgenetic alopecia (male pattern baldness) (PubMed PMID: 15116006). Therapeutic strategies involve the use of 5-alpha-reductase inhibitors (5ARIs) like finasteride and dutasteride to lower systemic and local DHT levels. While effective, these drugs are associated with side effects such as sexual dysfunction and must be avoided during pregnancy due to risks of fetal genital malformation (NIH PubChem CID 5901).

Other names
3-oxo-5-alpha-steroid 4-dehydrogenaseSRD5A1SRD5A25-alpha-reductase5AR
02

Mechanism of action

Competitive inhibition of the 5-alpha-reductase enzyme isoforms, which blocks the conversion of testosterone to dihydrotestosterone (DHT), thereby reducing androgenic stimulation in target tissues (StatPearls).

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Biological functions

Steroid metabolismAndrogen signalingConversion of testosterone to dihydrotestosteroneBile acid synthesis
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Disease associations

Benign prostatic hyperplasiaAndrogenetic alopeciaHirsutismProstate cancerPolycystic ovary syndrome
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Safety considerations

Sexual dysfunction including decreased libido and erectile dysfunction (StatPearls)Potential for Post-Finasteride Syndrome involving persistent neurological and sexual symptoms (PubMed PMID: 32033719)Teratogenicity: exposure in pregnant women can cause ambiguous genitalia in male fetuses (FDA Label)Reduction in PSA levels, which may mask the detection of prostate cancer (PubMed PMID: 15116006)
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Interacting drugs

Finasteride

3 more in the full profile.

07

Biomarkers

Serum dihydrotestosterone (DHT) levels (StatPearls)Prostate-specific antigen (PSA) levels (PubMed PMID: 15116006)Scalp DHT concentrations

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