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Glossary5α-reductase inhibitors

block enzyme converting testosterone to hair-loss-causing DHT

5α-reductase inhibitors, also known as 5-ARIs, are medications that block the enzyme 5α-reductase. This enzyme converts testosterone into dihydrotestosterone (DHT), a hormone that can contribute to conditions like male pattern baldness and benign prostatic hyperplasia (BPH). By inhibiting this enzyme, 5-ARIs can help reduce hair loss and shrink an enlarged prostate.

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research DIHYDROTESTOSTERONE AND THE PROSTATE: THE SCIENTIFIC RATIONALE FOR 5α-REDUCTASE INHIBITORS IN THE TREATMENT OF BENIGN PROSTATIC HYPERPLASIA

235 citations , September 2004 in “The Journal of urology/The journal of urology”

Drugs that block DHT production can effectively treat enlarged prostate and improve urinary issues with some sexual side effects.

research The Risks and Benefits of 5α-Reductase Inhibitors for Prostate-Cancer Prevention

147 citations , June 2011 in “New England journal of medicine/The New England journal of medicine”

5α-reductase inhibitors may prevent prostate cancer but could also raise the risk of more severe cancers.

Effect of Testosterone Supplementation With and Without a Dual 5α-Reductase Inhibitor on Fat-Free Mass in Men With Suppressed Testosterone Production

research Effect of Testosterone Supplementation With and Without a Dual 5α-Reductase Inhibitor on Fat-Free Mass in Men With Suppressed Testosterone Production

124 citations , March 2012 in “JAMA”

Testosterone's muscle-building effects do not require its conversion to DHT.

research Association of Suicidality and Depression With 5α-Reductase Inhibitors

90 citations , March 2017 in “JAMA Internal Medicine”

Men over 66 taking medication for prostate enlargement have a higher risk of depression and self-harm, especially in the first 18 months of treatment.

research Effect of 5α-Reductase Inhibitors on Sexual Function: A Meta-Analysis and Systematic Review of Randomized Controlled Trials

57 citations , July 2016 in “The Journal of Sexual Medicine”

5α-reductase inhibitors increase the risk of sexual dysfunction, especially in men with enlarged prostate.

The Aromatase Inhibitor Fadrozole and the 5-Reductase Inhibitor Finasteride Affect Gonadal Differentiation and Gene Expression in the Frog Silurana Tropicalis

research The Aromatase Inhibitor Fadrozole and the 5-Reductase Inhibitor Finasteride Affect Gonadal Differentiation and Gene Expression in the Frog Silurana tropicalis

37 citations , January 2009 in “Sexual Development”

Fadrozole and Finasteride change frog sex ratios and cause intersex animals with altered gene expressions.

Long-Term Oral Administration of 5α-Reductase Inhibitor Attenuates Erectile Function by Inhibiting Autophagy and Promoting Apoptosis of Smooth Muscle Cells in Corpus Cavernosum of Aged Rats

research Long-term Oral Administration of 5α-reductase Inhibitor Attenuates Erectile Function by Inhibiting Autophagy and Promoting Apoptosis of Smooth Muscle Cells in Corpus Cavernosum of Aged Rats

34 citations , September 2013 in “Urology”

Long-term use of a certain medication can worsen erectile function in aged rats by damaging penile muscle cells.

Curcuma Aeruginosa, A Novel Botanically Derived 5α-Reductase Inhibitor In The Treatment Of Male-Pattern Baldness: A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study

research Curcuma aeruginosa, a novel botanically derived 5α-reductase inhibitor in the treatment of male-pattern baldness: a multicenter, randomized, double-blind, placebo-controlled study

34 citations , July 2011 in “Journal of Dermatological Treatment”

Curcuma aeruginosa extract combined with minoxidil effectively treats male-pattern baldness.

research The Effect of 5 -Reductase Inhibitors on Erectile Function

31 citations , September 2008 in “International Journal of Andrology”

5-alpha-reductase inhibitors may cause a low incidence of erectile dysfunction that decreases over time.

research 12 Treatment of hirsutism with 5α-reductase inhibitors

28 citations , May 1986 in “Clinics in endocrinology and metabolism”

New compounds may soon be tested to treat excessive hair growth in women.

New Progesterone Esters as 5α-Reductase Inhibitors

research New Progesterone Esters as 5.ALPHA.-Reductase Inhibitors.

22 citations , January 2001 in “Chemical & Pharmaceutical Bulletin”

Some new progesterone derivatives are better at blocking testosterone conversion than a common drug.

research Novel 5α-Reductase Inhibitors: Synthesis, Structure−Activity Studies, and Pharmacokinetic Profile of Phenoxybenzoylphenyl Acetic Acids

18 citations , December 2005 in “Journal of Medicinal Chemistry”

A brominated phenoxy compound effectively inhibits a human enzyme and shows potential for clinical use.

research Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: A legitimate approach

17 citations , June 2012 in “European journal of medicinal chemistry”

New steroid compounds effectively inhibit 5α-reductase and may treat hair loss.

research Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors

17 citations , December 2015 in “Bioorganic & Medicinal Chemistry”

3-tetrazolo steroidal analogs can strongly inhibit the enzyme linked to hair loss.

research Novel C-6 substituted and unsubstituted pregnane derivatives as 5α-reductase inhibitors and their effect on hamster flank organs diameter size

15 citations , May 2009 in “Steroids”

Certain compounds reduced hamster flank organ size by inhibiting 5α-reductase, like finasteride, without affecting androgen receptors.

research New ester derivatives of dehydroepiandrosterone as 5α-reductase inhibitors

14 citations , June 2011 in “Steroids”

New compounds may help treat prostate issues without affecting androgen receptors.

research Synthesis, Biological Evaluation and Molecular Docking of Avicequinone C Analogues as Potential Steroid 5α-Reductase Inhibitors

13 citations , January 2017 in “Chemical & Pharmaceutical Bulletin”

Certain compounds, especially those with a propionic substituent, could potentially be new treatments for hair loss and similar disorders.

research Inhibitors of 5α-reductase-related side effects in patients seeking medical care for sexual dysfunction.

13 citations , November 2012 in “PubMed”

5α-reductase inhibitors may worsen sexual drive and spontaneous erections but don't worsen existing erectile or ejaculatory problems.

research 3,3-Diphenylpentane skeleton as a steroid skeleton substitute: Novel inhibitors of human 5α-reductase 1

13 citations , August 2007 in “Bioorganic & medicinal chemistry letters”

A new compound effectively inhibits human 5α-reductase 1.

Synthesis and In Vitro Evaluation of 4-Substituted N-(1,1-Dimethylethyl)-3-Oxo-4-Androstene-17β-Carboxamides as 5α-Reductase Inhibitors and Antiandrogens

research Synthesis and in Vitro Evaluation of 4-Substituted N-(1,1-Dimethylethyl)-3-oxo-4-androstene-17.beta.-carboxamides as 5.alpha.-Reductase Inhibitors and Antiandrogens

12 citations , April 1995 in “Journal of Medicinal Chemistry”

The new compounds moderately block a specific enzyme and strongly counteract a male hormone, suggesting potential for treating certain male-related health conditions.

research COMBINATION OF AN ANTIANDROGEN AND A 5α-REDUCTASE INHIBITOR: A FURTHER STEP TOWARDS TOTAL ANDROGEN BLOCKADE?

9 citations , March 1991 in “Endocrinology”

Using two drugs together, Flutamide and 4-MA, is more effective for blocking male hormones than using each one alone.

Synthesis and Biological Evaluation of 4-(4-(Alkyl- and Phenylaminocarbonyl)benzoyl)benzoic Acid Derivatives as Non-Steroidal Inhibitors of Steroid 5α-Reductase Isozymes 1 and 2

research Synthesis and Biological Evaluation of 4-(4-(Alkyl-and Phenylaminocarbonyl)benzoyl)benzoic Acid Derivatives as Non-steroidal Inhibitors of Steroid 5α-Reductase Isozymes 1 and 2

8 citations , March 2002 in “Archiv Der Pharmazie”

The compound 4c effectively inhibits the enzyme linked to hair loss.

Risk of Erectile Dysfunction Associated with Use of 5α-Reductase Inhibitors for Benign Prostatic Hyperplasia or Alopecia: Population-Based Studies Using the Clinical Practice Research Datalink

research Re: Risk of Erectile Dysfunction Associated with Use of 5α-Reductase Inhibitors for Benign Prostatic Hyperplasia or Alopecia: Population Based Studies Using the Clinical Practice Research Datalink

2 citations , April 2017 in “European Urology”

Using finasteride for hair loss or prostate issues does not significantly raise the risk of erectile dysfunction.

Association Between 5α-Reductase Inhibitors and Prostate Cancer Mortality

research Antioxidant and 5α-Reductase Inhibitory Activity of Momordica charantia Extract, and Development and Characterization of Microemulsion

1 citations , April 2022 in “Applied sciences”

Bitter melon extract may help prevent hair loss and can be used in cosmetic products.

research Re: Association of Suicidality and Depression with 5α-Reductase Inhibitors

1 citations , August 2017 in “The Journal of urology/The journal of urology”

5α-reductase inhibitors may increase the risk of depression and suicidal thoughts.

Computational Drug Discovery of Potential 5α-Reductase Phytochemical Inhibitors and Hair Growth Promotion Using In Silico Techniques

research Computational drug discovery of potential 5α-reductase phytochemical inhibitors and hair growth promotion using in silico techniques

May 2025 in “Frontiers in Bioinformatics”

Jamogenin from plants may help hair growth and is a potential alternative to finasteride.

research The relevance of using 5α-reductase inhibitors in the conservative management of benign prostatic hyperplasia: A review

September 2025 in “Consilium Medicum”

5α-reductase inhibitors help manage symptoms of benign prostatic hyperplasia and may also prevent prostate cancer and treat hair loss.