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Glossary Androgen Receptor Antagonists

block male hormones like testosterone from affecting tissues

Androgen Receptor Antagonists, also known as antiandrogens, are medications that block the action of androgens, which are male sex hormones like testosterone. These drugs work by binding to androgen receptors, preventing androgens from exerting their effects on tissues, and are commonly used in the treatment of conditions like prostate cancer, androgenic alopecia (male-pattern baldness), and certain types of acne.

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Research

5 / 1000+ results

research Androgen Receptor Antagonists (Antiandrogens) Structure-Activity Relationships

204 citations , February 2000 in “Current Medicinal Chemistry”

This review discusses the use of antiandrogens like flutamide and its derivatives in prostate cancer treatment and highlights the need for next-generation antiandrogens for improved efficacy; it reports no new clinical results.

research Design and synthesis of novel androgen receptor antagonists with sterically bulky icosahedral carboranes

45 citations , August 2005 in “Bioorganic & medicinal chemistry”

This study found that novel androgen antagonists incorporating a carborane moiety showed anti-androgenic activity comparable to flutamide in a laboratory setting.

research Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production

17 citations , August 2007 in “Bioorganic & Medicinal Chemistry Letters”

This study found that a specific amino-pyridine compound showed potent androgen receptor antagonist activity, stimulating hair growth in mice and reducing sebum production in a hamster model.

research (1R,2S)-4-(2-Cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production

14 citations , August 2007 in “Bioorganic & Medicinal Chemistry Letters”

This study reported that the compound (1R, 2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile effectively stimulated hair growth in mice and reduced sebum production in hamsters.

research Highly efficient nucleophilic addition of alkyl Grignard reagents to 17-ketosteroids in the presence of cerium(III) chloride: Synthesis of 17α-propyl-17β-hydroxy-4-androsten-3-one, an androgen receptor antagonist

14 citations , February 1994 in “Tetrahedron Letters”

This study found that using anhydrous cerium(III) chloride with alkyl Grignard reagents significantly improved the addition to sterically hindered 17-ketosteroids, resulting in high yields and stereoselectivity.

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Community Join

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community Is there any role for topical DHT antagonists, or does a 5-AR inhibitor remove the need for them as therapy

2 upvotes 1 year ago

Topical androgen receptor antagonists may not be necessary if 5-AR inhibitors like finasteride or dutasteride effectively reduce DHT levels. Combining a 5-AR inhibitor with a topical androgen antagonist could potentially enhance treatment, but oral use of androgen antagonists is too risky due to severe side effects.

community Anyone know by what percentage Pyrilutamide or Ru decrease your androgens?

in Chat 1 upvotes 1 year ago

Pyrilutamide and RU58841 are androgen receptor antagonists that block receptors without significantly reducing testosterone or DHT levels. Any indirect effect on androgen levels is likely negligible.

community How is the GT20029 different to pyrilutamide as an androgenic antagonist

1 year ago

GT20029 and pyrilutamide are both androgen antagonists but work differently; GT20029 degrades the androgen receptor, while pyrilutamide blocks DHT from binding. GT20029 is expected to have similar efficacy to CosmeRNA.

community Is there a topical androgen receptor blocker so we don't have to fuck with the enzyme and destroy our allopregnanolone, but go and hit the end target straight?

in Treatment 44 upvotes 2 years ago

The conversation discusses topical androgen receptor blockers for hair loss, mentioning Clascoterone, Pyrilutamide, GT20029, and RU58841. Ketoconazole's effectiveness and application methods are also debated.

community Pyrilutamide ,the molecule’s true nature

in Research 302 upvotes 2 years ago

Pyrilutamide is a selective AR antagonist with a high binding affinity, making it effective in competing with DHT for androgen receptors. The 1% concentration is more effective than the 0.5%, but the latter may suffice for mild hair loss; the drug is considered a good option for those avoiding 5AR blockers due to side effects.

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Learn

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learn Clascoterone

Topical androgen-receptor blocker, approved as an acne cream

learn Spironolactone

Blood-pressure and diuretic drug with anti-androgen effects

How does spironolactone help reduce hair loss when used in topical or oral treatments? Spironolactone is thought to slow androgen-driven follicle miniaturisation by blocking androgen receptors; the trials are small, mostly in women and mostly alongside minoxidil. It is a prescription drug and its use for hair loss is off-label.

learn GT20029

Experimental topical drug designed to break down androgen receptors

learn Cyproterone

a synthetic anti-androgen and weak progestogen that inhibits DHT binding to androgen receptor

learn Fluridil

How is Fluridil different from other DHT blockers like finasteride? Fluridil is a topical androgen-receptor blocker applied to the scalp, while finasteride is an oral 5-alpha-reductase inhibitor that lowers DHT throughout the body. Finasteride is FDA-approved and far better studied; Fluridil rests on one 43-man trial and is not licensed as a hair-loss medicine, so its long-term safety and effect size are unknown.

learn Bicalutamide

Can bicalutamide stop DHT from shrinking your hair follicles? Bicalutamide blocks androgens at the receptor rather than lowering DHT, and some dermatologists prescribe it off-label for women with pattern hair loss, although its US label says it should not be used in women. The one randomised trial (74 women, 2025) found it added no benefit to oral minoxidil, and the drug needs liver monitoring because its label warns of severe and fatal liver injury; it is contraindicated in pregnancy.

learn Pyrilutamide

Experimental topical anti-androgen, also known as KX-826

What is pyrilutamide, and how does it help with androgenic alopecia or hair loss caused by DHT? Pyrilutamide (KX-826) is an investigational topical antiandrogen designed to block DHT at the androgen receptor in the scalp. Its sponsor reported that a 2023 China Phase III of a 0.5% tincture did not beat placebo and that a 2026 Phase III stage of a 1.0% tincture did; none of the data are peer-reviewed and it is not approved as a medicine anywhere.

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