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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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    1. Androgen Receptor Antagonists (Antiandrogens) Structure-Activity Relationships Current Medicinal Chemistry · 2000 · 204 citations
    2. Design and synthesis of novel androgen receptor antagonists with sterically bulky icosahedral carboranes Bioorganic & medicinal chemistry · 2005 · 45 citations
    3. Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production Bioorganic & Medicinal Chemistry Letters · 2007 · 17 citations
    4. (1R,2S)-4-(2-Cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production Bioorganic & Medicinal Chemistry Letters · 2007 · 14 citations
    5. 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 Tetrahedron Letters · 1994 · 14 citations
    6. 4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production Bioorganic & Medicinal Chemistry Letters · 2009 · 11 citations
    7. Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production Bioorganic & Medicinal Chemistry Letters · 2007 · 11 citations
    8. Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production Bioorganic & Medicinal Chemistry Letters · 2009 · 7 citations
    9. Pantolactams as androgen receptor antagonists for the topical suppression of sebum production Bioorganic & Medicinal Chemistry Letters · 2011 · 5 citations
    10. Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists Bioorganic & medicinal chemistry letters · 2017 · 3 citations
    11. Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety for Androgenetic Alopecia Figshare · 2026
    12. Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety for Androgenetic Alopecia Figshare · 2026
    13. Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety for Androgenetic Alopecia Figshare · 2026
    14. Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety for Androgenetic Alopecia Figshare · 2026
    15. Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety for Androgenetic Alopecia Figshare · 2026
    16. Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety for Androgenetic Alopecia Figshare · 2026
    17. Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety for Androgenetic Alopecia Figshare · 2026
    18. Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety for Androgenetic Alopecia Figshare · 2026
    19. Novel DualSoftDrug Strategy Enables Developmentof Topical Androgen Receptor Antagonists with Enhanced Efficacy andOptimized Safety for Androgenetic Alopecia Figshare · 2026
    20. Novel Dual Soft Drug Strategy Enables Development of Topical Androgen Receptor Antagonists with Enhanced Efficacy and Optimized Safety for Androgenetic Alopecia Journal of Medicinal Chemistry · 2026
    21. Design, synthesis and anti-tumor evaluation of novel thiohydantoin congeners as androgen receptor antagonists with in vivo study. Journal of molecular structure · 2024
    22. Emerging and traditional 5-α reductase inhibitors and androgen receptor antagonists for male androgenetic alopecia Expert opinion on emerging drugs · 2024
    23. Androgen Biosynthesis Inhibitors and Androgen Receptor Antagonists Elsevier eBooks · 2004
    24. Discovery of (2<i>S</i>)-<i>N</i>-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-3-(6-(4-cyanophenyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)-2-hydroxy-2-methylpropanamide as a Highly Potent and Selective Topical Androgen Receptor Antagonist for Androgenetic Alopecia Treatment Journal of Medicinal Chemistry · 2023
    25. Treatment of female pattern hair loss with the androgen receptor antagonist flutamide Australasian Journal of Dermatology · 2011 · 30 citations
    26. Rational Design of a Topical Androgen Receptor Antagonist for the Suppression of Sebum Production with Properties Suitable for Follicular Delivery Journal of Medicinal Chemistry · 2010 · 11 citations
    27. Androgens and acne: perspectives on clascoterone, the first topical androgen receptor antagonist Expert opinion on pharmacotherapy · 2021 · 9 citations
    28. Cortexolone 17α-Propionate (Clascoterone) is an Androgen Receptor Antagonist in Dermal Papilla Cells In Vitro PubMed · 2019 · 4 citations
    29. Rational Design and Synthesis of 4-((1<i>R</i>,2<i>R</i>)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a Novel, Nonsteroidal Androgen Receptor Antagonist Devoid of Phototoxicity for Dermatological Indications Journal of medicinal chemistry · 2008 · 23 citations
    30. Androgen Receptor Ligands: Agonists and Antagonists Elsevier eBooks · 2017 · 2 citations