Editing Antiandrogen (section)

==Research==
{{See also|List of investigational sex-hormonal agents#Androgenics}}

===Topical administration===
There has been much interest and effort in the development of topical AR antagonists to treat androgen-dependent conditions like acne and pattern hair loss in males.<ref name="HelmsQuan2006">{{cite book| vauthors = Helms RA, Quan DJ |title=Textbook of Therapeutics: Drug and Disease Management|url=https://books.google.com/books?id=aVmRWrknaWgC&pg=PA211|year=2006|publisher=Lippincott Williams & Wilkins|isbn=978-0-7817-5734-8|pages=211–}}</ref> Unfortunately, whereas systemic administration of antiandrogens is very effective in treating these conditions, topical administration has disappointingly been found generally to possess limited and only modest effectiveness, even when high-[[affinity (pharmacology)|affinity]] steroidal AR antagonists like cyproterone acetate and spironolactone have been employed.<ref name="HelmsQuan2006" /> Moreover, in the specific case of acne treatment, topical AR antagonists have been found much less effective compared to established treatments like [[benzoyl peroxide]] and [[antibiotic]]s.<ref name="HelmsQuan2006" />

A variety of AR antagonists have been developed for topical use but have not completed development and hence have never been marketed. These include the steroidal AR antagonists [[cyproterone]], [[rosterolone]], and [[topterone]] and the nonsteroidal AR antagonists [[cioteronel]], [[inocoterone acetate]], [[RU-22930]], [[RU-58642]], and [[RU-58841]]. However, one topical AR antagonist, [[topilutamide]] (fluridil), has been introduced in a few European countries for the treatment of pattern hair loss in men.<ref name="TrüebLee2014" /> In addition, a topical 5α-reductase inhibitor and weak estrogen, [[alfatradiol]], has also been introduced in some European countries for the same indication, although its effectiveness is controversial.<ref name="TrüebLee2014" /> [[Spironolactone]] has been marketed in [[Italy]] in the form of a topical cream under the brand name Spiroderm for the treatment of acne and hirsutism, but this formulation was discontinued and hence is no longer available.<ref name="FARIDDiamanti-Kandarakis2009">{{cite book|vauthors=Farid NR, Diamanti-Kandarakis E|title=Diagnosis and Management of Polycystic Ovary Syndrome|url=https://books.google.com/books?id=fgMYVxmPDnMC&pg=PA235|date=27 February 2009|publisher=Springer Science & Business Media|isbn=978-0-387-09718-3|pages=235–|access-date=30 December 2016|archive-date=11 January 2023|archive-url=https://web.archive.org/web/20230111121904/https://books.google.com/books?id=fgMYVxmPDnMC&pg=PA235|url-status=live}}</ref>

Topical [[clascoterone]], brand name Winlevi, was approved to treat acne in males and females in the [[United States]] in 2020.<ref name="AdisInsight">{{cite web | title=Clascoterone - Cosmo Pharmaceuticals | website=AdisInsight | date=12 February 2025 | url=https://adisinsight.springer.com/drugs/800026561 | access-date=8 May 2025}}</ref><ref name="Dhillon2020">{{cite journal | vauthors = Dhillon S | title = Clascoterone: First Approval | journal = Drugs | volume = 80 | issue = 16 | pages = 1745–1750 | date = November 2020 | pmid = 33030710 | doi = 10.1007/s40265-020-01417-6 | url = }}</ref> However, although significantly more effective than [[placebo]], topical clascoterone, like previous topical antiandrogens that have been developed, showed modest effectiveness in treating acne in [[clinical trial]]s, and it appeared to be far less effective than [[systemic administration|systemic]] [[spironolactone]].<ref name="BasendwhAlharbiBukhamsin2024">{{cite journal | vauthors = Basendwh MA, Alharbi AA, Bukhamsin SA, Abdulwahab RA, Alaboud SA | title = The efficacy of Topical Clascoterone versus systematic spironolactone for treatment of acne vulgaris: A systematic review and network meta-analysis | journal = PLOS ONE | volume = 19 | issue = 5 | pages = e0298155 | date = 2024 | pmid = 38814916 | pmc = 11139337 | doi = 10.1371/journal.pone.0298155 | doi-access = free | bibcode = 2024PLoSO..1998155B | url = }}</ref>

===Male contraception===
Antiandrogens, such as cyproterone acetate, have been studied for potential use as [[male hormonal contraceptive]]s.<ref name="pmid793446">{{cite journal | vauthors = Neumann F, Diallo FA, Hasan SH, Schenck B, Traore I | title = The influence of pharmaceutical compounds on male fertility | journal = Andrologia | volume = 8 | issue = 3 | pages = 203–35 | date = 1976 | pmid = 793446 | doi = 10.1111/j.1439-0272.1976.tb02137.x| s2cid = 24859886 | doi-access = free }}</ref><ref name="pmid797248">{{cite journal | vauthors = Prasad MR, Rajalakshmi M | title = Target sites for suppressing fertility in the male | journal = Adv Sex Horm Res | volume = 2 | pages = 263–87 | date = 1976 | pmid = 797248 }}</ref><ref name="pmid206192">{{cite journal | vauthors = Ewing LL, Robaire B | title = Endogenous antispermatogenic agents: prospects for male contraception | journal = Annu. Rev. Pharmacol. Toxicol. | volume = 18 | pages = 167–87 | date = 1978 | pmid = 206192 | doi = 10.1146/annurev.pa.18.040178.001123 }}</ref><ref name="pmid6354690">{{cite journal | vauthors = Gombe S | title = A review of the current status in male contraceptive studies | journal = East Afr Med J | volume = 60 | issue = 4 | pages = 203–11 | date = April 1983 | pmid = 6354690 }}</ref><ref name="pmid6205409"/><ref name="pmid2687939">{{cite book | vauthors = Srivastava RP, Bhaduri AP | title = Progress in Drug Research | chapter = Emerging concepts towards the development of contraceptive agents | series = Progress in Drug Research. Fortschritte der Arzneimittelforschung. Progres des Recherches Pharmaceutiques | volume = 33 | pages = 267–315 | date = 1989 | pmid = 2687939 | doi = 10.1007/978-3-0348-9146-2_9| isbn = 978-3-0348-9925-3 |editor=Ernst Jucker |publisher=Birkhäuser }}</ref><ref name="pmid3075164">{{cite journal | vauthors = Wu FC | title = Male contraception: current status and future prospects | journal = Clin. Endocrinol. (Oxf) | volume = 29 | issue = 4 | pages = 443–65 | date = October 1988 | pmid = 3075164 | doi = 10.1111/j.1365-2265.1988.tb02894.x| s2cid = 36608203 }}</ref><ref name="pmid14667989">{{cite journal | vauthors = Nieschlag E, Zitzmann M, Kamischke A | title = Use of progestins in male contraception | journal = Steroids | volume = 68 | issue = 10–13 | pages = 965–72 | date = November 2003 | pmid = 14667989 | doi = 10.1016/s0039-128x(03)00135-1| s2cid = 22458746 }}</ref> While effective in suppressing [[male fertility]], their use as monotherapies is precluded by side effects, such as [[hypoandrogenism|androgen deficiency]] (e.g., [[demasculinization]], [[sexual dysfunction]], [[hot flash]]es, [[osteoporosis]]) and [[feminization (biology)|feminization]] (e.g., [[gynecomastia]]).<ref name="pmid6205409" /><ref name="pmid2687939" /><ref name="pmid3075164" /><ref name="pmid20933120">{{cite journal | vauthors = Nieschlag E | title = Clinical trials in male hormonal contraception | journal = Contraception | volume = 82 | issue = 5 | pages = 457–70 | year = 2010 | pmid = 20933120 | doi = 10.1016/j.contraception.2010.03.020 | url = http://www.kup.at/kup/pdf/10172.pdf | access-date = 2019-07-08 | archive-date = 2020-12-05 | archive-url = https://web.archive.org/web/20201205082822/https://www.kup.at/kup/pdf/10172.pdf | url-status = live }}</ref> The combination of a primary antigonadotropin such as cyproterone acetate to prevent fertility and an androgen like testosterone to prevent systemic androgen deficiency, resulting in a selective antiandrogenic action locally in the testes, has been extensively studied and has shown promising results, but has not been approved for clinical use at this time.<ref name="pmid3075164" /><ref name="pmid14667989" /><ref name="pmid16313066">{{cite journal | vauthors = Rajalakshmi M | title = Male contraception: expanding reproductive choice | journal = Indian J. Exp. Biol. | volume = 43 | issue = 11 | pages = 1032–41 | date = November 2005 | pmid = 16313066 }}</ref><ref name="pmid27016468">{{cite journal | vauthors = Chao JH, Page ST | title = The current state of male hormonal contraception | journal = Pharmacol. Ther. | volume = 163 | pages = 109–17 | date = July 2016 | pmid = 27016468 | doi = 10.1016/j.pharmthera.2016.03.012 }}</ref><ref name="pmid20933120" /> [[Dimethandrolone undecanoate]] (developmental code name CDB-4521), an [[oral administration|orally active]] dual AAS and progestogen, is under investigation as a potential male contraceptive and as the first male [[birth control pill]].<ref name="pmid16497801">{{cite journal | vauthors = Attardi BJ, Hild SA, Reel JR | title = Dimethandrolone undecanoate: a new potent orally active androgen with progestational activity | journal = Endocrinology | volume = 147 | issue = 6 | pages = 3016–26 | date = June 2006 | pmid = 16497801 | doi = 10.1210/en.2005-1524 | doi-access = free }}</ref><ref name="pmid27907978">{{cite journal | vauthors = Ayoub R, Page ST, Swerdloff RS, Liu PY, Amory JK, Leung A, Hull L, Blithe D, Christy A, Chao JH, Bremner WJ, Wang C | title = Comparison of the single dose pharmacokinetics, pharmacodynamics, and safety of two novel oral formulations of dimethandrolone undecanoate (DMAU): a potential oral, male contraceptive | journal = Andrology | volume = 5 | issue = 2 | pages = 278–285 | date = March 2017 | pmid = 27907978 | pmc = 5352517 | doi = 10.1111/andr.12303 }}</ref>

===Breast cancer===
Antiandrogens such as [[bicalutamide]], [[enzalutamide]], and [[abiraterone acetate]] are under investigation for the potential treatment of [[breast cancer]], including AR-expressing [[triple-negative breast cancer]] and other types of AR-expressing breast cancer.<ref name="pmid24740738">{{cite journal | vauthors = Fioretti FM, Sita-Lumsden A, Bevan CL, Brooke GN | title = Revising the role of the androgen receptor in breast cancer | journal = J. Mol. Endocrinol. | volume = 52 | issue = 3 | pages = R257–65 | date = June 2014 | pmid = 24740738 | doi = 10.1530/JME-14-0030 | doi-access = free }}</ref><ref name="pmid27816190">{{cite journal | vauthors = Gucalp A, Traina TA | title = Targeting the androgen receptor in triple-negative breast cancer | journal = Curr Probl Cancer | volume = 40 | issue = 2–4 | pages = 141–150 | date = 2016 | pmid = 27816190 | pmc = 5580391 | doi = 10.1016/j.currproblcancer.2016.09.004 }}</ref><ref name="pmid24888812">{{cite journal | vauthors = Arce-Salinas C, Riesco-Martinez MC, Hanna W, Bedard P, Warner E | title = Complete Response of Metastatic Androgen Receptor-Positive Breast Cancer to Bicalutamide: Case Report and Review of the Literature | journal = J. Clin. Oncol. | volume = 34 | issue = 4 | pages = e21–4 | date = February 2016 | pmid = 24888812 | doi = 10.1200/JCO.2013.49.8899 }}</ref><ref name="pmid28216075">{{cite journal | vauthors = Héquet D, Mzoughi S, Rouzier R, Guccione E | title = [Androgen receptors in breast cancer: Expression, value and therapeutic prospects] | language = fr | journal = Bull Cancer | volume = 104 | issue = 4 | pages = 363–369 | date = April 2017 | pmid = 28216075 | doi = 10.1016/j.bulcan.2017.01.005 }}</ref><ref name="pmid29940524">{{cite journal | vauthors = Gerratana L, Basile D, Buono G, De Placido S, Giuliano M, Minichillo S, Coinu A, Martorana F, De Santo I, Del Mastro L, De Laurentiis M, Puglisi F, Arpino G | title = Androgen receptor in triple negative breast cancer: A potential target for the targetless subtype | journal = Cancer Treat. Rev. | volume = 68 | pages = 102–110 | date = June 2018 | pmid = 29940524 | doi = 10.1016/j.ctrv.2018.06.005 | doi-access = free | hdl = 11567/914067 | hdl-access = free }}</ref>

===Miscellaneous===
Antiandrogens might be effective and useful in the treatment of [[obsessive–compulsive disorder]] (OCD).<ref name="pmid31814547">{{cite journal |vauthors=Nomani H, Mohammadpour AH, Moallem SM, YazdanAbad MJ, Barreto GE, Sahebkar A |title=Anti-androgen drugs in the treatment of obsessive-compulsive disorder: a systematic review |journal=Curr Med Chem |date=December 2019 |volume=27 |issue=40 |pages=6825–6836 |pmid=31814547 |doi=10.2174/0929867326666191209142209|s2cid=208956450 }}</ref>