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Glossary Nonsteroidal Antiandrogens

medications that block male hormones without activating their receptors

Nonsteroidal Antiandrogens (NSAA) are medications that block the action of androgens (male hormones like testosterone) by binding to androgen receptors without activating them. They are commonly used in the treatment of conditions like prostate cancer and androgenic alopecia (hair loss) by preventing androgens from stimulating the growth of cancer cells or hair follicles.

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Synthesis and Structure–Activity Relationships of the First Ferrocenyl-Aryl-Hydantoin Derivatives of the Nonsteroidal Antiandrogen Nilutamide

research Synthesis and Structure–Activity Relationships of the First Ferrocenyl-Aryl-Hydantoin Derivatives of the Nonsteroidal Antiandrogen Nilutamide

88 citations , February 2008 in “Journal of Medicinal Chemistry”

Scientists made the first metal-based compounds from a nonsteroidal antiandrogen drug, which showed potential in fighting both hormone-dependent and independent prostate cancer cells.

Histological and Immunohistochemical Examination of the Effect of the Nonsteroidal Antiandrogen Flutamide on Some Organs of the Male Reproductive System in Albino Rats

research Histological and immunohistochemical examination of the effect of the nonsteroidal antiandrogen {flutamide} on some organs of the male reproductive system in albino rats

September 2012 in “The Egyptian Journal of Histology”

In this study, flutamide at therapeutic doses caused significant histological changes in the testes and epididymis of adult albino rats, reducing androgen receptor immunoreactivity and increasing estrogen receptor immunoreactivity.

Preliminary Pharmacokinetics and Metabolism of Novel Non-Steroidal Antiandrogens in the Rat: Relation of Their Systemic Activity to the Formation of a Common Metabolite

research Preliminary pharmacokinetics and metabolism of novel non-steroidal antiandrogens in the rat: Relation of their systemic activity to the formation of a common metabolite

16 citations , October 1994 in “The Journal of Steroid Biochemistry and Molecular Biology”

Two non-steroidal antiandrogens, RU 58841 and RU 56187, form a common metabolite at different rates, which may influence their effects; RU 56187 could be used for prostate cancer treatment and RU 58841 for acne treatment.

A Controlled Study of the Effects of RU58841, a Non-Steroidal Antiandrogen, on Human Hair Production by Balding Scalp Grafts Maintained on Testosterone-Conditioned Nude Mice

research A controlled study of the effects of RU58841, a non-steroidal antiandrogen, on human hair production by balding scalp grafts maintained on testosterone-conditioned nude mice

10 citations , November 1997 in “British Journal of Dermatology”

This study found that the non-steroidal antiandrogen RU58841 increased hair growth rates and promoted hair cycle initiation in balding human scalp grafts on testosterone-conditioned nude mice, indicating a positive effect on hair growth.

research A controlled study of the effects of RU58841, a non-steroidal antiandrogen, on human hair production by balding scalp grafts maintained on testosterone-conditioned nude mice

9 citations , November 1997 in “British Journal of Dermatology”

research Pharmacology of antiandrogens

97 citations , November 1986 in “Journal of Steroid Biochemistry”

This review discusses the pharmacological properties and clinical applications of cyproterone acetate and similar antiandrogens, noting previous failures in local applications due to concentration limitations; it reports no new empirical results.

research Recent Advances in the Chemistry and Pharmacological Activity of New Steroidal Antiandrogens and 5α-Reductase Inhibitors

20 citations , March 2005 in “Current Medicinal Chemistry”

This study reports that newly synthesized steroidal trienones exhibit higher 5α-reductase inhibitory activity than dienones in various biological models, suggesting potential use in treating androgen-dependent diseases.

Female Antiandrogens: Significance, Treatment, and Environmental Concerns

research Female Antiandrogens

1 citations , October 2017 in “Elsevier eBooks”

This review examines the effects of antiandrogens on female reproductive systems, particularly regarding environmental endocrine disruptors, and presents no new research findings.

The Transcriptional Co-Activator cAMP Response Element-Binding Protein-Binding Protein Is Expressed in Prostate Cancer and Enhances Androgen- and Anti-Androgen-Induced Androgen Receptor Function

research The Transcriptional Co-Activator cAMP Response Element-Binding Protein-Binding Protein Is Expressed in Prostate Cancer and Enhances Androgen- and Anti-Androgen-Induced Androgen Receptor Function

72 citations , January 2003 in “American Journal of Pathology”

This study found that the co-activator CBP enhances the agonistic action of hydroxyflutamide on androgen receptors, suggesting a mechanism for therapy resistance in prostate cancer.

research Natural Product-InspiredBis(trifluoromethyl) PhenylHydroxycinnamate Derivatives as Promising Nonsteroidal Inhibitorsof Human Steroid 5α-Reductase Type-1: Synthesis, InVitro, and In Silico Studies

August 2025 in “OPAL (Open@LaTrobe) (La Trobe University)”

This study found that hydroxycinnamate derivatives, especially a compound named 10a, effectively inhibited SRD5A1 activity and protein expression in cell assays, suggesting potential for treating androgen-related conditions.

research Clinical applications of antiandrogens

29 citations , October 1988 in “Journal of Steroid Biochemistry”

This review discusses the use of antiandrogens for various conditions like prostate cancer and highlights their potential benefits in remission rates and symptom improvement, but it reports no new clinical results.

research The antiandrogenic effect of finasteride against a mutant androgen receptor

20 citations , May 2011 in “Cancer Biology & Therapy”

This study found that finasteride decreased DHT-stimulated AR activity and cell growth in prostate cancer cells with mutant AR, but not in those with wild type AR.

research Antiandrogens

December 2022 in “CRC Press eBooks”

This research outlines that antiandrogens have mechanisms involving competitive inhibition of androgen binding and enzyme inhibition, with contraindications during pregnancy due to potential fetal risks.

research Development of radioiodinated nonsteroidal androgen receptor ligands for spect imaging of prostate cancer

1 citations , May 2001 in “Journal of Labelled Compounds and Radiopharmaceuticals”

Scientists at the University of Michigan Medical School successfully created a special compound that can be used to improve imaging of prostate cancer.

Androgen Receptor Antagonists Structure-Activity Relationships

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 Non polycystic ovary syndrome–related endocrine disorders associated with hirsutism

39 citations , May 2011 in “European Journal of Clinical Investigation”

This review discusses the various causes of hirsutism other than PCOS, emphasizing the importance of distinguishing potentially life-threatening conditions like androgen-secreting tumors from more benign causes; it reports no new clinical findings.

Proxalutamide Improves Inflammatory, Immunologic, and Thrombogenic Markers in Mild-to-Moderate COVID-19 Males and Females: An Exploratory Analysis of a Randomized, Double-Blinded, Placebo-Controlled Trial Early Antiandrogen Therapy with Proxalutamide

research Proxalutamide Improves Inflammatory, Immunologic, and Thrombogenic Markers in Mild-to-Moderate COVID-19 Males and Females: an Exploratory Analysis of a Randomized, Double-Blinded, Placebo-Controlled Trial Early Antiandrogen Therapy (EAT) with Proxalutamide (The EAT-Proxa Biochemical AndroCoV-Trial)

5 citations , July 2021 in “medRxiv (Cold Spring Harbor Laboratory)”

This study found that proxalutamide improved immunologic, inflammatory, thrombotic, and oxygen markers in both female and male COVID-19 outpatients, which may support its association with lower hospitalization rates compared to standard care.

research Oral Contraceptives as Anti-Androgenic Treatment of Acne

16 citations , July 2002 in “JOGC/Journal of obstetrics and gynaecology Canada”

This review discusses treatments for female acne, highlighting the effectiveness of low-dose oral contraceptives and noting their similar side effects to placebo; it reports no new clinical results.

research New Methods of Endocrine Management of Prostatic Cancer

67 citations , January 1987 in “The Journal of urology/The journal of urology”

New hormonal therapies can help treat advanced prostate cancer but may cause testicular issues.

research Recent discoveries and developments of androgen receptor based therapy for prostate cancer

17 citations , January 2015 in “MedChemComm”

New treatments for prostate cancer are less toxic and show promise, but more research is needed to enhance their effectiveness and reduce side effects.

research Efficacy and safety of bicalutamide in female hair loss: a review of the literature

March 2025 in “JAAD reviews.”

This study suggests bicalutamide may be effective in reducing hair loss severity in female pattern hair loss, particularly when other antiandrogen therapies are less effective due to hyperandrogenic conditions.

research Bicalutamide in Dermatology: A Narrative Review

1 citations , August 2024 in “Indian Dermatology Online Journal”

In this study, bicalutamide showed promise in managing female pattern hair loss and reducing minoxidil-induced hypertrichosis, though further research is necessary to refine its use and establish its role in treatment.

research Bioavailability File: Bicalutamide

August 2025 in “Fabad Journal of Pharmaceutical Sciences”

This review highlights that bicalutamide, a non-steroidal antiandrogen used in prostate cancer treatment, is mainly effective through its (R)-enantiomer and emphasizes the need to monitor its adverse effects despite its targeted antiandrogenic action.

research Structural perspectives on the androgen receptor, the elusive shape-shifter

August 2024 in “Steroids”

This review summarizes structural insights into androgen receptor dynamics, highlighting its flexibility in binding numerous partners, which may explain adaptive resistance mutations in cancer and loss of function in androgen insensitivity syndrome.

research Targets to treat androgen excess in polycystic ovary syndrome

14 citations , September 2015 in “Expert Opinion on Therapeutic Targets”

This review discusses potential treatments for androgen excess in polycystic ovary syndrome and reports no new findings, emphasizing the importance of individualized antiandrogenic management to minimize side effects.

Proxalutamide Reduction of Mortality Rate in Hospitalized COVID-19 Patients Depends on Treatment Duration – An Exploratory Analysis of the Proxa-Rescue AndroCoV Trial

research Proxalutamide Reduction of Mortality Rate in Hospitalized COVID-19 Patients Depends on Treatment Duration – an Exploratory Analysis of the Proxa-Rescue AndroCoV Trial

5 citations , July 2021 in “bioRxiv (Cold Spring Harbor Laboratory)”

This study found that a 14-day treatment with proxalutamide significantly reduced the 28-day mortality rate in hospitalized COVID-19 patients compared to placebo, with greater benefits observed among those who adhered to the treatment.

Diagnosis and Treatment of Cutaneous Androgenization During Menopausal Transition and Peri-/Postmenopause: Hirsutism and Alopecia

research Diagnostik und Therapie der kutanen Androgenisierung im klimakterischen Übergang sowie in der Peri- und Postmenopause: Hirsutismus und Alopezie

2 citations , January 2012 in “Journal für Kardiologie (Krause & Pachernegg GmbH)”

This review discusses therapeutic principles for managing hirsutism and androgenetic alopecia during the menopausal transition and peri-/postmenopause but reports no new clinical results.

research Flutamide

January 2025

Flutamide helps with prostate cancer and some skin conditions but can harm the liver.

research Effects of Transcutol P and Precirol ATO-5 on Percutaneous Absorption of Flutamide from Emulgels

June 2021 in “Pharmaceutical sciences”

This study found that flutamide emulgels with 1% Transcutol P enhanced percutaneous absorption through rat skin more effectively than other formulations tested.

research RU 58841, a new specific topical antiandrogen: A candidate of choice for the treatment of acne, androgenetic alopecia and hirsutism

49 citations , January 1994 in “The Journal of Steroid Biochemistry and Molecular Biology”

This study found that the topically applied non-steroidal antiandrogen RU 58841 may reduce androgen-dependent skin conditions in a hamster model with minimal systemic effects.