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GlossaryNonsteroidal 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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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”

RU58841 significantly increases hair growth rate and initiates more hair cycles, but doesn't affect hair thickness, suggesting it could be a new treatment for baldness.

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”

Flutamide caused damage to male rat reproductive organs and may affect fertility.

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 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)”

Certain hydroxycinnamate derivatives may effectively inhibit enzymes linked to hair loss with low toxicity.

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”

Antiandrogens like flutamide are effective in treating conditions like prostate cancer and hair loss, but there's a need for more potent versions. Understanding their structure can help develop better treatments.

research Clinical applications of antiandrogens

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

Antiandrogens are effective for conditions like prostate cancer and skin issues, but more research is needed to confirm their benefits and minimize side effects.

research The antiandrogenic effect of finasteride against a mutant androgen receptor

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

Finasteride may improve prostate cancer treatment outcomes.

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)”

Proxalutamide improved blood markers related to inflammation, immune response, and clotting in COVID-19 patients, potentially reducing hospitalizations.

research Antiandrogens

December 2022 in “CRC Press eBooks”

Antiandrogens block male hormones and are not safe during pregnancy.

research Oral Contraceptives as Anti-Androgenic Treatment of Acne

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

Birth control pills can help reduce mild to moderate acne in women.

research Pharmacology of antiandrogens

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

Antiandrogens affect androgen-dependent body functions and are used for various medical conditions, with some risks like fetus feminization, but new forms like 17α-propylmesterolone show promise for acne without systemic effects.

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”

New compounds show promise for treating hair loss, enlarged prostate, and prostate cancer, with some being more effective and having different side effects than current treatments.

Female Antiandrogens: Significance, Treatment, and Environmental Concerns

research Female Antiandrogens

1 citations , October 2017 in “Elsevier eBooks”

Antiandrogens can treat female hormonal conditions, but environmental ones may harm reproductive health.

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”

A protein called CBP is found in prostate cancer and can increase the effectiveness of certain prostate cancer treatments.

Evaluation of RU58841 as an Anti-Androgen in Prostate PC3 Cells and a Topical Anti-Alopecia Agent in the Bald Scalp of Stumptailed Macaques

research Evaluation of RU58841 as an Anti-Androgen in Prostate PC3 Cells and a Topical Anti-Alopecia Agent in the Bald Scalp of Stumptailed Macaques

18 citations , January 1998 in “Endocrine”

RU58841, a nonsteroidal anti-androgen, showed potential as a topical treatment for hair loss, increasing hair density, thickness, and length without systemic side effects in Stumptailed Macaques.

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)”

Completing a 14-day proxalutamide treatment significantly lowers death rates in hospitalized COVID-19 patients.

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)”

Hirsutism and alopecia during menopause can be diagnosed and treated with specific hormonal and topical therapies.

research Bicalutamide in Dermatology: A Narrative Review

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

Bicalutamide may effectively treat female pattern hair loss with minimal side effects.

research Bioavailability File: Bicalutamide

August 2025 in “Fabad Journal of Pharmaceutical Sciences”

Bicalutamide effectively treats prostate cancer but needs careful monitoring for side effects.

research Flutamide

January 2025

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

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Related Terms

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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

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

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

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

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

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

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

research Androgen Receptor Antagonists (Antiandrogens) Structure-Activity Relationships

research Clinical applications of antiandrogens

research The antiandrogenic effect of finasteride against a mutant androgen receptor

research Antiandrogens

research Oral Contraceptives as Anti-Androgenic Treatment of Acne

research Pharmacology of antiandrogens

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

research Female Antiandrogens

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

research Evaluation of RU58841 as an Anti-Androgen in Prostate PC3 Cells and a Topical Anti-Alopecia Agent in the Bald Scalp of Stumptailed Macaques

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

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

research Bicalutamide in Dermatology: A Narrative Review

research Bioavailability File: Bicalutamide

research Flutamide

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

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

research Targets to treat androgen excess in polycystic ovary syndrome

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

research New Methods of Endocrine Management of Prostatic Cancer

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

research Diseases on Hair Follicles Leading to Hair Loss Part I: Nonscarring Alopecias