Delving into the Latest Updates on Cyproterone Acetate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

CyPat, Cyproterone 17-O-acetate, Cyproterone acetate (JAN/USAN)

+ [6]

Target

AR

Action

antagonists

Mechanism

AR antagonists(Androgen Receptor antagonists)

Therapeutic Areas

NeoplasmsEndocrinology and Metabolic DiseaseSkin and Musculoskeletal Diseases+ [1]

Active Indication

Acne VulgarisHirsutismProstatic Cancer+ [1]

Inactive Indication

Hot Flashes

Originator Organization

Bayer AG

Active Organization

Schering Espana Sa

Bayer Australia Ltd.

Inactive Organization

Barr Laboratories, Inc.

License Organization

Bayer AGADVANZ PHARMA Holdco Ltd.

Drug Highest PhaseApproved

First Approval Date

China (25 Oct 2001),

Acne VulgarisHirsutismProstatic Cancer+ [1]

RegulationOrphan Drug (United States)

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Structure/Sequence

Molecular FormulaC24H29ClO4

InChIKeyUWFYSQMTEOIJJG-FDTZYFLXSA-N

CAS Registry427-51-0

Cyproterone acetate (CA), a synthetic anti-androgen, was injected i.p. into fish at two doses (5 and 50 mg/kg body weight) to evaluate its effects on physiol., biochem., and reproductive parameters.A total of 180 fish were divided into three groups: Control (C), low-dose (LCA), and high-dose (HCA), with two replicates per group.Fish were observed daily for behavior, and water quality was controlled throughout the study.After 28-days of exposure, blood samples were collected to analyze plasma biochem. parameters.Sperm motility, concentration, and histol. analyses of testes and liver tissues were also conducted.Results showed a significant dose-dependent decrease in cholesterol, triglycerides, and testosterone levels in the CA-treated groups, with the highest reduction observed in the HCA group (P < 0.05).Sperm motility was significantly reduced in the low-dose (66.1 ± 2.2%) and high-dose (36.5 ± 3.9%) groups compared to the control group (79.5 ± 2.2%).Similarly, sperm concentration and motility time were significantly reduced in the CA-treated groups (P < 0.05).The gonadosomatic index (GSI) also decreased significantly in the treated groups, with the HCA group showing the lowest GSI (P < 0.05), indicating impaired gonadal development.Histol. anal. of the testes revealed delayed spermatogenesis, with the HCA group predominantly showing immature gonadal stages (Stage II), and a significant reduction in spermatocytes and spermatozoa.Liver histol. indicated necrosis, cell death, blood congestion, and vacuolization in both the LCA and HCA groups, particularly at the high dose (P < 0.05), suggesting hepatotoxicity.In conclusion, CA exerted significant endocrine-disrupting effects in fish, impairing sperm motility, gonadal development, and liver function in a dose-dependent manner.The high-dose treatment caused pronounced effects, including hepatocellular injury and a severe decline in reproductive health.These findings highlight the potential risks of cyproterone acetate as an endocrine disruptor and emphasize the importance of its effects on aquatic species, particularly in ecotoxicol. assessments.

01 Jul 2025·JOURNAL OF HAZARDOUS MATERIALS

Screening and risk assessment of priority organic micropollutants for control in reclaimed water in China

Article

Author: Wang, Zijian ; Meng, Qingling ; Wen, Zhao ; Sun, Kaicheng ; Xue, Honghai

Organic micropollutants (OMPs) in reclaimed water have been frequently detected over the past decades, posing significant risks to ecosystems and human health. Given the complexity of these pollutants and the differences in their risk and toxicity, current assessments remain incomplete. This study conducted a large-scale investigation of OMPs in reclaimed water across China and developed a comprehensive multi-criteria integrated scoring method based on OMP toxicity and exposure potential. This method aims to protect aquatic organisms and human health by screening and prioritizing OMPs in reclaimed water, classifying their priority levels, and creating a prioritized control list. The study quantified OMP exposure potential, environmental persistence, bioaccumulation, and impacts on ecology and human health. The survey detected 369 OMPs from 11 chemical classes, with 325 compounds passing pre-selection. According to the prioritization scheme, 29 OMPs were identified as high priority, 171 as medium priority, and 125 as low priority. The BPs and Other Industrial Chemicals categories had the highest average maximum concentrations, followed by HPCCs and PAEs. High-priority pollutants were dominated by PAHs and PCBs, each comprising 31.03 %. Medium- and low-priority groups were mainly composed of Pesticides. PAHs and PCBs showed higher risk quotients, indicating significant ecological risks, while PCB 126, BaP, and PFOA exhibited high toxicity and potential health risks. This study provides valuable information for controlling priority pollutants in Chinese reclaimed water and establishes a foundation for OMP risk management. Future research should intensify monitoring to ensure the safe and sustainable use of water resources.

19 May 2025·JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Effect of Spironolactone and Cyproterone Acetate on Breast Growth in Transgender People: A Randomized Clinical Trial

Article

Author: Leemaqz, Shalem Y ; Kasielska-Trojan, Anna K ; Doery, James C G ; Cheung, Ada S ; Mikołajczyk, Maksym ; Zajac, Jeffrey D ; Angus, Lachlan M

Abstract:

Context:

Transgender people with sex recorded male at birth desiring feminization commonly use cyproterone acetate or spironolactone as antiandrogens with estradiol, but the optimal antiandrogen is unclear.

Objective:

We aimed to assess the effect of antiandrogens on breast development. We hypothesized this would be greater in those treated with cyproterone acetate than spironolactone due to more potent androgen receptor antagonism and suppression of serum total testosterone concentrations.

Methods:

A randomized clinical trial was conducted between 2020-2022 at an outpatient endocrinology clinic. Transgender people aged 18+ years old commencing feminizing gender affirming hormone therapy were included. The intervention was standardized estradiol therapy plus either spironolactone 100 mg daily or cyproterone acetate 12.5 mg daily for 6 months. The primary outcome was breast development as measured by the breast–chest distance. Secondary outcomes included estimated breast volume, suppression of serum total testosterone concentration <2 nmol/L, and Gender Preoccupation and Stability Questionnaire (GPSQ).

Results:

Sixty-three people (median age 25 years) were enrolled, randomized, and included in intention to treat analysis (cyproterone acetate n = 32, spironolactone n = 31). At 6 months, there was no between-group difference in breast–chest distance (mean difference 0.27 cm, 95% CI −0.82 to 1.35, P = .6) or estimated breast volume (mean difference 17.26 mL, 95% CI −16.94 to 51.47, P = .3). Cyproterone acetate was more likely to suppress serum testosterone concentration to <2 nmol/L (odds ratio 9.01, 95% CI 1.83 to 4.44, P = .008). Changes in GPSQ were similar between groups.

Conclusion:

Antiandrogen choice should be based on clinician and patient preference with consideration of side effects. Further research is needed to optimize breast development in transgender people.

1

News (Medical) associated with Cyproterone Acetate

16 Jul 2019

·www.bioportfolio.com

Canada: National Pharmacare Or ‘Fill The Gaps’?

A national pharmacare program in Canada could make it harder to access higher cost drugs. Related Stories ‘UK Waiver’ For SPCs Proposed In Case Of No-Deal Brexit EMA Reviews Meningioma Risk With Cyproterone Medicines NICE Overcomes UK Reimbursement Doubts Over Forxiga, US FDA Says No To Approval

100 Deals associated with Cyproterone Acetate

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External Link

KEGG	Wiki	ATC	Drug Bank
D01368	Cyproterone Acetate	G03HA01	DB04839

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Acne Vulgaris	China	Schering Espana Sa	25 Oct 2001
Hirsutism	China	Schering Espana Sa	25 Oct 2001
Prostatic Cancer	China	Schering Espana Sa	25 Oct 2001
Puberty, Precocious	China	Schering Espana Sa	25 Oct 2001

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hot Flashes	Phase 3	United States	Barr Laboratories, Inc.	01 Dec 1999

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ENDO2024	Not Applicable	-	-	Cyproterone Acetate 12.5mg	jjnlkjykqn(menrmrtdcs) = nzsusdqlsl pnnzfgbrtf (ezgdxklpud, 158.6) View more	-	01 Jun 2024
				Spironolactone 100mg	jjnlkjykqn(menrmrtdcs) = vuefakrbox pnnzfgbrtf (ezgdxklpud, 112.03) View more
SAT397 (ENDO2023)	Not Applicable	-	89	Cyproterone Acetate 12.5 mg/day	qmietlcnll(oedotifevh) = yblnwavypy xutrxoaemn (xcenziclpv, ( - 25.86) to ( to 1.58)) View more	Positive	05 Oct 2023
				Standard Dose of Cyproterone Acetate	qcmjvrawxb(njpbnenpru) = wvyuikkdcw xalsffyjvl (twqswuxyts )
ESH2023	Not Applicable	-	56	Cyproterone acetate <25 mg/day	eeoggigrod(xhambxjmfa) = zanaklwflw nmknwdblmk (jrsutkmxfu ) View more	Negative	01 Jun 2023
				Cyproterone acetateoestradiol (Reference population (oestradiol without antiandrogen))	eeoggigrod(xhambxjmfa) = umktnzartp nmknwdblmk (jrsutkmxfu ) View more
SUN-042 (ENDO2020)	Not Applicable	-	-	Low Dose Cyproterone Acetate	rjihsuulcy(dkdjxgwbxc) = four cases in the High Dose Cyproterone Acetate group wflvxwelaz (grjnijjple ) View more	Positive	08 May 2020
				High Dose Cyproterone Acetate
ESPE2016	Not Applicable	-	27	Cyproterone Acetate (CA)	uyfnbmcuvc(obzadcmwbp) = became more unfavourable during CA, but restored with addition of E nanbqgrmmy (xwjnysibcx ) View more	-	10 Sep 2016
				Cyproterone Acetate + Estrogens (CA+E)
ESPE2014	Not Applicable	Fibrous Dysplasia, Polyostotic \| Puberty, Precocious	-	Ketoconazole	fhbtocjxlx(kkhynvfiia) = jbejfnjgxr sdrqjlssed (wxiklcyfgb )	-	18 Sep 2014
				Cyproterone Acetate	fhbtocjxlx(kkhynvfiia) = jjpjmrqnje sdrqjlssed (wxiklcyfgb )