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

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 SaBayer Australia Ltd.

Inactive Organization

Barr Laboratories, Inc.

Drug Highest PhaseApproved

First Approval Date

CN (25 Oct 2001),

Acne VulgarisHirsutismProstatic Cancer+ [1]

RegulationOrphan Drug (US)

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Structure/Sequence

Molecular FormulaC24H29ClO4

InChIKeyUWFYSQMTEOIJJG-FDTZYFLXSA-N

CAS Registry427-51-0

ABSTRACTPurposeTo measure the impact of national regulatory actions implemented in France in August 2018 and June 2019 to reduce the risk of meningioma associated with the use of cyproterone acetate (CPA).MethodsUsing the French National Healthcare database, we calculated the monthly number of CPA users among cisgender women, men and transgender women in 2010–2021, the monthly proportion of users with cerebral imaging screening, and the annual rate of meningioma surgery associated with CPA use. CPA discontinuations and switches were analysed.ResultsBetween 2018 and 2021, the number of individuals exposed to CPA fell by 85% (55 000 in August 2018 versus 7900 users of high‐dose CPA in December 2021), corresponding to two waves of decrease in both use and initiation. This drop was greater among cisgender women (88%) than men (69%) or transgender women (50%). Cerebral imaging screening increased from 11% in June 2018 to 70% in June 2021 for ciswomen (13%–51% for men, 9%–60% for transwomen). After CPA discontinuation, no massive shift to a single product was observed, but, instead, dispersion towards other hormonal therapies. The overall annual rate of meningioma surgery associated with CPA exposure spectacularly decreased between 2017 and 2021 (−93% for ciswomen and −86% for men).ConclusionIn France, high‐dose CPA use sharply decreased after the implementation of national regulatory measures without a massive switch to other hormonal therapies. The increase in cerebral imaging screening did not result in an increase in meningioma surgery associated with CPA, but rather a massive drop of over 90%.

01 Nov 2024·Diabetologia

Transgender healthcare: metabolic outcomes and cardiovascular risk

Review

Author: Andersen, Marianne S ; Glintborg, Dorte ; Christensen, Louise L

Transgender identity is often associated with gender dysphoria and minority stress. Gender-affirming hormone treatment (GAHT) includes masculinising or feminising treatment and is expected to be lifelong in most cases. Sex and sex hormones have a differential effect on metabolism and CVD in cisgender people, and sex hormone replacement in hypogonadism is associated with higher vascular risk, especially in ageing individuals. Using narrative review methods, we present evidence regarding metabolic and cardiovascular outcomes during GAHT and propose recommendations for follow-up and monitoring of metabolic and cardiovascular risk markers during GAHT. Available data show no increased risk for type 2 diabetes in transgender cohorts, but masculinising GAHT increases lean body mass and feminising GAHT is associated with higher fat mass and insulin resistance. The risk of CVD is increased in transgender cohorts, especially during feminising GAHT. Masculinising GAHT is associated with a more adverse lipid profile, higher haematocrit and increased BP, while feminising GAHT is associated with pro-coagulant changes and lower HDL-cholesterol. Assigned male sex at birth, higher age at initiation of GAHT and use of cyproterone acetate are separate risk factors for adverse CVD markers. Metabolic and CVD outcomes may improve during gender-affirming care due to a reduction in minority stress, improved lifestyle and closer surveillance leading to optimised preventive medication (e.g. statins). GAHT should be individualised according to individual risk factors (i.e. drug, dose and form of administration); furthermore, doctors need to discuss lifestyle and preventive medications in order to modify metabolic and CVD risk during GAHT. Follow-up programmes must address the usual cardiovascular risk markers but should consider that biological age and sex may influence individual risk profiling including mental health, lifestyle and novel cardiovascular risk markers during GAHT.

15 Oct 2024·The Journal of Clinical Endocrinology & Metabolism

Impact of Distinct Antiandrogen Exposures on the Plasma Metabolome in Feminizing Gender-affirming Hormone Therapy

Article

Author: Pang, Ken ; Saffery, Richard ; Mansell, Toby ; Novakovic, Boris ; Arman, Bridget ; Kim, Bo Won ; Zajac, Jeffrey D ; Burgner, David ; Kerr, Jessica A ; Cheung, Ada ; Lange, Katherine ; Angus, Lachlan M ; Shepherd, Rebecca

AbstractContextThe plasma metabolome is a functional readout of metabolic activity and is associated with phenotypes exhibiting sexual dimorphism, such as cardiovascular disease. Sex hormones are thought to play a key role in driving sexual dimorphism.ObjectiveGender-affirming hormone therapy (GAHT) is a cornerstone of transgender care, but longitudinal changes in the plasma metabolome with feminizing GAHT have not been described.MethodsBlood samples were collected at baseline and after 3 and 6 months of GAHT from transgender women (n = 53). Participants were randomized to different anti-androgens, cyproterone acetate or spironolactone. Nuclear magnetic resonance-based metabolomics was used to measure 249 metabolic biomarkers in plasma. Additionally, we used metabolic biomarker data from an unrelated cohort of children and their parents (n = 3748) to identify sex- and age-related metabolite patterns.ResultsWe identified 43 metabolic biomarkers altered after 6 months in both anti-androgen groups, most belonging to the very low- or low-density lipoprotein subclasses, with all but 1 showing a decrease. We observed a cyproterone acetate-specific decrease in glutamine, glycine, and alanine levels. Notably, of the metabolic biomarkers exhibiting the most abundant “sex- and age-related” pattern (higher in assigned female children and lower in assigned female adults, relative to assigned males), 80% were significantly lowered after GAHT, reflecting a shift toward the adult female profile.ConclusionOur results suggest an anti-atherogenic signature in the plasma metabolome after the first 6 months of feminizing GAHT, with cyproterone acetate also reducing specific plasma amino acids. This study provides novel insight into the metabolic changes occurring across feminizing GAHT.

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	CN	Schering Espana Sa	25 Oct 2001
Hirsutism	CN	Schering Espana Sa	25 Oct 2001
Prostatic Cancer	CN	Schering Espana Sa	25 Oct 2001
Puberty, Precocious	CN	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	Preclinical	US	Barr Laboratories, Inc.	01 Dec 1999
Prostatic Cancer	Preclinical	US	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	kdlflejfhj(vzzslxvsrf) = qvrjarxoxa kyrqdnnshn (zeklabtcwq, 158.6) View more	-	01 Jun 2024
				Spironolactone 100mg	kdlflejfhj(vzzslxvsrf) = fvuywpxxbo kyrqdnnshn (zeklabtcwq, 112.03) View more
SAT397 (ENDO2023)	Not Applicable	-	89	Cyproterone Acetate 12.5 mg/day	wkxwyzsikl(gfsorhuhyx) = iddfuguina myxnsxraxg (joyqlzmtig, ( - 25.86) to ( to 1.58)) View more	Positive	05 Oct 2023
				Standard Dose of Cyproterone Acetate	ffmfymcjyq(qxtjjpcsdn) = zmtmdzewfo mfviscpfvk (cgqmvmsxke )
ESH2023	Not Applicable	-	56	Cyproterone acetate <25 mg/day	pehhdjtmku(dymsqkxgtc) = btyadiryxy rjsxpeyhzj (lfeznqurmu ) View more	Negative	01 Jun 2023
				Cyproterone acetateoestradiol (Reference population (oestradiol without antiandrogen))	pehhdjtmku(dymsqkxgtc) = wxfxspkfdf rjsxpeyhzj (lfeznqurmu ) View more
SUN-042 (ENDO2020)	Not Applicable	-	-	Low Dose Cyproterone Acetate	skdexbucsk(hdlicgjwds) = four cases in the High Dose Cyproterone Acetate group ppjitwslkr (hlawhfsmic ) View more	Positive	08 May 2020
				High Dose Cyproterone Acetate
ESPE2016	Not Applicable	-	27	Cyproterone Acetate (CA)	(llrrfjqitl) = became more unfavourable during CA, but restored with addition of E sbbtlemjer (kafsjtfbzn ) View more	-	10 Sep 2016
				Cyproterone Acetate + Estrogens (CA+E)
ESPE2014	Not Applicable	Fibrous Dysplasia, Polyostotic \| Puberty, Precocious	-	Ketoconazole	rnjorwfurj(luhhgwtdpe) = tzgmmlgxxe ucdzceqxlk (eqcratmslx )	-	18 Sep 2014
				Cyproterone Acetate	rnjorwfurj(luhhgwtdpe) = edbjlpdjll ucdzceqxlk (eqcratmslx )