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Last update 20 Mar 2025

Clostebol Acetate

Last update 20 Mar 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

4-Chlorotestosterone acetate, Chlorotestosterone acetate, 醋酸4-氯睾丸素

+ [1]

Target

Action

agonists

Mechanism

AR agonists(Androgen Receptor agonists)

Therapeutic Areas

Endocrinology and Metabolic DiseaseHemic and Lymphatic DiseasesSkin and Musculoskeletal Diseases+ [1]

Active Indication

Androgen deficiencyLeukopeniaOsteoporosis+ [1]

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC21H29ClO3

InChIKeyXYGMEFJSKQEBTO-KUJXMBTLSA-N

CAS Registry855-19-6

100 Clinical Results associated with Clostebol Acetate

100 Translational Medicine associated with Clostebol Acetate

100 Patents (Medical) associated with Clostebol Acetate

385

Literatures (Medical) associated with Clostebol Acetate

29 Jan 2025·Clinical Chemistry and Laboratory Medicine (CCLM)

Clostebol and sport: about controversies involving contamination vs. doping offence

Author: Plebani, Mario ; Kintz, Pascal ; Gheddar, Laurie ; Salomone, Alberto ; Pichini, Simona

AbstractClostebol, the 4-chloro derivative of testosterone, available as Over The Counter product in pharmacies and drugstores in several countries, is mostly commercialized as a cream or spray in the form of acetate ester. As other anabolic steroids, clostebol is listed as a prohibited substance by the World Anti-Doping Agency (WADA). Controlled transdermal application of clostebol acetate has been reported to produce detectable amounts of its metabolites in urine, even after a single exposure. Indeed, a low urine concentration can be interpreted as the tail of a drug voluntarily used to enhance performance or a direct consequence of a contamination. The increased number of adverse analytical findings (AAFs) involving clostebol reported in the last years should lead to highlight the need for athletes to be warned against personal and /or accidental use/exposure of dermal preparation containing this doping agent. Further discussion on possible threshold limits and laboratory testing on different matrices (e.g. hair) to better clarify the origin of minimal amounts of clostebol in urines is advisable.

01 Dec 2024·Journal of Veterinary Research

Determination of clostebol residues in the urine of slaughter animals using liquid chromatography–tandem mass spectrometry

Article

Author: Kłopot, Alicja ; Matraszek-Żuchowska, Iwona ; Zdonek, Paulina ; Grzelak, Justyna

AbstractIntroductionSynthetic anabolic hormones, which may pose a potential risk to human health, should not be used in fattening food-producing animals. Because of the hormonal effects they cause, growth-promoting compounds are banned by legislation in the EU for use in animal husbandry. Consequently, all EU member states are required to conduct monitoring tests on the content and residues of these compounds in prescribed biological matrices to ensure the safety of food consumers. The aim of this research was to develop a liquid chromatography–tandem mass spectrometry method for the detection of the residue of one such anabolic hormone, clostebol in food animal urine.Material and MethodsClostebol and its marker metabolite residues were determined by a method involving enzymatic hydrolysis, isolation of compounds from urine on a C18 solid-phase extraction (SPE) column, purification of the extract by liquid–liquid extraction using n-pentane and a NH2 SPE column, and detection by liquid chromatography–tandem mass spectrometry.ResultsNo traces of this anabolic steroid hormone or its metabolites were found in any of the samples tested. The method was validated in accordance with the current requirements for confirmatory methods, and the determined parameters of the decision limits necessary for assessing sample compliance met the specified criteria.ConclusionIn 2023, the method was introduced for testing under the National Control Plan in Poland. Up to July 19, 2024, 53 urine samples from different animal species had been tested.

01 Mar 2024·The Journal of Steroid Biochemistry and Molecular Biology

Biotransformation of anabolic androgenic steroids in human skin cells

Article

Author: Karim, Ziaul ; Zoschke, Christian ; Parr, Maria Kristina ; Botrè, Francesco ; Schlörer, Nils ; de la Torre, Xavier ; Liu, Lingyu

In comparison to well-known drug-metabolizing organs such as the liver, the metabolic capacity of human skin is still not well elucidated despite the widespread use of topical drug application. To gain a comprehensive insight into anabolic steroid metabolism in the skin, six structurally related anabolic androgenic steroids, testosterone, metandienone, methyltestosterone, clostebol, dehydrochloromethyltestosterone, and methylclostebol, were applied to human keratinocytes and fibroblasts derived from the juvenile foreskin. Phase I metabolites obtained from incubation media were analyzed by gas chromatography-mass spectrometry. The 5α-reductase activity was predominant in the metabolic pathways as supported by the detection of 5α-reduced metabolites after incubation of testosterone, methyltestosterone, clostebol, and methylclostebol. Additionally, the stereochemistry structures of fully reduced metabolites (4α,5α-isomers) of clostebol and methylclostebol were newly confirmed in this study by the help of inhouse synthesized reference materials. The results provide insights into the steroid metabolism in human skin cells with respect to the characteristics of the chemical structures.

100 Deals associated with Clostebol Acetate

External Link

KEGG	Wiki	ATC	Drug Bank
-	Clostebol Acetate	G03B	DB15984

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Androgen deficiency	Italy	-	-
Androgen deficiency	Germany	-	-
Leukopenia	China	-	-
Osteoporosis	China	-	-
Wounds and Injuries	China	-	-

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