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Publication
Safety profile of gestrinone: a systematic review
Advisor(s)
Abstract(s)
Background: Gestrinone is a synthetic hormone derived from 19-nortestosterone, exhibiting androgenic, anabolic, anti-progestogenic, and antiestrogenic effects. Gestrinone subcutaneous implants have been used “off label” for aesthetic purposes due to their anabolic action, promoting accelerated metabolism and muscle gain. Objective: Our goal is to conduct a systematic review focused exclusively on identifying the safety profile of gestrinone use, without addressing efficacy. Methods: This systematic review was performed according to the Joanna Briggs Institute and Cochrane Collaboration recommendations and is reported following the Preferred Reporting Items for Systematic Reviews and Network Meta-Analyses. This article’s searches were carried out in the PubMed, Embase, and Web of Science databases. Results: A total of 32 articles were included in this study. The reported adverse events associated with the use of gestrinone were amenorrhea (41.4% of cases), acne, seborrhea (42.7% of reports), decreased libido (26.5%), and hot flushes (24.2%). Other nonspecific symptoms, such as hoarseness and cramps, were also fairly reported (3.5% and 18.6%, respectively). Other reported effects were associated with breast size reduction (23.7% of patients) and increased transaminases (15.1%). Most studies (40%, n = 24 studies) found significant weight gain (ranging from 0.9 to 8 kg per patient). Abnormalities in bone mineral density were reported in four studies. Conclusions: The evidence remains insufficient to fully understand the risks of gestrinone use associated with its widespread, unregulated use. Thus, further standardized studies and regulatory oversight to ensure patient safety are needed to mitigate potential health risks.
Description
The authors express their gratitude to the Brazilian National Council of Technological and Scientific Development (CNPq) and Coordenação de Aperfeiçoamento de Pessoal de
Nível Superior—Brasil (CAPES)-Finance Code 001.
Keywords
Adverse effects Anabolic action Gestrinone Hormonal implants Synthetic hormones
Citation
Fagundes VL, Marques NC, Lima AF, Cobre AF, Tonin FS, Lazo RE, et al. Safety profile of gestrinone: a systematic review. Pharmaceutics. 2025;17(5):638.
Publisher
MDPI AG