Gestrinone 2.5mg capsules

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 uses associated with its widespread, unregulated use. Thus, further standardized studies and regulatory oversight to ensure patient safety are needed to mitigate potential health risks.

Abstract licence: CC BY 4.0

BackgroundEndometriosis (EMT) is a benign and common estrogen-dependent disease. Hormonal therapy improves pain symptoms in most women with EMT. However, in many cases, laparoscopic fertility preservation surgery is considered a common treatment for EMT. The present study aimed to evaluate the efficacy and safety of dienogest, leuprolide, danazol, gestrinone, mifepristone and levonorgestrel intrauterine system (LNG-IUS) in relieving symptoms and delaying the recurrence of EMT cysts after fertility protection surgery.MethodsWe searched PubMed, the Cochrane Library, Web of Science, EMBase, China National Knowledge Infrastructure, VIP Database, China Biology Medicine disc, WanFang Data databases to collect randomized controlled trials (RCT) related to dienogest, leuprolide, danazol, gestrinone, mifepristone and LNG-IUS as a follow-up treatment after fertility preserving surgery for EMT. After literature screening, data extraction and quality evaluation, effective rate, recurrence rate, pregnancy rate and adverse reaction rate were used as outcome indicators to evaluate the efficacy and safety of drugs. Evidence networks included in the study were drawn and publication bias was assessed. The drugs most likely to be the best postoperative treatment were explored through mixed comparison of different drugs and efficacy ranking.ResultEffective rate: dienogest, leprerelin, gestrinone and LNG-IUS were better than placebo after EMT fertility preservation surgery; dienogest was superior to mifepristone and danazol. LNG-IUS is superior to danazol. LNG-IUS has the highest potential for improving the effectiveness of EMT symptoms. Recurrence rate: the application of dienogest, leuprolide, gestrinone, mifepristone and LNG-IUS after EMT fertility preservation surgery was lower than that of placebo; dienogest and LNG-IUS were lower than danazol. The recurrence rate of dinorgestrel was the last place with the highest performance. Pregnancy rate: in the cases with fertility requirements, dienogest and,leuprolide were better than placebo after EMT fertility preservation surgery; dienogest was superior to danazol, gestrinone and mifepristone. Leuprolide is superior to danazol and gestrinone. The first rank of dienogest pregnancy rate was the highest. Adverse reaction rate: the application of dienogest, leuprolide, danazol, gestrinone, mifepristone and LNG-IUS after EMT fertility preservation surgery was higher than that of placebo. After placebo, LNG-IUS had the highest adverse reaction rate.ConclusionFor patients after fertility preserving surgery for EMT, the recurrence rate of dienogest was the last place with highest preference. The first rank of dienogest pregnancy was the highest.

Abstract licence: CC BY-NC

PurposeEndometriosis is a common, chronic gynecological disease that affects women's fertility potential. Dydrogesterone is an effective and safe drug that is under-utilized due to limited clinical research. The purpose of this evidence mapping is to identify, describe, and analyze the current available evidence regarding dydrogesterone for the treatment of endometriosis.Materials and methodsWe performed a search in electronic databases: Medline, The Cochrane Library, EMBASE, PubMed, CNKI, Wanfang, VIP, and CBM. We also hand-searched google for relevant studies. Our primary outcomes included changes in pain relief including pelvic pain, dysmenorrhea, and dyspareunia. Secondary outcomes included pregnancy rate, frequency of analgesic use, and other reported outcomes according to specific settings in the studies.ResultsOf 377 references screened, 19 studies were included in the data synthesis involving 1709 female participants. Nearly three-quarters were either randomized control trials or clinical control trials. Compared with gestrinone, dydrogesterone relieved dysmenorrhea, increased the pregnancy rate, and reduced the risk of certain adverse events. Compared with GnRH-a, dydrogesterone also lowered the risk of endometriosis recurrence and elevated transaminase levels. Whether there was any difference in efficacy between dydrogesterone and leuprolide acetate, letrozole or traditional Chinese medicine remains unclear due to insufficient data.ConclusionsThe amount and quality of evidence evaluating the effects of dydrogesterone for the treatment of endometriosis is generally very low. Limited evidence suggests that dydrogesterone may have some advantages over gestrinone, GnRH agonists, and other therapeutic interventions in treating endometriosis. However, this conclusion should be interpreted with caution.

Abstract licence: CC BY

Background Pelvic pain secondary to endometriosis is a disabling condition. There are multiple treatments available, with variable endpoints. No prospective controlled studies were carried out evaluating subdermal pellets of gestrinone in this population.Methods One hundred participants with documented deep infiltrative endometriosis who underwent surgery without satisfactory response will be randomly assigned (1:1) to either gestrinone 85 mg subdermal bioabsorbable pellets or placebo. Both arms will receive levonorgestrel-releasing intrauterine system (LNG-IUS 12). The treatment duration will be 6 months, with baseline, 3 months and 6 months clinical visits. The primary endpoint is a combination of serious adverse events (SAEs) accumulated within 6 months of insertion of the gestrinone or placebo pellet and collected through spontaneous reports and clinical findings. They include death, threat or risk to life, need for hospitalization, prolongation of pre-existing hospitalization, permanent disability or damage, congenital anomaly; or significant medical occurrences such as venous thromboembolism. The primary safety outcome will be the percentage of patients who do not experience SAEs 6 months after randomization. Androgenization, changes in laboratory exams and in pelvic pain intensity as well as quality of life (SF-36 and EHP-30 questionnaires) will be further evaluated. Daily data on uterine bleeding patterns and the use of pain relief medication will be remotely collected using an App. Pharmacokinetics profile of gestrinone pellet will be characterized.Conclusion This is the first multicenter randomized controlled trial to evaluate the safety, tolerability and pharmacokinetics profile of subdermal gestrinone pellets and might inform clinical practice for treating these patients.Administrative Information GLADE trial is registered at ClinicalTrials.gov (NCT05570786). This is an investigator-initiated research supported by Biòs Farmacêutica.

Abstract licence: CC BY 4.0