Comparative assessment of effectiveness of new drugs for targeted therapy of endometriosis by experimental model

M I Yarmoliskaya, М. А. Petrosyan, M A Petrosyan, Margarita S. Florova, M S Florova, A S Molotkov, A S Denisova, Alexandra S. Denisova, Е. В. Суслова, E V Suslova, Saimat Sh. Tkhazaplizheva, S Sh Tkhazaplizheva
Gynecology · 2018 · vol. 20(5) , pp. 46–51 · doi:10.26442/2079-5696_2018.5.46-51 · W2905145001
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⚙ AI-generated summary by claude@2026-06, 2026-06-09 ⓘ

This study compared new endometriosis therapies to dienogest in rats, finding dienogest and letrozole most effective, but no oral drug matched dienogest's overall efficacy.

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⚙ AI-generated deep summary by claude@2026-06, 2026-06-09 ⓘ

The paper reviews and compares the experimental effectiveness of several proposed targeted drug classes for endometriosis, using dienogest as a reference and drawing on in vitro and animal-model data for aromatase inhibitors, dopamine agonists, biguanides (metformin), vitamin D, and melatonin. Across the cited studies, key reported findings include reduction of endometriotic lesion growth and/or inflammation and angiogenesis (e.g., decreased VEGF/VEGFR-2 signaling, MMP expression, and proinflammatory cytokines), with dienogest highlighted for anti-proliferative and anti-angiogenic effects and for maintaining benefits even under progesterone-receptor blockade in some experiments. The authors explicitly frame the work as a comparative assessment based on heterogeneous preclinical and limited clinical evidence, with varying model systems and outcome measures. This paper is centrally about endometriosis — it evaluates targeted drug effectiveness for endometriosis in experimental models, with dienogest and several alternative agents compared.

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Abstract

Introduction. The chronic, progressive, recurrent nature of the endometriosis results new avenues of targeted therapy for genital endometriosis with high therapeutic efficacy and minimal side effects must be explored. Nowadays, the standard of prolonged specific therapy for endometriosis is the dienogest 2 mg daily, which has already been proven to be effective in vitro, in vivo and in clinical practice. Purpose: to evaluate the effectiveness of new types of targeted pathogenetic therapy for endometriosis on the model of endometriosis in rats compared to dienogest and without treatment. Materials and methods. Endometriosis was induced on 69 Wistar rats by autotransplantation of uterine fragments onto the inner surface of the abdominal wall. After 14 days, the heterotopies had been measured by laparoscopy and then rats were randomized of into one of 6 experimental groups (dienogest, letrozole, cabergoline, metformin, vitamin D, melatonin) or a control group. All drugs were administered daily orally for three weeks, after which an autopsy and re-measuring of the size of endometrial implants were performed. Results. The most pronounced decrease in the size of endometrial implants was observed in the group of animals treated with dienogest (complete resorption - 48%, regression - 48%, without dynamics - 4%) and letrozole (complete resorption - 44%, regression - 56%) without the statistically significant difference between groups. In other groups, a significant decrease in the size of endometrial implants was demonstrated compared with the control, without a statistically significant difference between the groups. Findings. The presented study confirms the absence at the present time of oral drugs for the treatment of endometriosis, comparable in efficacy and safety with dienogest. Further research are needed to evaluate the different combinations of dopamine agonists, biguanides, vitamin D, melatonin as the supplement to the classic hormone-modulating therapy for endometriosis or as monotherapy in patients with contraindications to standard hormone therapy.

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endometriosis

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