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Dienogest is a derivative of nortestosterone, characterized by antiandrogenic activity that is approximately one-third that of cyproterone acetate. Dienogest binds to progesterone receptors in the human uterus with only 10% relative affinity for progesterone receptors. Despite its low affinity for progesterone receptors, dienogest is characterized by a potent progestagenic effect in vivo. Dienogest has no significant mineralocorticoid or glucocorticoid activity in vivo.

Dienogest acts on endometriosis by inhibiting the trophic effects of estrogen on eutopic and ectopic endometrium, due to decreased estrogen production in the ovaries and decreased plasma concentrations.

With prolonged use causes initial decidualization of endometrial tissue with subsequent atrophy of endometrioid foci. Additional properties of dienogest, such as immunologic and antiangiogenic, probably contribute to its suppressive effect on cell proliferation. The benefit of dienogest over placebo for pelvic pain associated with endometriosis was demonstrated in a placebo-controlled clinical trial of the efficacy and safety of dienogest for the treatment of endometriosis.

After 3 months of therapy, a statistically significant difference between dienogest and placebo was demonstrated, as well as a clinically significant reduction in pain compared with baseline: mean reduction was 27.4 mm ± 22.9 on a visual analog scale (VAS, 0-100 mm). In the extended open-label phase of this study, a sustained reduction in endometriosis-associated pelvic pain was observed with a duration of therapy up to 15 months.

No reduction in bone mineral density (BMD) was observed, and there was no significant effect of dienogest on standard laboratory parameters, including total and biochemical blood counts, liver enzymes, lipids, and glycated hemoglobin (HbA1C). Currently, there are no data available on a long-term study of MPCT and fracture risk with dienogest therapy. In a 12-month clinical trial involving adolescent girls, 93% of the patients showed a 1.2% decrease in lumbar spine (at the L2-L4 level) MSCT during dienogest therapy compared to baseline data; 6 months after the end of treatment, MSCT increased by 0.6%.

During the period of dienogest therapy a moderate decrease in the concentration of endogenous estrogens was observed.

Preclinical data obtained in animal pharmacological safety studies do not indicate the existence of a risk for humans. However, it should be taken into account that sex hormones can stimulate the growth of hormone-dependent tissues and tumors.

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LLC Pharmasyntez-Tyumen

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