Endovelle Mechanism of Action

Pharmacotherapeutic group: Progestogens. ATC code: G03DB08.
Pharmacology: Pharmacodynamics: Pharmacodynamic effects: Dienogest is a nortestosterone derivative with no androgenic but rather an antiandrogenic activity of approximately one third of that of cyproterone acetate. Dienogest binds to the progesterone receptor of the human uterus with only 10% of the relative affinity of progesterone. Despite its low affinity to the progesterone receptor, dienogest has a strong progestogenic effect in vivo. Dienogest has no significant androgenic, mineralocorticoid or glucocorticoid activity in vivo.
Mechanism of action: Dienogest acts on endometriosis by reducing the endogenous production of estradiol and thereby suppresses the trophic effects of estradiol on both the eutopic and ectopic endometrium. When given continuously, dienogest leads to a hypoestrogenic, hypergestagenic endocrine environment causing initial decidualization of endometrial tissue followed by atrophy of endometriotic lesions. Additional properties, like immunologic and antiangiogenic effects, seem to contribute to the inhibitory action of dienogest on cell proliferation.
Pharmacokinetics: Methodology: This is an open-label, single-dose, randomized, two-period, two-sequence, two-treatment, crossover study, designed to evaluate the comparative bioavailability of two formulations of dienogest 2 mg tablets administered to healthy female subjects under fasting conditions.
Subjects were randomly assigned to one of the two dosing sequence AB or BA under fasting conditions.
Concentrations of dienogest were measured from the samples collected over a 60-hour interval after dosing in each period.
Summary-Conclusion: Pharmacokinetic Results: Analyte: Dienogest (N=27). (See Table 1.)


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Safety Results: No serious AEs were reported during the conduct of this study.
None of the AEs had a significant impact on the safety of the subjects or on the integrity of the study results.