Drug intelligence / Profile preview

dienogest

Development stage
Phase 4
Lead developer
Bayer HealthCare Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Dienogest is a synthetic oral progestin (progestogen) and a derivative of 19-nortestosterone, used primarily for the treatment of endometriosis as monotherapy and as an oral contraceptive in combination with estrogens such as ethinylestradiol or estradiol valerate[2][3][4]. It acts mainly as an agonist at the progesterone receptor, producing potent progestogenic effects in the endometrium that lead to antiproliferative, immunologic, and antiangiogenic actions. This results in decidualization and subsequent atrophy of endometrial tissue[2][8]. Dienogest also exhibits antiandrogenic activity by antagonizing androgen receptors, which can improve symptoms like acne and hirsutism[2][6]. Its unique structure confers high oral bioavailability (>90%) and a short plasma half-life (~10 hours), reducing risk of accumulation[6][8]. Unlike some other progestins, it has minimal impact on metabolic or cardiovascular systems. Developed for both contraception (in combination pills) and management of endometriosis-related pain, it is approved for these indications in Europe, Japan, Australia, Malaysia, Singapore—and marketed under several brand names including Visanne (for endometriosis) and Natazia/Qlaira (as contraceptives)[2][7].

Brand names
NataziaVisanneQlaira
Other names
dienogest
02

Targets

SHBG (Sex hormone-binding globulin)SERPINA6 (Corticosteroid-binding globulin)AR (Adrenergic receptors)PR (Progesterone receptor)

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