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Dienogest

A Review of its Use in the Treatment of Endometriosis

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Abstract

Dienogest (Visanne®) is a synthetic oral progestogen with unique pharmacological properties that is indicated at a dosage of 2mg/day for the treatment of endometriosis. It is generally highly selective for the progesterone receptor and displays strong progestational effects and moderate antigonadotrophic effects, but no androgenic, glucocorticoid or mineralocorticoid activity. Dienogest has moderate affinity for progesterone receptors (10% that of progesterone) and at a dosage of 2mg/day only moderately suppresses estradiol levels. It has high oral bioavailability and a half-life suitable for once-daily administration.

In randomized clinical trials, oral dienogest was significantly more effective than placebo in reducing pelvic pain in patients with confirmed endometriosis. In trials comparing oral dienogest for 16 or 24 weeks with gonadotropin-releasing hormone (GnRH) agonists commonly used in the treatment of endometriosis, dienogest was noninferior to depot leuprorelin in reducing pelvic pain and was not significantly different from intranasal buserelin and depot triptorelin in improving combined symptoms/signs scores or revised American Fertility Society (rAFS) staging scores, respectively. Improvements were also noted in some measures of health-related quality of life. The efficacy of dienogest was sustained during long-term treatment for more than 1 year. Dienogest was generally well tolerated and was not considered to be associated with clinically relevant androgenic effects. It appeared to have fewer hypoestrogenic effects than the GnRH agonists. Dienogest was associated with a high incidence of abnormal menstrual bleeding patterns, although this was generally well tolerated by patients, with few discontinuing therapy, and the bleeding intensity and frequency decreased over time. Therefore, oral dienogest offers an effective, generally well tolerated therapeutic option for the long-term treatment of endometriosis.

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Authors and Affiliations

  1. Adis, a Wolters Kluwer Business, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore, Auckland, 0754, New Zealand

    Paul L. McCormack

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  1. Paul L. McCormack
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Correspondence to Paul L. McCormack.

Additional information

Various sections of the manuscript reviewed by: S. Ferrero, Department of Obstetrics and Gynaecology, San Martino Hospital and University of Genoa, Genoa, Italy; G. Köhler, Department of Gynecology and Obstetrics, University of Greifswald, Greifswald, Germany; M.R. Laufer, Division of Gynecology, Brigham and Women’s Hospital, Harvard Medical School, Boston, Massachusetts, USA; E. Somigliana, Fondazione Cà Granda, Ospedale Maggiore Policlinico, Milan, Italy; C. Templeman, Department of Obstetrics and Gynecology, Women’s and Children’s Hospital, Keck School of Medicine of the University of Southern California, Los Angeles, California, USA.

Data Selection

Sources: Medical literature published in any language since 1980 on ‘dienogest’, identified using MEDLINE and EMBASE, supplemented by AdisBase (a proprietary database). Additional references were identified from the reference lists of published articles. Bibliographical information, including contributory unpublished data, was also requested from the company developing the drug.

Search strategy: MEDLINE, EMBASE and AdisBase search terms were ‘dienogest’ and ‘endometriosis’. Searches were last updated 1 October 2010.

Selection: Studies in patients with endometriosis who received oral dienogest. Inclusion of studies was based mainly on the methods section of the trials. When available, large, well controlled trials with appropriate statistical methodology were preferred. Relevant pharmacodynamic and pharmacokinetic data are also included.

Index terms: Dienogest, endometriosis, pharmacodynamics, pharmacokinetics, therapeutic use, tolerability.

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McCormack, P.L. Dienogest. Drugs 70, 2073–2088 (2010). https://doi.org/10.2165/11206320-000000000-00000

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