Skip to main content
Log in

Dienogest

  • Adis New Drug Profile
  • Published:
Drugs Aims and scope Submit manuscript

Abstract

  • ▴ The progestogen dienogest exhibits highly selective binding to the progesterone receptor. It has high progestational and significant antiandrogenic activity, but only moderate antigonadotrophic activity.

  • ▴ Dienogest inhibits ovulation, produces secretory transformation of the endometrium and has antiproliferative effects.

  • ▴ Oral dienogest 2 mg/day plus ethinylestradiol 30 μg/day provides effective contraception (Pearl Index approximately 0.2). Cycle stability is good during long term use of this combination; irregular vaginal bleeding was evident in 6% of women after 12 months’ use.

  • ▴ Androgenic symptoms (including hirsutism, seborrhoea, alopecia, acne vulgaris and hair and skin greasiness) improved in women treated with dienogest plus ethinylestradiol.

  • ▴ The adverse events associated with dienogest are typical of those expected of a progestogen. The drug does not produce androgenic adverse effects and has little clinically significant effect on metabolic, lipid and haemostatic parameters.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. Oettel M, Carol W, Elger W, et al. A 19-norprogestin without 17α-ethinyl group II: dienogest from a pharmacodynamic point of view. Drugs Today 1995 Oct–Nov; 31: 517–36

    CAS  Google Scholar 

  2. Oettel M, Bervoas-Martin S, Elger W, et al. A 19-norprogestin without a 17α-ethinyl group I: dienogest from a pharmacokinetic point of view. Drugs Today 1995 Oct–Nov; 31: 499–516

    CAS  Google Scholar 

  3. Juchem M, Schaffrath M, Pollow K, et al. Dienogest: Bindungsstudien an verschiedenen Rezeptor- und Serumproteinen. In: Teichmann AT, editor. Dienogest: Präklinik und Klinik eines Gestagens. 2nd ed. Berlin: Walter de Gruyter, 1995: 119–33

    Google Scholar 

  4. Stolzner W, Kurischko A, Freund H, et al. Progestagenic and antigonadotrophic activities of STS 557. Exp Clin Endocrinol 1983 Feb;81: 115–21

    Article  PubMed  CAS  Google Scholar 

  5. Oettel M, Kurischko A. STS 557, a new orally active progestin with antiprogestational and contragestational properties in rabbits. Contraception 1980 Jan; 21: 61–9

    Article  PubMed  CAS  Google Scholar 

  6. Böhm W, Hempel E, Carlsohn G. The problematic nature of dosage transformation determination of gestagens [in German]. In: Stech D, Carol W, editors. Proceedings of the IIIrd Jenaer Symposium zur hormonalen Kontrazeption; 1984 Apr 10–11; Jena, Germany. Jena: Friedrich-Schiller-Universität, 1985: 109–13

    Google Scholar 

  7. Katsuki Y, Sasagawa S, Takano Y, et al. Animal studies on the endocrinological profile of dienogest, a novel synthetic steroid. Drugs Exp Clin Res 1997; 23(2): 45–62

    PubMed  CAS  Google Scholar 

  8. Oettel M, Komor A, Goncharov NP, et al. STS 557 as an interceptive in rodents and baboons. Contraception 1980 May; 21: 537–49

    Article  PubMed  CAS  Google Scholar 

  9. Oettel M, Tkocz H, Löw O, et al. Effects of levonorgestrel and STS 557 on testis in rodents. Endokrinologie 1980 Jul; 76: 13–22

    PubMed  CAS  Google Scholar 

  10. Moore C, Walter F, Klinger G, et al. The influence of dienogest on ovulation in younger women and on chosen endocrinological parameters [in German]. In: Teichmann AT, editor. Dienogest: Präklinik und Klinik eines Gestagens. 2nd ed. Berlin: Walter de Gruyter, 1995: 161–9

    Google Scholar 

  11. Schleuβner E, Michels W, Bethge S, et al. Die Wirkung von Dienogest auf die hypothalamisch-hypophysäre Achse: Ergebnisse einer Pilotstudie. In: Teichmann AT, editor. Dienogest: Präklinik und Klinik eines Gestagens. 2nd ed. Berlin: Walter de Gruyter, 1995: 171–9

    Google Scholar 

  12. Spona J, Feichtinger W, Kindermann C, et al. Modulation of ovarian function by an oral contraceptive containing 30μg ethinyl estradiol in combination with 2.00mg dienogest. Contraception 1997 Sep; 56: 185–91

    Article  PubMed  CAS  Google Scholar 

  13. Köhler G, Göretzlehner G, Rudolf K, et al. The effect of a single midcycle administration of 0.5 or 2.0 mg dienogest (17α-cyanomethyl-17β-hydroxy-estra-4,9-dien-3-one) on pituitary and ovarian function: investigation for the use as a postcoital contraceptive. Exp Clin Endocrinol 1984 Dec; 84: 299–304

    Article  PubMed  Google Scholar 

  14. Oettel M, Elger W, Ernst M, et al. Experimentelle Endokrinpharmakologie von Dienogest. In: Teichmann AT, editor. Dienogest: Präklinik und Klinik eines Gestagens. 2nd ed. Berlin: Walter de Gruyter, 1995: 11–21

    Google Scholar 

  15. Oettel M, Carol W, Gräser T, et al. The influence of an ethinyl-estradiol-dienogest combination on serum androgen concentrations. Zentralbl Gynakol 1997; 119(12): 597–606

    PubMed  CAS  Google Scholar 

  16. Hagen H, Hagen A, Lehnert W, et al. The clinical recording of anti-androgenic effects of dienogest [in German]. In: Teichmann AT, editor. Dienogest: Präklinik und Klinik eines Gestagens. 2nd ed. Berlin: Walter de Gruyter, 1995: 223–30

    Google Scholar 

  17. Coll i Capdevila C. Clinical experience with Valette® [abstract no. 101]. Eur J Contracept Reprod Health Care 1998 June; 3 Suppl. 1: 77

    Google Scholar 

  18. Koch M. Influence of STS 557 on the mitotic activity in the endometrium of ovariectomized mice and comparison with the effects of progesterone and levonorgestrel. Exp Clin Endocrinol 1984 May; 83: 310–4

    Article  PubMed  CAS  Google Scholar 

  19. Koch M, Stracke R, Peschke T. Effects of antifertility estrogens and progestins on the endometrial surface of early pregnant rats: a scanning electron microscopic study. Exp Clin Endocrinol 1985 Apr; 85: 138–46

    Article  PubMed  CAS  Google Scholar 

  20. Katsuki Y, Shibutani Y, Aoki D, et al. Dienogest, a novel synthetic steroid, overcomes hormone-dependent cancer in a different manner than progestins. Cancer 1997 Jan 1; 79: 169–76

    Article  PubMed  CAS  Google Scholar 

  21. Lippert TH, Seeger H, Mueck AO, et al. Effect of estradiol, progesterone, and progestogens on calcium influx in cell cultures of human vessels. Menopause 1996; 3(1): 33–7

    Article  Google Scholar 

  22. Strecke J, Stolzner W, Freund H, et al. Interceptive activities of STS 557 in rabbits, mice and rats. Exp Clin Endocrinol 1983 Feb; 81: 122–36

    Article  PubMed  CAS  Google Scholar 

  23. Schubert K, Hobe G, Kauffman G, et al. Synthesis, effects, and metabolism of the progestagen and potential interceptive dienogest. Presented at the International Symposium on the Chemistry of Natural Products; 1984 Jul 9–14; Poznan, Poland. In: Zalewski RI, Skolik JJ, editors. Natural products chemistry. Amsterdam: Elsevier Science Publishers, 1985: 143–58

    Google Scholar 

  24. Komor A, Goncharov NP, Schubert K, et al. STS 557 as an interceptive in baboons. Exp Clin Endocrinol 1983 Feb; 81: 217–21

    Article  PubMed  CAS  Google Scholar 

  25. Komor A, Goncharov NP, Oettel M. Further report on the interceptive STS 557 in baboons. Endokrinologie 1982 Jul; 79: 428–30

    PubMed  CAS  Google Scholar 

  26. Chaudhary J, Sharma RK, Majumdar SS, et al. Effect of STS-557 (17 alpha-cyanomethyl 17β-hydroxy-estra-4,9 (10)-dien-3-one) on blood hormone levels, the testis, accessory sex organs and fertility of rats. Int J Andrology 1990; 13(5): 398–407

    Article  CAS  Google Scholar 

  27. Freund H, Hesse G, Oettel M. Effect of STS 557 on semen composition, fertility and sexual behaviour of male rabbits. Contraception 1980 Jun; 21: 641–50

    Article  PubMed  CAS  Google Scholar 

  28. Majumdar SS, Chaudhary J, Sharma RK, et al. Contraceptive potentiality of STS-557: a feasibility study in male bonnet monkey (Macaca radiata). Contraception 1990 Jun; 41: 641–53

    Article  PubMed  CAS  Google Scholar 

  29. Oettel M, Freund H, Hesse G, et al. Inhibition of male fertility by STS 557. Exp Clin Endocrinol 1983 Feb; 81: 137–45

    Article  PubMed  CAS  Google Scholar 

  30. Sharma RK, Das R. Effects of STS-557 and 20 AET-1 on sperm functions and serum level of testosterone in bonnet monkey (Macaca radiata). Contraception 1992 May; 45: 483–91

    Article  PubMed  CAS  Google Scholar 

  31. Srivastava A, Maikhuri JP, Setty BS. Evaluation of STS-557 as an oral contraceptive in male rat. Contraception 1987 Aug; 36: 253–72

    Article  PubMed  CAS  Google Scholar 

  32. Hobe G, Hillesheim HG, Schumann W, et al. Studies on pharmacokinetics of STS 557 in animal species and man. Exp Clin Endocrinol 1983 Feb; 81: 158–67

    Article  PubMed  CAS  Google Scholar 

  33. Carol W, Klinger G, Michels W, et al. Studies on the pharmacokinetics of contraceptive steroids under steady-state conditions [in German]. Zentralbl Gynakol 1991; 113: 1298–303

    PubMed  CAS  Google Scholar 

  34. Dittgen M, Gräser T, Kaufmann G, et al. Hot spin mixing — a new technology to manufacture solid dispersions. Part 2: Dienogest. Pharmazie 1995; 50(6): 438–9

    CAS  Google Scholar 

  35. Böcker R, Kleingeist B. Der Einfluβ von Dienogest auf das humane Cytochrom P450-Enzymsystem in vitro. In: Teichmann AT, editor. Dienogest: Präklinik und Klinik eines Gestagens. 2nd ed. Berlin: Walter de Gruyter, 1995: 141–7

    Google Scholar 

  36. Balogh A, Lautenschlager MT, Hippius M, et al. The influence of ethinylestradiol (EE) containing contraceptives in combination with dienogest (DNG) or levonorgestrel (LNG) on cytochrome P450IIIA4 in vivo [abstract]. Eur J Endocrinol 1994 Jun; 130 Suppl. 2: 166

    Google Scholar 

  37. Balogh A, Liewald T, Liewald S, et al. The influence of a new sexual steroid — dienogest on the metabolism of caffeine and metamizol [in German]. Zentralbl Gynakol 1990; 112(12): 735–46

    PubMed  CAS  Google Scholar 

  38. Moore C, Walter F, Mellinger U, et al. Multicentre study on contraceptive safety, cycle control and tolerance of MP 2000 Micropille: an interim report [in German]. In: Teichmann AT, editor. Dienogest: Präklinik und Klinik eines Gestagens. 2nd ed. Berlin: Walter de Gruyter, 1995: 203–12

    Google Scholar 

  39. Llewellyn-Jones D, editor. Fundamentals of obstetrics and gynaecology. Volume 2. Gynaecology. 5th ed. London: Faber and Faber Ltd., 1990

    Google Scholar 

  40. Köhler VG, Canzler E, Lembke S, et al. Postcoital contraception with dienogest [in German]. Zentralbl Gynakol 1987; 109: 1296–302

    PubMed  Google Scholar 

  41. Spona J, Feichtinger W, Kindermann C, et al. Clinical profile of Valette® [abstract no. 100]. Eur J ContraceptReprod Health Care 1998 June; 3 Suppl. 1: 77

    Google Scholar 

  42. Köhler G. Die Therapie der Endometriose mit Dienogest: eine Renaissance der Gestagene. In: Teichmann AT, editor. Dienogest: Präklinik und Klinik eines Gestagens. 2nd ed. Berlin: Walter de Gruyter, 1995: 243–51

    Google Scholar 

  43. Heinecke H, Köhler D. Prenatal toxic effects of STS 557. II. Investigation in rabbits: preliminary results. Exp Clin Endocrinol 1983; 81(2): 206–9

    Article  PubMed  CAS  Google Scholar 

  44. Jemilev ZA, Komor A, Strecke J, et al. Chromosomal analysis of baboons and their mothers, following application to mothers of potentially post-ovulation fertility-inhibiting steroids [in German]. Zentralbl Gynakol 1981; 103: 1215–9

    PubMed  CAS  Google Scholar 

  45. Schöneich J, Becker K, Braun R. Investigations on the mutagenic activity of STS 557. Exp Clin Endocrinol 1983 Feb; 81: 210–6

    Article  PubMed  Google Scholar 

  46. Köhler G, Göretzlehner G, Brachmann K. Lipid metabolism during treatment of endometriosis with the progestin dienogest. Acta Obstet Gynecol Scand 1989 Jul; 68: 633–5

    Article  PubMed  Google Scholar 

  47. Nikschick S, Köhler G, Männchen E. Carbohydrate metabolism during treatment of endometriosis with the progestin dienogest. Exp Clin Endocrinol 1989 Sep; 94: 211–4

    Article  PubMed  CAS  Google Scholar 

  48. Köhler G, Lembke S, Brachmann K, et al. Routine liver function testing during treatment of endometriosis with the progestin dienogest [in German]. Zentralbl Gynakol 1989; 111: 807–10

    PubMed  Google Scholar 

  49. Lembke S, Köhler G, Kalmar B, et al. Clinical and paraclinical results with dienogest-combination preparation: the influence on glucose metabolism and voice function [in German]. In: Carol W, Stech D, editors. Proceedings of the IVth Jenaer Symposium zur hormonalen Kontrazeption; 1988 Mar 22–23; Jena, Germany. Jena: Friedrich-Schiller-Universität, 1989: 179–84

    Google Scholar 

  50. Spona J, Feichtinger W, Kindermann C, et al. Double-blind, randomized, placebo controlled study on the effects of the monophasic oral contraceptive containing 30μg ethinyl estradiol and 2.00 mg dienogest on the hemostatic system. Contraception 1997 Aug; 56: 67–75

    Article  PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Rachel H. Foster.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Foster, R.H., Wilde, M.I. Dienogest. Drugs 56, 825–833 (1998). https://doi.org/10.2165/00003495-199856050-00007

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003495-199856050-00007

Keywords

Navigation