Gestogens and anti-gestogens as treatment of endometriosis

In: Modern Approaches to Endometriosis · 1991 · pp. 221–238 · doi:10.1007/978-94-011-3864-2_12 · W32483892
book-chapter OA: closed CC0 ⤵ 3 in-corpus citations
Full text JSON View on OpenAlex View at publisher
AI-generated summary by claude@2026-06+body, 2026-06-28

This chapter describes the therapeutic role of gestagens and anti-gestagens, such as gestrinone, in treating endometriosis as first- and second-line drugs.

One-sentence paraphrase of the abstract; not a substitute for reading it. No clinical advice. How this works

AI-generated deep summary by claude@2026-06, 2026-06-07 · read from full text

This chapter reviews the therapeutic role of gestagens (progestagens) and anti-gestagens in endometriosis, contrasting this history with the better-known development of danazol and LHRH analogues since the 1970s. It describes gestagens first and then focuses on anti-gestagens exemplified by gestrinone, discussing the place of these drug classes as first- and second-line options, while noting that other drug developments have overshadowed progestagens/anti-gestagens in the literature. The main limitation is that the text is a narrative account intended to situate these therapies rather than present new primary experimental results, and it points readers elsewhere for details on danazol and LHRH analogues. This paper is centrally about endometriosis — it is a chapter describing the place of gestogens/progestagens and anti-gestagens (especially gestrinone) in endometriosis treatment.

Read from the paper's body, not the abstract. Not a substitute for reading the paper. No clinical advice. How this works

Full text 13,415 characters · extracted from oa-doi-fallback · 3 sections · click to expand

Abstract

Since the 1970s the main thrust of drug research and development in endometriosis has been with danazol and latterly the LHRH analogues. The role of these drugs is explored in detail elsewhere in this book and there is no doubt about their efficacy. However, these developments have tended to overshadow the use of progestagens and anti-gestagens in treatment of the disease and yet both these types of compounds are also effective. They undoubtedly have an important therapeutic role both as first- and second- line drugs. The purpose of this chapter is to describe the place of these drugs in the treatment of endometriosis. We shall begin by describing gestagens, then move on to anti-gestagens as exemplified by the new compound, gestrinone (Roussel - UCLAF, Paris). Preview Unable to display preview. Download preview PDF. Similar content being viewed by others

References

Kistner, R.W. (1958). The use of newer progestins in the treatment of endometriosis. Am. J. Obstet Gynecol., 75, 264–278 Kistner, R.W. (1965). Current status of the hormonal treatment of endometriosis. Clin. Obstet. Gynecol., 9, 271–292 Kistner, R.W. (1959). Treatment of endometriosis by inducing pseudo-pregnancy with ovarian hormones. Fertil. Steril., 10, 539–554 Andrews, M.C., Andrews, W.C. and Strauss, M.D. (1959). Effects of progestin-induced pseudopregnancy on endometriosis: Clinical and microscopic studies. Am. J. Obstet. Gynecol., 78, 776–785 Thomassen, H. and Berthelsen, H.G. (1966). Treatment of endometriosis with progestogens. Dan. Med. Bull., 13, 33–35 Chalmers, J.A. (1962). Treatment of endometriosis with Anovlar. J. Obstet. Gynaecol Br. Commonw., 69, 801–803 Ostergaard, E. (1965). The oral progestational and anti-ovulatory properties of megestrol acetate and its therapeutic use in gynaecological disorders. J. Obstet. Gynaecol Br. Commonw., 72, 45–58 Kourides, I.A. and Kistner, R.W. (1968). Three new synthetic progestins in the treatment of endometriosis. Obstet. Gynecol., 31, 821–828 Thomas, H.H. (1960). Conservative treatment of endometriosis. Use of long-acting ovarian steroid hormones. Obstet. Gynecol., 15, 498–503 Noble, A.D. and Letchworth, A.T. (1979). Medical treatment of endometriosis: a comparative trial. Postgrad. Med. J., 55 (suppl. 5), 37–39 Noble, A.D. and Letchworth, A.T. (1980). Treatment of endometriosis: A study of medical management. Br. J. Obstet. Gynaecol., 87, 726–729 Kistner, R.W. (1965). The effects of new synthetic progestogens on endometriosis in the human female. Fertil. Steril., 16, 61–80 Riva, H.L., Wilson, J.H. and Kawaski, D.M. (1961). Effect of norethynodrel on endometriosis. Am. J. Obstet. Gynecol., 81, 109–118 Lebherz, T.B. and Fobes, CD. (1961). Management of endometriosis with nor-progesterone. Am. J. Obstet. Gynecol., 83, 102–110 Dito, W.R. and Batsakis, J.G. (1961). Norethynodrel-treated endometriosis: A morphologic and histochemical study. Obstet. Gynecol., 18, 1–12 Riva, H.L., Kawaski, D.M. and Messinger, A.J. (1962). Further experience with norethynodrel in treatment of endometriosis. Obstet. Gynecol., 19, 111–117 Williams, B.P.F. (1962). Conservative treatment of endometriosis with progestin therapy. Am. J. Obstet. Gynecol., 83, 715–719 Williams, B.F.P. (1967). Conservative management of endometriosis: Follow-up observations of progestin therapy. Obstet. Gynecol., 30, 76-S2 Soiva, K. and Castren, O. (1963). The conservative treatment of endometriosis with lynestrenol. Ann. Chir. Gynaecol. Venn., 52, 376–382 Soiva, K. and Castren, O. (1964). Clinical observations on the effect of lynestrenol on endometriosis and ovarian function. Int. J. Fertil., 9, 253–255 Timonen, S. and Johansson, C.-J. (1968). Endometriosis treated with lynestrenol. Ann. Chir. Gynaecol. Fenn., 57, 144–147 Mettler, L. (1987). Vergleich der medikamentösen Behandlung der Endometriosis genitalis externa mit Gestrinon, Lynestrenol und Danazol in Rahmen-Stufen-Behandlung. Fertilitat, 3, 133–139 Mettler, L. and Semm, K. (1984). 3-Step therapy of genital endometriosis in cases of human infertility with lynestrenol, danazol or gestrinone administration with the 2nd step. In Raynaud, J.P., Ojasso, T. and Martini, L. (eds.) Medical Management of Endometriosis, pp. 233–247. (New York: Raven Press) Gunning, J.E. and Moyer, D. (1967). The effect of medroxyprogesterone acetate on endometriosis in the human female. Fertil. Steril., 18, 759–774 Moghissi, K.S. and Boyce, C.R. (1976). Management of endometriosis with oral medroxyprogesterone acetate. Obstet. Gynecol., 47, 265–267 Roland, M., Leisten, D. and Kane, R. (1976). Endometriosis therapy with medroxyprogesterone acetate. J. Reprod. Med., 17, 249–252 Luciano, A.A., Turksoy, R.N. and Carleo, J. (1988). Evaluation of oral medroxyprogsterone acetate in the treatment of endometriosis. Obstet. Gynecol., 72, 323–327 American Fertility Society. (1985). Revised American Fertility Society classification for endometriosis. Fertil. Steril., 43, 351–352 Telimmaa, S., Puolakka, J., Ronnberg, L. and Kauppila, A. (1987). Placebo-controlled comparison of danazol and high-dose medroxyprogesterone acetate in the treatment of endometriosis. Gynecol. Endocrinol., 1, 13–23 Aydar, C.K. and Greenblatt, R.B. (1964). 6-Dehydro-retroprogesterone (Duphaston) an interesting progesterone-like compound. Int. J. Fertil., 9, 585–95 Backer, M.H. (1962). Isopregnenone (Duphaston): A new progestational agent. Obstet. Gynecol., 19, 724–729 Johnston, W.I.H. (1976). Dydrogesterone and endometriosis. Br. J. Obstet. Gynaecol., 83, 77–80 Grant, A. (1961). The non-surgical treatment of endometriosis by progestagens. Med. J. Amt., 48, 936–938 Grant, A. (1963). An evaluation of the conservative treatment of endometriosis. Aust. N.Z. Obstet. Gynaecol., 3, 162–167 Evers, J. (1987). The second look laparoscopy for the evaluation of the results of medical treatment of endometriosis should not be performed during ovarian suppression. Fertil. Steril., 47, 502–504 Scott, R.B. and Wharton, L.R. (1957). The effect of estrone and progesterone on the growth of experimental endometriosis in rhesus monkey. Am. J. Obstet. Gynecol., 74, 852–863 Teichmann, A.T., Cremer, P., Wieland, H., Kuhn, W. and Seidel, D. (1988). Lipid metabolic changes during hormonal treatment of endometriosis. Maturitas, 10, 27–33 Sakiz, E. and Azadian-Boulanger, G. (1970). R-2323 — An original contraceptive compound. In Hormonal Steroids. Proceedings of the Third International Congress. Excerpta Medical International Congress Series, No. 219, pp. 865–871 Azadian-Boulanger, G., Secchi, J. and Sakiz, E. (1971). Biological study of the anti-progesterone effect of R2323. In Recent Investigations in Reproduction. Excerpta Medica International Congress Series, No. 278, pp. 129–133 Sakiz, E., Azadian-Boulanger, G. and Raynaud, J.P. (1972). Antiestrogens, antiprogesterones. In Proceedings of the Fourth International Congress of Endocrinology. Excerpta Medica International Congress Series, No. 273, pp. 988–994 Azadian-Boulanger, G., Secchi, J., Laraque, F., Raynaud, J.P. and Sakiz, E. (1976). Action of the midcycle contraceptive (R 2323) on the human endometrium. Am. J. Obstet. Gynecol., 125, 1049–1056 Moguilewsky, M. and Philibert, D. (1984). Dynamics of the receptor interactions of danazol and gestrinone in the rat: Correlation with biological activities. In Raynaud, J-P., Ojasoo, T. and Martini, L. (eds.) Medical Management of Endometriosis, pp. 163–181. (New York: Raven Press) Proulx, L., Labrie, F., Veilleux, R. and Azadian-Boulanger, G. (1984). Actions of progestins and androgens at the hypothalamo-adenohypophyseal level in the female rat. In Raynaud, J-P., Ojasoo, T. and Martini, L. (eds.) Medical Management of Endometriosis, pp. 149–162. (New York: Raven Press) Pugeat, M., Nicolas, B., Tournaire, J. and Forest, M.G. (1984). Interaction of gestrinone with human plasma steroid binding proteins. In Raynaud, J-P., Ojasoo, T. and Martini, L. (eds.) Medical Management of Endometriosis, pp. 183–192. (New York: Raven Press) Kauppila, A., Isomaa, V., Ronnberg, L., Vierikko, P. and Vihko, R. (1985). Effect of gestrinone in endometriosis tissue and endometrium. Fertil. Steril., 44, 466–470 Thomas, E.J. and Cooke, I.D. (1987). The impact of gestrinone upon the course of asymptomatic endometriosis. Br. Med. J., 294, 272–274 Dowsett, M., Attree, S.L., Virdee, S.S. and Jeffcoate, S.L. (1985). Oestrogen-related changes in sex hormone binding globulin levels during normal and gonadotrophin stimulated menstrual cycles. Clin. Endocrinol., 23, 303–312 Dowsett, M., Forbes, K.L., Rose, G.L., Mudge, J.E. and Jeffcoate, S.L. (1986). A comparison of the effects of danazol and gestrinone on testosterone binding to sex hormone binding globulin in vitro and in vivo. Clin. Endocrinol, 24, 555–563 Bergquist, A., Landgren, B-M. and Diczfalusy, E. (1988). Clinical, pharmacokinetic and pharmacodynamic study of three progestagens in the treatment of endometriosis. New Trends Gynaecol. Obstet., 4, 65–84 Venturini, P.L., Fasce, V., Bertolini, S. et al (1989). Endocrine metabolic and clinical effects of gestrinone in women with endometriosis. Fertil. Steril., 52, 589–599 Robyn, C., Delogne-Desnoeck, J., Bourdoux, P. and Copinschi, G. (1984). Endocrine effects of gestrinone. In Raynaud, J-P., Ojasoo, T. and Martini, L. (eds.) Medical Management of Endometriosis, pp. 207–222. (New York: Raven Press) Kitawaki, J., Yamamoto, T. and Okada, H. (1988). Induction of estradiol dehydrogenase activity in human uterine endometrium by synthetic steroids. J. Endocrinol Invest., 11, 351–354 Rose, G.L., White, J.O., Dowsett, M., Mudge, J.E. and Jeffcoate, S.L. (1988). The inhibitory effects of danazol, danazol metabolites, gestrinone and testosterone on the growth of human endometrial cells in vitro. Fertil. Steril., 49, 224–228 Brosens, I.A., Verleyen, A. and Cornillie, F. (1987). The morphologic effect of short-term medical therapy of endometriosis. Am. J. Obstet. Gynecol., 157, 1215–1221 Cornillie, F.J., Brosens, I.A., Vasquez, G. and Riphagen, I. (1986). Histologic and ultrastructural changes in human endometriotic implants treated with the antiprogesterone steroid ethylgestrienone (Gestrinone) during 2 months. Int. J. Gynaecol. Pathol., 5, 95–109 Raynaud, J-P., Salmon, J., Azadian-Boulanger, G., Bucourt, R. and Sakiz, E. (1973). Metabolic studies of R-2323, an original contraceptive compound. In Abstracts, Federation International Pharmac., Stockholm, p. 39 Salmon, J., Cousty, C. and Mouren, M. (1984). Gestrinone pharmacokinetics and metabolism. In Raynaud, J-P., Ojasoo, T. and Martini, L. (eds.) Medical Management of Endometriosis, pp. 103–206. (New York: Raven Press) Hornstein, M.D., Gleason, R.E. and Barbieri, R.L. (1990). A randomised double blind prospective trial of two doses of gestrinone in the treatment of endometriosis. Fertil. Steril., 53, 237–241 Coutinho, E.M. (1982). Treatment of endometriosis with gestrinone (R-2323) a synthetic antiestrogen, antiprogesterone. Am. J. Obstet. Gynecol., 144, 895–898 Coutinho, E.M., Husson, J.M. and Azadian-Boulanger, G. (1984). Treatment of endometriosis with gestrinone — five years experience. In Raynaud, J-P., Ojasoo, T. and Martini, L. (eds.) Medical Management of Endometriosis, pp. 249–261. (New York: Raven Press) Coutinho, E.M. and Azadian-Boulanger, G. (1988). Treatment of endometriosis by vaginal administration of gestrinone. Fertil. Steril., 49, 418–422 Sakiz, E., Azadian-Boulanger, G., Laraque, F. and Raynaud, J.P. (1974). A new approach to estrogen-free contraception based on progesterone receptor blockade by mid-cycle administration of ethyl norgestrienone. Contraception, 10, 467–474 David, S.S., Huggins, G.R., Garcia, C-R. and Busacca, C. (1979). A synthetic steroid (R-2323) as a once a week contraceptive. Fertil. Steril., 31, 278–281 Deltour, G., Azadian-Boulanger, G., Nelson, J. and Sakiz, E. (1984). Tolerance and contraceptive efficacy of gestrinone in 800 patients in the United States from 1974 to 1978. In Raynaud, J-P., Ojasoo, T. and Martini, L. (eds.) Medical Management of Endometriosis, pp. 223–232. (New York: Raven Press) Coutinho, E.M. and Goncalves, M.T. (1989). Long-term treatment of leiomyomas with gestrinone. Fertil. Steril., 51, 939–946 American Fertility Society (1979). Classification of endometriosis. Fertil. Steril., 32, 633 Fedele, L., Bianchi, S., Viezzoli, T., Arcaini, L. and Candiani, G.B. (1989). Gestrinone versus danazol in the treatment of endometriosis. Fertil. Steril., 51, 781–785 Editor information Editors and Affiliations Rights and permissions Copyright information © 1991 Springer Science+Business Media Dordrecht About this chapter Cite this chapter Thomas, E.J., Mettler, L. (1991). Gestogens and anti-gestogens as treatment of endometriosis. In: Thomas, E.J., Rock, J.A. (eds) Modern Approaches to Endometriosis. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-3864-2_12 Download citation DOI: https://doi.org/10.1007/978-94-011-3864-2_12 Publisher Name: Springer, Dordrecht Print ISBN: 978-94-010-5719-6 Online ISBN: 978-94-011-3864-2 eBook Packages: Springer Book Archive

Keywords

- Medroxyprogesterone Acetate - LHRH Analogue - Breakthrough Bleeding - American Fertility Society - Plasma Testosterone Concentration These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Text is read by the "Ask this paper" AI Q&A widget below. Extraction quality varies by source — PMC NXML preserves structure cleanly, OA-HTML may include some navigation residue, and OA-PDF can have broken hyphenation. The publisher copy (via DOI) is the canonical version.

My notes (saved in your browser only)

Ask this paper AI returns verbatim quotes from the full text · source: oa-doi-fallback

Answers must be backed by verbatim quotes from this paper's full text. Hallucinated quotes are dropped automatically; if no verbatim passage answers the question, we say so. How this works

Condition tags

endometriosis

Citation neighborhood

Papers in the corpus that this work cites (lower rings, blue) and that cite this one (upper rings, green). Dot size scales with the paper's in-corpus citation count — bigger dot = more influential within the endo/adeno field. Click a dot to open that paper. [ expand to 2 hops ] — adds papers reached through this work's immediate citers/citees. Heavier; up to 60 extra dots.

References (61)

Cited by (3)

Source provenance

openalex
last seen: 2026-06-10T17:14:06.276822+00:00
unpaywall
last seen: 2026-06-02T02:00:03.124865+00:00
License: CC0 · commercial use OK