The pharmacology of nomegestrol acetate

Maturitas

Volumn 71, Issue 4, 2012, Pages 345-353

  Ruan, Xiangyan ^a   Seeger, Harald ^b   Mueck, Alfred O ^b  

^a CAPITAL MEDICAL UNIVERSITY   (China)

^b UNIVERSITY HOSPITAL TÜBINGEN   (Germany)

Author keywords

Estradiol; Ethinyl estradiol; Nomegestrol acetate; Pharmacology

Indexed keywords

16ALPHA ETHYL 21 HYDROXY 19 NORPREGN 4 ENE 3,20 DIONE; CHLORMADINONE ACETATE; CYPROTERONE ACETATE; DIENOGEST; DROSPIRENONE; ESTRADIOL; ESTRANE DERIVATIVE; ESTROGEN; ETHINYLESTRADIOL; ETONOGESTREL; GESTAGEN; GESTODENE; LEVONORGESTREL; MEDROXYPROGESTERONE ACETATE; MEGESTROL ACETATE; NOMEGESTROL; NOMEGESTROL ACETATE; NORETHISTERONE; NORGESTIMATE; PREGNANE DERIVATIVE; PROGESTERONE; SPIRONOLACTONE; STEROID RECEPTOR;

ADD ON THERAPY; BLEEDING; CELL PROLIFERATION; CONTRACEPTION; DRUG ABSORPTION; DRUG BINDING; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; ESTROGEN METABOLISM; HEMOSTASIS; HORMONE SUBSTITUTION; HUMAN; MULTIPLE CYCLE TREATMENT; NONHUMAN; PHARMACOLOGY; REVIEW; VENOUS THROMBOEMBOLISM;

ANDROGEN ANTAGONISTS; CONTRACEPTIVES, ORAL; ENDOMETRIUM; ESTROGENS; FEMALE; GONADOTROPINS; HUMANS; MEGESTROL; MENSTRUAL CYCLE; NORPROGESTERONES; OVULATION; PROGESTERONE CONGENERS; PROGESTINS;

EID: 84858071136     PISSN: 03785122     EISSN: 18734111     Source Type: Journal    
DOI: 10.1016/j.maturitas.2012.01.007     Document Type: Review

References (57)

1. R. Sitruk-Ware New progestogens: a review of their effects in perimenopausal and postmenopausal women Drugs Aging 21 2004 865 883 (Pubitemid 39487071)
2. E.M. Coutinho One year contraception with a single subdermal implant containing nomegestrol acetate (Uniplant) Contraception 47 1993 97 105
3. H. Abdel-Aleem, E.S.M. Abol-Oyoun, and M.M. Shaaban The use of nomegestrol acetate subdermal contraceptive implant, Uniplant, during lactation Contraception 54 1996 281-186
4. D.I. Fraser, M.L. Padwick, M.I. Whitehead, J. White, T.A. Ryder, and J. Pryse-Davies The effects of the addition of nomegestrol acetate to postmenopausal oestrogen therapy Maturitas 11 1989 21 34 (Pubitemid 19076762)
5. J. Conard, A. Basdevant, and J.L. Thomas Cardiovascular risk factors and combined estrogen-progestin replacement therapy: a placebo-controlled study with nomegestrol acetate and estradiol Fertil Steril 45 1995 70 74
6. B. Blanc, L. Cravello, M.-C. Micheletti, C. d'Ercole, and M. Zartarian Continuous hormone replacement therapy for menopause combining nomegestrol acetate and gel, patch, or oral estrogen: a comparison of amenorrhea rates Clin Ther 20 1998 901 912 (Pubitemid 28535726)
7. J. Shields-Botella, A.O. Mueck, and H. Seeger Nomegestrol acetate: a progestin that deserves recognition Horm Metab Res 36 2004 257 259 (Pubitemid 38626416)
8. A.O. Mueck, and R. Sitruk-Ware Nomegestrol acetate, a novel progestogen for oral contraception Steroids 76 2011 531 539
9. D. Mansour, C. Verhoeven, and W. Sommer Efficacy and tolerability of a monophasic combined oral contraceptive containing nomegestrol acetate and 17β-oestradiol in a 24/4 regimen, in comparison to an oral contraceptive containing ethinylestradiol and drospirenone in a 21/7 regimen Eur J Contracept Reprod Health Care 16 2011 430 443
10. X. Ruan, H. Seeger, and A.O. Mueck The Pharmacology of dienogest Maturitas 71 2012 337 344
11. F. Fruzzetti, and J. Bitzer Review of clinical experience with estradiol in combined oral contraceptives Contraception 81 2010 8 15
12. A.O. Mueck The long road to the pill with (natural) estradiol Gynaecol Forum 14 2009 3 4
13. R. Sitruk-Ware Pharmacological profile of progestins Maturitas 61 2008 151 157
14. S. Bello Nomegestrol acetate: pharmacology, safety profile and therapeutic efficacy Drugs 70 2010 541 559
15. E. Ezan, H. Benech, and R. Bucourt Enzyme immunoassay for nomegestrol acetate in human plasma J Steroid Biochem Mol Biol 46 1993 507 514 (Pubitemid 23312322)
16. A.E. Schindler, C. Campagnoli, and R. Druckmann Classification and pharmacology of progestins Maturitas 61 2003 171 180
17. I. Duc, J. Botella, R. Delansorne, and J. Paris Interaction of [3H]nomegestrol acetate with cytosolic progesterone receptors from the rat uterus Steroids 56 1991 325 328
18. J. Botella, I. Duc, R. Delansorne, J. Paris, and B. Lahlou Regulation of rat uterine steroid receptors by nomegestrol acetate, a new 19-nor-progesterone derivative J Pharmacol Exp Ther 248 1989 758 761 (Pubitemid 19090251)
19. J. Botella, J. Paris, and B. Lahlou The cellular mechanism of the antiandrogenic action of nomegestrol acetate, a new 19-nor progestagen, on the rat prostate Acta Endocrinol (Copenh) 115 1987 544 550 (Pubitemid 17101084)
20. I. Duc, J. Botella, P. Bonnet, F. Fraboul, R. Delansorne, and J. Paris Antiandrogenic properties of nomegestrol acetate Arzneimittelforschung 45 1995 70 74
21. J. Paris, J. Botella, P. Fournau, P. Bonnet, and R. Thevenot Extinction of mineralocorticoid effects in 19-norprogesterone derivatives: structure-activity relationships J Pharmacol Exp Ther 243 1987 288 291 (Pubitemid 17162730)
22. I.J. Duijkers, C. Klipping, P. Grob, and T. Korver Effects of a monophasic combined oral contraceptive containing nomegestrol acetate and 17β-oestradiol on ovarian function in comparison to a monophasic combined oral contraceptive containing drospirenone and ethinylestradiol Eur J Contracept Reprod Health Care 15 2010 314 325
23. U.M. Agren, M.M. Anttila, and K. Enp-Liukko Effects of a monophasic combined oral contraceptive containing nomegestrol acetate and 17β-oestradiol compared with one containing levonorgestrel and ethinylestradiol on haemostasis, lipids and carbohydrate metabolism Eur J Contracept Reprod Health Care 16 2011 444 457
24. U.M. Agren, M.M. Anttila, and K. Enp-Liukko Effects of a monophasic combined oral contraceptive containing nomegestrol acetate and 17β-oestradiol in comparison to one containing levonorgestrel and ethinylestradiol on markers of endocrine function Eur J Contracept Reprod Health Care 16 2011 458 467
25. P. Gaussem, M. Alhenc-Gelas, and J.L. Thomas Haemostatic effects of a new combined oral contraceptive, nomegestrol acetate/17β-estradiol, compared with those of levonorgestrel/ethinyl estradiol. A double-blind, randomised study Thromb Haemost 105 2011 560 567
26. I.C. Barbosa, H. Maia Jr. , and E. Coutinho Effects of a single Silastic contraceptive implant containing nomegestrol acetate (Uniplant) on endometrial morphology and ovarian function for 1 year Contraception 74 2006 492 497 (Pubitemid 46037538)
27. I. Barbosa, E. Coutinho, C. Athayde, O.A. Ladipo, S.E. Olsson, and U. Ulmsten Effects of a single contraceptive silastic implant containing nomegestrol acetate on ovarian function and cervical mucus production during 2 years Fertil Steril 65 1996 724 729 (Pubitemid 26096909)
28. E. Gurpide, and C. Marks Influence of endometrial 17 beta-hydroxysteroid dehydrogenase activity on the binding of estradiol to receptors J Clin Endocrinol Metab 52 1981 252 255 (Pubitemid 11183620)
29. S. Yang, Z. Fang, and B. Gurates Stromal PRs mediate induction of 17beta-hydroxysteroid dehydrogenase type 2 expression in human endometrial epithelium: a paracrine mechanism for inactivation of E2 Mol Endocrinol 15 2001 2093 2105 (Pubitemid 33141129)
30. J.M. Foidart, A. Beliard, and B. Hedon Impact of percutaneous oestradiol gels in postmenopausal hormone replacement therapy on clinical symptoms and endometrium Br J Obstet Gynaecol 104 1997 305 310 (Pubitemid 27112661)
31. B. Bazin, R. Thevenot, C. Bursaux, and J. Paris Effect of nomegestrol acetate, a new 19-nor-progesterone derivative, on pituitary-ovarian function in women Br J Obstet Gynaecol 94 1987 1199 1204 (Pubitemid 18058561)
32. B. Couzinet, J. Young, and M. Kujas The antigonadotropic activity of a 19-nor-progesterone derivative is exerted both at the hypothalamic and pituitary levels in women J Clin Endocrinol Metab 84 1999 4191 4196 (Pubitemid 30644216)
33. N. Chabbert-Buffet, D. Chassard, E. Ochsenbein, J.L. Thomas, and S. Christin-Maitre Inhibition of ovulation by NOMAC/E2, a novel monophasic oral contraceptive combining nomegestrol acetate and 17β-oestradiol: a double-blind, randomised, dose-finding pilot study Eur J Contracept Reprod Health Care 16 2011 76 84
34. S. Christin-Maitre, C. Sertaty, N.C. Chabbert-Buffet, E. Ochsenbein, C. Chassard, and J.-L. Thomas Comparison of a 24-day and a 21-day pill regimen for the novel combined oral contraceptive, nomegestrol acetate and 17β-estradiol (NOMAC/E2): a double-blind, randomized study Human Reprod 26 2011 1338 1347
35. G.S. Chetrite, J.L. Thomas, J. Shields-Botella, J. Cortes-Prieto, J.C. Philippe, and J.R. Pasqualini Control of sulfatase activity by nomegestrol acetate in normal and cancerous human breast tissues Anticancer Res 25 2005 2827 2830 (Pubitemid 41044668)
36. J. Shields-Botella, G. Chetrite, S. Meschi, and J.R. Pasqualini Effect of nomegestrol acetate on estrogen biosynthesis and transformation in MCF-7 and T47-D breast cancer cells J Steroid Biochem Mol Biol 93 2005 1 13 (Pubitemid 40312728)
37. G.S. Chetrite, and J.R. Pasqualini Nomegestrol acetate is an anti-aromatase agent in human MCF-7aro breast cancer cells Horm Mol Biol Clin Invest 3 2010 417 424
38. A.O. Mueck, and X. Ruan Benefits and risks during HRT - main safety issue breast cancer Horm Mol Biol Clin Invest 5 2011 105 116
39. W.H. Catherino, M.H. Jeng, and V.C. Jordan Norgestrel and gestodene stimulate breast cancer cell growth through an oestrogen receptor mediated mechanism Br J Cancer 67 1993 945 952 (Pubitemid 23147484)
40. J. Botella, E. Duranti, I. Duc, A.M. Cognet, R. Delansorne, and J. Paris Inhibition by nomegestrol acetate and other synthetic progestins on proliferation and progesterone receptor content of T47-D human breast cancer cells J Steroid Biochem Mol Biol 50 1994 41 47 (Pubitemid 24230493)
41. A. Cahill Progesterone receptor membrane component 1: an integrative review J Steroid Biochem Mol Biol 105 2007 16 36
42. H. Neubauer, Y. Yang, and H. Seeger The presence of a membrane-bound progesterone receptor sensitizes the estradiol-induced effect on the proliferation of human breast cancer cells Menopause 18 2011 845 850
43. F.Z. Stanczyk, and Editorial: Can the increase in breast cancer observed in the estrogen plus progestin arm of the Women's Health Initiative trial be explained by progesterone receptor membrane component 1? Menopause 18 2011 833 834
44. Ruan X, Neubauer H, Yang Y, et al. Progestogens and membrane-initiated effects on the proliferation of human breast cancer cells. Climacteric 2012 (in press).
45. A. Basdevant, C. Pelissier, J. Conard, H. Degrelle, T.T. Guyene, and J.L. Thomas Effects of nomegestrol acetate (5 mg/d) on hormonal, metabolic and hemostatic parameters in premenopausal women Contraception 44 1991 599 605
46. P. Dorangeon, J.L. Thomas, H. Choisy, M. Lumbroso, and M.C. Hazard Effects of nomegestrol acetate on carbohydrate metabolism Diabetes Metab 19 1993 441 445 (Pubitemid 24039446)
47. M. Zerr-Fouineau, M. Chataigneau, C. Blot, and V.B. Schini-Kerth Progestins overcome inhibition of platelet aggregation by endothelial cells by down-regulating endothelial NO synthase via glucocorticoid receptors FASEB J 21 2007 265 273 (Pubitemid 46052565)
48. M. Zerr-Fouineau, M. Jourdain, C. Boesch, M. Hecker, C. Bronner, and V.B. Schini-Kerth Certain progestins prevent the enhancing effect of 17β-estradiol on NO-mediated inhibition of platelet aggregation by endothelial cells Arterioscler Thromb Vasc Biol 29 2009 586 593
49. J.K. Williams, E.K. Honore, S.A. Washburn, and T.B. Clarkson Effects of hormone replacement therapy on reactivity of atherosclerotic coronary arteries in cynomolgus monkeys J Am Coll Cardiol 24 1994 1757 1761 (Pubitemid 24369203)
50. J.K. Williams, J.M. Cline, E.K. Honore, R. Delansorne, and J. Paris Coadministration of nomegestrol acetate does not diminish the beneficial effects of estradiol on coronary artery dilator responses in nonhuman primates (Macaca fascicularis) Am J Obstet Gynecol 179 1998 1288 1294 (Pubitemid 28533789)
51. M. Zatarian, T. Chevallier, M.C. Micheletti, C. Leber, and C. Jamin Biological and clinical safety of nomegestrol acetate administered alone then associated in inverse sequence with transdermal estradiol, in women at risk of dyslipoproteinemia type IIa Ann Endocrinol (Paris) 59 1998 411 416 (Pubitemid 29039458)
52. M. Canonico, E. Oger, and G. Plu-Bureau Hormone therapy and venous thromboembolism among postmenopausal women. Impact of the route of estrogen administration and progestogens: the ESTHER Study Circulation 115 2007 840 845 (Pubitemid 46294724)
53. M. Canonico, M. Alhenc-Gelas, G. Plu-Bureau, V. Olie, P.-Y. Scarabin, and [ESTHER Study] Activated protein C resistance among postmenopausal women using transdermal estrogens: importance of the progestogen Menopause 17 2010 1122 1127
54. A.O. Mueck Exogenous hormones, the risk of venous thromboembolism, and activated protein C resistance. Editorial Menopause 17 2010 1099 1103
55. C.A. Mashchak, R.A. Lobo, and R.D. Dozono-Takano Comparison of pharmacodynamic properties of various estrogen formulations Am J Obstet Gynecol 144 1982 511 516
56. H. Kuhl Adverse effects of estrogen treatment: natural vs. synthetic estrogens T.H. Lippert, A.O. Mueck, J. Ginsburg, Sex steroids and the cardiovascular system 1998 Parthenon Publishing New York, London 201 210
57. J. Trussel Contraceptive failure in the United States Contraception 83 2011 397 404