Nomegestrol acetate/estradiol hormonal oral contraceptive and breast cancer risk

Anti-Cancer Drugs

Volumn 25, Issue 7, 2014, Pages 745-750

  Del Pup, Lino ^a   Berretta, Massimiliano ^a   Di Francia, Raffaele ^a   Cavaliere, Carla ^b   Di Napoli, Marilena ^b   Facchini, Gaetano ^b   Fiorica, Francesco ^c   Mileto, Mario ^a   Schindler, Adolf E ^d  

^a CENTRO DI RIFERIMENTO ONCOLOGICO   (Italy)

^b NATIONAL CANCER INSTITUTE   (Italy)

^c UNIVERSITY HOSPITAL OF FERRARA   (Italy)

^d Institute for Medical Research and Education Essen   (Germany)

Author keywords

breast cancer; cancer prevention; contraceptives; estradiol; nomegestrol

Indexed keywords

ESTRADIOL; ESTRADIOL PLUS NOMEGESTROL ACETATE; PROGESTERONE; PROGESTERONE RECEPTOR; PROGESTERONE RECEPTOR MEMBRANE COMPONENT 1; UNCLASSIFIED DRUG; MEGESTROL; MEMBRANE PROTEIN; NOMEGESTROL ACETATE; ORAL CONTRACEPTIVE AGENT; PGRMC1 PROTEIN, HUMAN; PREGNANE DERIVATIVE;

ANTIPROLIFERATIVE ACTIVITY; BREAST CANCER; BREAST CANCER CELL LINE; CANCER RISK; DRUG FORMULATION; ESTROGEN SYNTHESIS; HORMONAL CONTRACEPTION; HUMAN; PRIORITY JOURNAL; REVIEW; RISK REDUCTION; BREAST; BREAST NEOPLASMS; CELL PROLIFERATION; CHEMICALLY INDUCED; DRUG EFFECTS; FEMALE; METABOLISM; NEOPLASMS, HORMONE-DEPENDENT; PATHOLOGY; RISK;

BREAST; BREAST NEOPLASMS; CELL PROLIFERATION; CONTRACEPTIVES, ORAL, HORMONAL; ESTRADIOL; FEMALE; HUMANS; MEGESTROL; MEMBRANE PROTEINS; NEOPLASMS, HORMONE-DEPENDENT; NORPREGNADIENES; RECEPTORS, PROGESTERONE; RISK;

EID: 84903815181     PISSN: 09594973     EISSN: 14735741     Source Type: Journal    
DOI: 10.1097/CAD.0000000000000050     Document Type: Review

References (46)

1. Collaborative Group on Hormonal Factors in Breast Cancer. Breast cance r and hormonal contraceptives: collaborative reanalysis of individual data on 53 297 women with breast cancer and 100 239 women without breast cancer from 54 epidemiological studies. Collaborative Group on Hormonal Factors in Breast Cancer. Lancet 199 6; 347: 1713-1727.
2. Marchbanks PA, McDonald JA, Wilson HG, Folger SG, Mandel MG, Daling JR, et al. Oral contraceptives and the risk of breast cancer. N Engl J Med 2002; 346:2025-2032. (Pubitemid 34680593)
3. Vessey M, Painter R. Oral contraceptive use and cancer. Findings in a large cohort study, 1968- 2004. Br J Cancer 2006; 95:385-389. (Pubitemid 44187603)
4. Nelson HD, Zakher B, Cantor A, Fu R, Griffin J, O'Meara ES, et al. Risk factors for breast cancer for women aged 40 to 49 years: a systematic review and meta-analysis. Ann Intern Med 2012; 156:635-648.
5. Zhu H,Lei X,Feng J,Wang Y, Oral contraceptive use and risk of breast cancer: a meta-analysis of prospective cohort studies, Eur J Contracept Reprod Health Care,2012,17,402-4 14.
6. Althuis MD, Brogan DR, Coates RJ, Daling JR, Gammon MD, Malone KE, et al. Hormonal content and potency of oral contraceptives and breast cancer risk among young women. Br J Cancer 2003; 88:50-57. (Pubitemid 36241218)
7. Dumeaux V, Alsaker E, Lund E. Breast cancer and specific types of oral contraceptives: a large Norwegian cohort study. Int J Cancer 2003; 105:844-850. (Pubitemid 36706110)
8. Sitruk-Ware R . Pharmacological profile of progestins. Maturitas 2004; 47:277-283. (Pubitemid 38523308)
9. Ruan X, Seeger H, Mueck AO. The pharmacology of nomegestrol acetate. Maturitas 2012; 71:345-353.
10. Gerrits MG, Schnabel PG, Post TM, Peeters PA. Pharmacokinetic profile of nomegestrol acetate and 17b-estradiol after multiple and single dosing in healthy women. Contraception 2013; 87:193-200.
11. U.S. Food and Drug Administration. Guidance for industry: drug interaction studies-study design, data analysis, implications for dosing, and labeling recommendations. Available at: http://www.fda.gov/downloa ds/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm292362.pdf. [Accessed 18 March 2013].
12. Lello S. Nomegestrol acetate: pharmacology, safety profile and therapeutic efficacy. Drugs 2010; 70:541-559.
13. Merki-Feld GS, Seeger H, Mueck AO. Proliferative effects of estradiol-or ethinylestradiol-P combinations on human breast cancer cells in an intermitted and a long-term regimen. Horm Metab Res 2012; 44:415-421.
14. Duc I, Botella J, Bonnet P, Fraboul F, Delansorne R, Paris J. Antiandrogenic properties of nomegestrol acetate. Arzneimittelforschung 1995; 45:70-74.
15. Shields-Botella J, Duc I, Duranti E, Puccio F, Bonnet P, Delansorne R, et al. An overview of nomegestrol acetate selective receptor binding and lack of estrogenic action on hormone dependent cancer cells. J St eroid Biochem Mol Biol 2003; 87:111-122. (Pubitemid 37532518)
16. Botella J, Duranti E, Duc I, Cognet AM, Delansorne R, Paris J. 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 1994; 50:41-47. (Pubitemid 24230493)
17. Botella J, Duranti E, Viader V, Duc I, Delansorne R, Paris J. Lack of estr ogenic potential of progesterone-or 19-nor-progesterone-derived progestins as opposed to testosterone or 19-nortestosterone derivatives on endometrial Ishikawa cells. J Steroid Biochem Mol Biol 1995; 55:77-84.
18. Catherino WH, Jordan VC. Nomegestrol acetate, a clinically useful 19-norprogesterone derivative which lacks estrogenic activity. J Steroid Biochem Mol Biol 1995; 55:239-246.
19. Cahill MA. Progester one receptor membrane component 1: an integrative review. J Steroid Biochem Mol Biol 2007; 105:16-36. (Pubitemid 47211947)
20. Lyytinen H, Pu kkala E, Ylikorkala O. Breast cancer risk in postmenopausal women using estradiol-P therapy. Obstet Gynecol 2009; 113:65-73.
21. Ruan X, Neubauer H, Yang Y, Schneck H, Schultz S, Fehm T, et al. Progestogens and membrane-initiated effects on the proliferation of human breast cancer cells. Climateric 2012; 15:467-472.
22. Chetrite GS, Thomas JL, Shields-Botella J, Cortes-Pri eto J, Philippe JC, Pasqualini JR. Control of sulfatase activity by nomegestrol acetate in normal and cancerous human breast tissues. Anticancer Res 2005; 25:2827-2830. (Pubitemid 41044668)
23. Chetrite G, Paris J, Botella J, Pasqualini JR. Effect of nomegestrol acetate on estrone-sulfatase and 17beta-hydroxysteroid dehydrogenase activities in human breast cancer cells. J Steroid Biochem Mol Biol 1996; 58:525-531. (Pubitemid 126657498)
24. Chetrite GS, Paris J, Shields-Botella J, Philippe JC, Pasqualini JR. Effect of nomegestrol acetate on human estrogen sulfotransferase activity in the hormone-dependent MCF-7 and T-47D breast cancer cell lines. Anticancer Res 2003; 23:4651-4655. (Pubitemid 38173880)
25. Pasqualini JR, Chetrite GS. Correlation of estrogen sulfotransferase activity and proliferation in normal and carcinomatous human breast: a hypothesis. Anticancer Res 2007; 27:3219-3225. (Pubitemid 47607545)
26. Chetrite GS,Pasqualini J.R. Nomegestrol acetate is an anti-aromatase agent in human MCF-7aro breast cancer cells, Horm Mol Biol Clin Invest,2010, 3, 417-424.
27. Covey DF, Hood WF, McMullan PC. Studies of the inactivation of human placental aromatase by 17 alpha-ethynyl-substituted 10 beta-hydroperoxy and related 19-nor steroids. Biochem Pharmacol 1986; 35:1671-1674. (Pubitemid 16067784)
28. Killinger DW, Perel E, Daniilescu D, Kharlip L, Blackstein ME. Aromatase activity in the breast and other peripheral tissues and its therapeutic regulation. Steroids 1987; 50:523-536.
29. Pasqualini JR, Chetrite G. The anti-aromatase effect of progesterone and of its natural metabolites 20alpha-and 5alpha-dihydroprogesterone in the MCF-7aro breast cancer cell line. Anticancer Res 2008; 28:2129-21 33.
30. Purohit A, Lai LC, Singh A, Coldham NG, Ghilchik MW, Reed MJ, et al. The effect of medroxyprogesterone acetate on aromatase and DNA polymerase alpha activities in breast tumours. J Steroid Bio chem 1989; 34:443-446. (Pubitemid 20061826)
31. Satoh T, Itoh S, Seki T, Nomura N, Yoshizawa I. On the inhibitory action of 29 drugs having side effect gynecomastia on estrogen production. J Steroid Biochem Mol Bi ol 2002; 82:209-216. (Pubitemid 35435369)
32. Li J, Xu LZ, He KL, Guo WJ, Zheng YH, Xia P, et al. Reversal effects of nomegestrol acetate on multidrug resistance in adriamycin-resistant MCF7 breast cancer cell line. Breast Cancer Res 2001; 3:253-263. (Pubitemid 32633348)
33. Agren UM, Anttila M, Mäenpää-Liukko K, Rantala ML, Rautiainen H, Sommer WF, et al. Effects of a monophasic combined oral contraceptive c ontaining nomegestrol acetate and 17b-oestradiol in comparison to one containing levonorgestrel and ethinylestradiol on markers of endocrine function. Eur J Contracept Reprod Health Care 2011; 16:458-467.
34. Simoncini T, Caruso A, Garibaldi S, Fu XD, Giretti MS, Baldacci C, et al. Activation of nitric oxide synthesis in human endothelial cells using nomegestrol acetate. Obstet Gynecol 2006; 108:969-978. (Pubitemid 44498260)
35. Williams JK, Cline JM, Honore EK, Delansorne R, Paris J. Coadministration of nomegestrol acetate does not diminish the beneficial effects of estradiol on coronary artery dilator responses in nonhum an primates (Macaca fascicularis). Am J Obstet Gynecol 1998; 179:1288-1294. (Pubitemid 28533789)
36. Zerr-Fouineau M, Jourdain M, Boesch C, Hecker M, Bronner C, Schini-Kerth VB. Certain progestins prevent the enhancing effect of 17beta-estradiol on NO-mediated inhibition of platelet aggregation by endothelial cells. Arterioscler Thromb Vasc Biol 2009; 29:586-593.
37. Hannaford PC, Selvaraj S, Elliott AM, An gus V, Iversen L, Lee AJ. Cancer risk among users of oral contraceptives: cohort data from the Royal College of General Practitioner's oral contraception study. Br Med J 2007; 335:651.
38. Vessey M, Yeates D, Flynn S. Factors affecting mortality in a large cohort study with special reference to oral contraceptive use. Contraception 2010; 82:221-229.
39. Duijkers IJ, Klipping C, Grob P, Korver T. Effects of a monophasic combined oral contraceptive containing nomegestrol acetate and 17b-oestradiol on ovarian function in comparison to a monophasic combined oral contraceptive containing drospirenone and ethinylestradiol. Eur J C ontracept Reprod Health Care 2010; 15:314-325.
40. Mueck AO, Sitruk-Ware R. Nomegestrol acetate, a novel progestogen for oral contraception. Steroids 2011; 76:531-539.
41. Hilakivi-Clarke L, de Assis S, Warri A. Exposures to synthetic estrogens at different times during the life, and their effect on breast cancer risk. J Mammary Gland Biol Neoplasia 2013; 18:25-42.
42. Shields-Botella J, Chetrite G, Meschia S, Pasqualini JR. Effect of nomegestrol acetate on estrogen biosynthesis and transformation in MCF-7 and T47-D breast cancer cells. J Steroid Biochem Mol Biol 2005; 93:1-1 3. (Pubitemid 40312728)
43. Del Pup L. Management of vaginal dryness and dyspareunia in estrogen sensitive cancer patients. Gynecol Endocrinol 2012; 28:740-745.
44. Del Pup L, Di Francia R, Cavalier e C, Facchini G, Giorda G, Paoli De, et al. Promestriene, a specific topic estrogen. Review of 40 years of vaginal atrophy treatment: is it safe even in cancer patients? Anticancer Drugs 2013; 24:989-998.
45. Del Pup L, Postruznik D, Corona G. Effect of one-month treatment with vaginal promestriene on serum estrone sulfate levels in cancer patients: a pilot study. Maturitas 2012; 72:93-94.
46. Ruan X, Schneck H, Schultz S, Fehm T, Cahill MA, Seeger H, et al. Nomegestrol acetate sequentially or continuously combined to estradiol did not negatively affect membrane-receptor associated progestogenic effects in hu man breast cancer cells. Gynecol Endocrinol 2012; 28:863- 866.