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Estetrol – a breath of fresh air on the calm level of contraceptives from the pharmacologist’s point of view


Authors: Jiří Slíva
Authors place of work: Ústav farmakologie, 3. LF UK, Praha
Published in the journal: Ceska Gynekol 2022; 87(5): 372-376
Category: Lékový profil
doi: https://doi.org/10.48095/cccg2022372


Zdroje

1. Hagen A, Barr M, Diczfalusy E. Metabolism of 17b-oestradiol-4-14C in early infancy. Acta Endocrinol (Copenh) 1965; 49 : 207–220.

2. Zucconi G, Lisboa BP, Simonitsch E et al. Isolation of 15-alpha-hydroxy-oestriol from pregnancy urine and from the urine of newborn infants. Acta Endocrinol (Copenh) 1967; 56 (3): 413–423. doi: 10.1530/acta.0.0560413.

3. Schwers J, Eriksson G, Diczfalusy E. Metabolism of oestrone and oestradiol in the human foeto-placental unit at midpregnancy. Acta Endocrinol (Copenh) 1965; 49 : 65–82. doi: 10.1530/acta.0.0490065.

4. Coelingh Bennink F, Holinka CF, Visser M et al. Maternal and fetal estetrol levels during pregnancy. Climacteric 2008; 11 (Suppl 1): 69–72. doi: 10.1080/13697130802056321.

5. Tulchinsky D, Frigoletto FD Jr, Ryan KJ et al. Plasma estetrol as an index of fetal well-being. J Clin Endocrinol Metab 1975; 40 (4): 560–567. doi: 10.1210/jcem-40-4-560.

6. Hammond GL, Hogeveen KN, Visser M et al. Estetrol does not bind sex hormone binding globulin or increase its production by human HepG2 cells. Climacteric 2008; 11 (Suppl 1): 41–46. doi: 10.1080/13697130701851814.

7. Fruzzetti F, Fidecicchi T, Montt Guevara MM et al. Estetrol: a new choice for contraception. J Clin Med 2021; 10 (23): 5625. doi: 10.3390/jcm 10235625.

8. Coelingh Bennink HJ, Skouby S, Bouchard P et al. Ovulation inhibition by estetrol in an in vivo model. Contraception 2008; 77 (3): 186–190. doi: 10.1016/j.contraception.2007.11.014.

9. Visser M, Holinka CF, Coelingh Bennink HJ. First human exposure to exogenous single-dose oral estetrol in early postmenopausal women. Climacteric 2008; 11 (Suppl 1): 31–40. doi: 10.1080/13697130802056511.

10. Duijkers IJ, Klipping C, Zimmerman Y et al. Inhibition of ovulation by administration of estetrol in combination with drospirenone or le­vonorgestrel: results of a phase II dose-finding pilot study. Eur J Contracept Reprod Health Care 2015; 20 (6): 476–489. doi: 10.3109/13625187. 2015.1074675.

11. Apter D, Zimmerman Y, Beekman L e tal. Bleeding pattern and cycle control with estetrol-containing combined oral contraceptives: Results from a phase II, randomised, dose-finding study (FIESTA). Contraception 2016; 94 (4): 366–373. doi: 10.1016/j.contraception.2016.04.015.

12. Apter D, Zimmerman Y, Beekman L et al. Estetrol combined with drospirenone: an oral contraceptive with high acceptability, user satisfaction, well-being and favourable body weight control. Eur J Contracept Reprod Health Care 2017; 22 (4): 260–267. doi: 10.1080/13625187. 2017.1336532.

13. Creinin MD, Westhoff CL, Bouchard C et al. Estetrol-drospirenone combination oral contraceptive: North American phase 3 efficacy and safety results. Contraception 2021; 104 (3): 222–228. doi: 10.1016/j.contraception.2021.05. 002.

14. Gemzell-Danielsson K, Apter D, Zatik J et al. Estetrol-Drospirenone combination oral contraceptive: a clinical study of contraceptive efficacy, bleeding pattern, and safety in Europe and Russia. BJOG 2022; 129 (1): 63–71. doi: 10.1111/1471-0528.16840.

15. Montt-Guevara MM, Palla G, Spina S et al. Regulatory effects of estetrol on the endothelial plasminogen pathway and endothelial cell migration. Maturitas 2017; 99 : 1–9. doi: 10.1016/j.maturitas.2017.02.005.

16. Valéra MC, Noirrit-Esclassan E, Dupuis M et al. Effect of estetrol, a selective nuclear estrogen receptor modulator, in mouse models of arterial and venous thrombosis. Mol Cell Endocrinol 2018; 477 : 132–139. doi: 10.1016/ j.mce.2018.06.010.

17. Kluft C, Zimmerman Y, Mawet M et al. Reduced hemostatic effects with drospirenone-based oral contraceptives containing estetrol vs. ethinyl estradiol. Contraception 2017; 95 (2): 140–147. doi: 10.1016/j.contraception.2016.08.018.

18. Douxfils J, Klipping C, Duijkers I et al. Evaluation of the effect of a new oral contraceptive containing estetrol and drospirenone on hemostasis parameters. Contraception 2020; 102 (6): 396–402. doi: 10.1016/j.contraception.2020.08.015.

19. Creinin MD, Westhoff CL, Bouchard C et al. Estetrol-Drospirenone combination oral contraceptive: North American phase 3 efficacy and safety results. Contraception 2021; 104 (3): 222–228. doi: 10.1016/j.contraception.2021.05.002.

20. Gemzell-Danielsson K, Apter D, Zatik J et al. Estetrol-Drospirenone combination oral contraceptive: a clinical study of contraceptive efficacy, bleeding pattern and safety in Europe and Russia. BJOG 2022; 129 (1): 63–71. doi: 10.1111/1471-0528.16840.

21. Gemzell-Danielsson K, Cagnacci A, Chabbert-Buffet N et al. A novel estetrol-containing combined oral contraceptive: European expert panel review. Eur J Contracept Reprod Health Care. 2022 : 1–11.

22. Coelingh Bennink HJ, Verhoeven C, Zimmerman Y et al. Pharmacokinetics of the fetal estrogen estetrol in a multiple-rising-dose study in postmenopausal women. Climacteric 2017; 20 (3): 285–289. doi: 10.1080/13697137.2017. 1291608.

23. Mawet M, Maillard C, Klipping C et al. Unique effects on hepatic function, lipid metabolism, bone and growth endocrine parameters of estetrol in combined oral contraceptives. Eur J Contracept Reprod Health Care 2015; 20 (6): 463–475. doi: 10.3109/13625187.2015.1068934.

24. Klipping C, Duijkers I, Mawet M et al. Endocrine and metabolic effects of an oral contraceptive containing estetrol and drospirenone. Contraception 2021; 103 (4): 213–221. doi: 10.1016/j.contraception.2021.01.001.

25. Coelingh Bennink HJ, Heegaard AM, Visser M et al. Oral bio­availability and bone-sparing effects of estetrol in an osteoporosis model. Climacteric 2008; 11 (Suppl 1): 2–14. doi: 10.1080/13697130701798692.

26. Coelingh Bennink HJ, Verhoeven C, Zimmerman Y et al. Pharmacodynamic effects of the fetal estrogen estetrol in postmenopausal women: results from a multiple-rising-dose study. Menopause 2017; 24 (6): 677–685. doi: 10.1097/GME.000000000000823.

27. Gallez A, Blacher S, Maquoi E et al. Estetrol combined to progestogen for menopause or contraception indication is neutral on breast cancer. Cancers (Basel) 2021; 13 (10) : 2486. doi: 10.3390/ cancers13102486.

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