Oral bioavailability and bone-sparing effects of estetrol in an osteoporosis model

References

• , et al. Osteoporosis prevention, diagnosis and therapy. NIH Consensus Statement 2000; 17: 1–45
   Google Scholar
• Riggs B L, Khosla S, Melton L J, III. Unitary model for involutional osteoporosis: estrogen deficiency causes both type I and type II osteoporosis in postmenopausal women and contributes to bone loss in aging men. J Bone Min Res 1998; 13: 763–773
   PubMed Web of Science ®Google Scholar
• Bilezikian J P. Sex steroids, mice, and men: when androgens and estrogens get very close to each other. J Bone Min Res 2002; 17: 563–566
   PubMed Web of Science ®Google Scholar
• Slemenda C W, Hui S L, Longcope C, Johnston C C. Sex steroids and bone mass: a study of changes about the time of menopause. J Clin Invest 1987; 80: 1261–1269
   PubMed Web of Science ®Google Scholar
• Harris S, Dawson-Hughes B. Rates of change in bone mineral density of the spine, heel, femoral neck and radius in healthy postmenopausal women. Bone Min 1992; 17: 87–95
   PubMedGoogle Scholar
• Quigley M ET, Martin P L, Burnier A M, Brooks P. Estrogen therapy arrests bone loss in elderly women. Am J Obstet Gynecol 1987; 156: 1516–1523
   PubMed Web of Science ®Google Scholar
• The Writing Group for the PEPI Trial. Effects of hormone therapy on bone mineral density. JAMA 1996; 276: 1389–1396
   PubMed Web of Science ®Google Scholar
• Komulainen M H, Kroger H, Tuppurainen M T, et al. HRT and Vit D in prevention of non-vertebral fractures in postmenopausal women; a 5 year randomized trial. Maturitas 1998; 31: 45–54
   PubMed Web of Science ®Google Scholar
• Lindsay R, Tohme J F. Estrogen treatment of patients with established postmenopausal osteoporosis. Obstet Gynecol 1990; 76: 290–295
   PubMed Web of Science ®Google Scholar
• Lufkin E G, Wahner H W, O'Fallon W M, et al. Treatment of postmenopausal osteoporosis with transdermal estrogen. Ann Intern Med 1992; 117: 1–9
   PubMed Web of Science ®Google Scholar
• The Writing Group for the Women's Health Initiative Investigators. Risks and benefits of estrogen plus progestin in healthy postmenopausal women. JAMA 2002; 288: 321–333
   PubMed Web of Science ®Google Scholar
• The Women's Health Initiative Steering Committee. Effects of conjugated equine estrogen in women with hysterectomy. JAMA 2004; 291: 1701–1712
   PubMed Web of Science ®Google Scholar
• Holinka C F, Karsdal M A, Christiansen C. Bone, cartilage and hormone therapy: established concepts and future scenarios. Climacteric 2007; 10: 270–272
   PubMed Web of Science ®Google Scholar
• Bagger Y Z, Tankó L B, Alexandersen P, et al. Two to three years of hormone replacement treatment in healthy women have long-term preventive effects on bone mass and osteoporotic fractures: the PERF study. Bone 2004; 34: 728–735
   PubMed Web of Science ®Google Scholar
• Bagger Y Z, Tankó L B, Alexandersen P, Qin G, Christiansen C, for the PERF Study Group. Early postmenopausal hormone therapy may prevent cognitive impairment later in life. Menopause 2005; 12: 12–17
   PubMed Web of Science ®Google Scholar
• Alexandersen P, Tankó L B, Bagger Y Z, Qin G, Christiansen C. The long-term impact of 2–3 years of hormone replacement therapy on cardiovascular mortality and atherosclerosis in healthy women. Climacteric 2006; 9: 108–118
   PubMed Web of Science ®Google Scholar
• Hagen A A, Barr M, Diczfalusy E. Metabolism of 17β-oestradiol-4-14C in early infancy. Acta Endocrinol 1965; 49: 207–220
   PubMedGoogle Scholar
• Schwers J, Eriksson G, Wiqvist N, Diczfalusy E. 15α-hydroxylation: a new pathway of estrogen metabolism in the human fetus and newborn. Biochim Biophys Acta 1965; 100: 313–316
   PubMed Web of Science ®Google Scholar
• Schwers J, Govaerts-Videtsky M, Wiqvist N, Diczfalusy E. Metabolism of oestrone sulphate by the previable human foetus. Acta Endocrinol 1965; 50: 597–610
   PubMedGoogle Scholar
• Mancuso S, Benagiano G, Dell'Acqua S, Shapiro M, Wiqvist N, Diczfalusy E. Studies on the metabolism of C-19 steroids in the human foeto-placental unit. Acta Endocrinol 1968; 57: 208–227
   PubMedGoogle Scholar
• Holinka C F, Diczfalusy E, Coelingh Bennink H JT. Estetrol: a unique steroid in human pregnancy. Climacteric 2008; 11(Suppl 1)1
   PubMed Web of Science ®Google Scholar
• Visser M, Foidart J-M, Coelingh Bennink H JT. In vitro effects of estetrol on receptor binding, drug targets and human liver cell metabolism. Climacteric 2008; 11(Suppl 1)64–68
   PubMed Web of Science ®Google Scholar
• Tseng L, Gurpide E. Competition of estetrol and ethinylestradiol with estradiol for nuclear binding in human endometrium. J Steroid Biochem 1976; 7: 817–822
   PubMedGoogle Scholar
• Tseng L, Gurpide E. Heterogeneity of saturable estradiol binding sites in nuclei of human endometrium; estetrol studies. J Steroid Biochem 1978; 9: 1145–1148
   PubMedGoogle Scholar
• Martucci C, Fishman J. Uterine estrogen receptor binding of catecholestrogens and of estetrol (1,3,5(10)-estratriene-3,15α,16α,17β-tetrol). Steroids 1976; 27: 325–333
   PubMed Web of Science ®Google Scholar
• Holinka C F, Gurpide E. In vivo effects of estetrol on the immature rat uterus. Biol Reprod 1979; 20: 242–246
   PubMed Web of Science ®Google Scholar
• Holinka C F, Bressler R S, Zehr D R, Gurpide E. Comparison of effects of estetrol and tamoxifen with those of estriol and estradiol on the immature rat uterus. Biol Reprod 1980; 22: 913–926
   PubMed Web of Science ®Google Scholar
• Jozan S, Kreitmann B, Bayard F. Different effects of oestradiol, oestriol, oestetrol and of oestrone on human breast cancer cells (MCF-7) in long term tissue culture. Acta Endocrinol 1981; 98: 73–80
   PubMedGoogle Scholar
• Heikkilä J. Excretion of 15α-hydroxyestriol and estriol in maternal urine during normal pregnancy. J Steroid Biochem 1971; 2: 83–93
   Google Scholar
• Tulchinsky D, Frigoletto F D, Ryan K J, Fishman J. Plasma estetrol as an index of fetal well-being. J Clin Endocrinol Metab 1975; 40: 560–567
   PubMed Web of Science ®Google Scholar
• Kundu N, Wachs M, Iverson G B, Petersen L P. Comparison of serum unconjugated estriol and estetrol in normal and complicated pregnancies. Obstet Gynecol 1981; 58: 276–281
   PubMed Web of Science ®Google Scholar
• Turner R T, Riggs B L, Spelsberg T C. Skeletal effects of estrogen. Endocr Rev 1994; 15: 275–300
   PubMed Web of Science ®Google Scholar
• Guidelines for the Preclinical and Clinical Evaluation of Agents Used in the Prevention or Treatment of Postmenopausal Osteoporosis. Division of Metabolic and Endocrine Drug Products. US Food and Drug Administration, Washington, DC 1994
   Google Scholar
• Visser M, Holinka C F, Coelingh Bennink H JT. First human exposure to exogenous single-dose oral estetrol in early postmenopausal women. Climacteric 2008; 11(Suppl 1)31–40
   PubMed Web of Science ®Google Scholar
• Vandenput L, Boonen S, Van Herck E, Swinnen J V, Bouillon R, Vanderschueren D. Evidence from the aged orchidectomized male rat model that 17β-estradiol is a more effective bone-sparing and anabolic agent that 5α-dihydrotestosterone. J Bone Miner Res 2002; 17: 2080–2086
   PubMed Web of Science ®Google Scholar
• Heegaard A M, Holinka C F, Kenemans P, Coelingh Bennink H JT. Estrogenic uterovaginal effects of oral estetrol in the modified Allen–Doisy test. Climacteric 2008; 11(Suppl 1)22–8
   PubMed Web of Science ®Google Scholar
• Holinka C F, Brincat M, Coelingh Bennink H JT. Preventive effect of oral estetrol in a menopausal hot flush model. Climacteric 2008; 11(Suppl 1)15–21
   PubMed Web of Science ®Google Scholar
• Coelingh Bennink H JT, Skouby S, Bouchard P, Holinka C F. Ovulation inhibition by estetrol in an in vivo model. Contraception 2008; 77: 186–90
   PubMed Web of Science ®Google Scholar
• Coelingh Bennink H JT, Singer S, Simoncini T. Estetrol, a pregnancy-specific human steroid, prevents and suppresses mammary tumor growth in a rat model. Climacteric 2008; 11(Suppl 1)29
   PubMed Web of Science ®Google Scholar
• Beral V, Banks E, Reeves G. Evidence from randomized trials on long-term effects of hormone replacement therapy. Lancet 2002; 360: 942–944
   PubMed Web of Science ®Google Scholar
• Donovan J M. Physical and metabolic factors in gallstone pathogenesis. Gastroenterol Clin North Am 1999; 28: 75–97
   PubMed Web of Science ®Google Scholar
• Cirillo D J, Wallace R B, Rodabough R J, et al. Effect of estrogen therapy on gallbladder disease. JAMA 2005; 293: 330–339
   PubMed Web of Science ®Google Scholar
• Hammond G, Hogeveen K, Visser M, Coelingh Bennink H JT. Estetrol does not bind sex hormone binding globulin or increase its production by human HepG2 cells. Climacteric 2008; 11(Suppl 1)41–46
   PubMed Web of Science ®Google Scholar
• Fishman J. Fate of 15α-hydroxyestriol-3H in adult man. J Clin Endocrinol 1970; 31: 436–438
   Web of Science ®Google Scholar
• Fishman J, Schut H, Solomon S. Metabolism, production and excretion rates of 15α-hydroxyestriol in late pregnancy. J Clin Endocrinol Metab 1972; 35: 339–344
   PubMed Web of Science ®Google Scholar