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Chemical Compound Review

tibilone     (7R,9S,14S,17S)-17-ethynyl- 17-hydroxy-7,13...

Synonyms: LS-97410, Org OD14, EINECS 227-069-1, Tibolonum [INN-Latin], Tibolona [INN-Spanish], ...
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Disease relevance of tibolone

  • In conclusion, tibolone can be regarded as an alternative to conventional HRT to prevent postmenopausal bone loss [1].
  • We conclude that 16 months of tibolone treatment prevents ovariectomy-induced deterioration of axial and peripheral skeleton and preserves cortical and trabecular bone strength by reducing bone resorption [2].
  • Progestogenic effects of tibolone on human endometrial cancer cells [3].
  • Because nitric oxide (NO) is a key regulator of vascular tone and atherogenesis, we studied its regulation by tibolone and its metabolites on human endothelial cells [4].
  • After adjustment for confounding factors, an increased risk of breast cancer was found for the current use of estrogen only (RR = 1.96; 95% CI = 1.16-3.35), for the combined use of estrogen and progestin (RR = 2.70; 95% CI = 1.96-3.73) and for current users of tibolone (RR = 4.27; 95% CI = 1.74-10.51) compared to the never use of HRT [5].

Psychiatry related information on tibolone

  • Women treated with tibolone report significant reductions in vaginal dryness and dyspareunia, effects that may be secondary to both estrogenic and androgenic actions [6].
  • CONCLUSIONS: Spine BMD increased significantly in response to tibolone irrespective of physical activity participation [7].
  • Maximal isometric strength of knee flexors was determined in 23 of the tibolone group, 26 of the oestrogen group and 12 of the no therapy group [8].
  • Based on the evidence available, the panel proposed a number of subgroups of postmenopausal women with vasomotor symptoms in whom tibolone might have added value; these included women with sexual dysfunction, mood disorders, fibroids and urogenital complaints, as well as those with breast tenderness or high mammographic breast density with EPT use [9].
  • At the end of the 6-month follow-up period, the QoL was better in the tibolone group in the area of mental health [10].

High impact information on tibolone


Chemical compound and disease context of tibolone


Biological context of tibolone

  • To compare the efficacy of conventional oral and transdermal HRT with that of tibolone in the prevention of postmenopausal bone loss, 140 postmenopausal women (age, 52 +/- 0.6 years; median duration of menopause, 3 years) were enrolled in an open 2-year study [1].
  • In a separate group of patients (four pairs + one post biopsy) on concurrent treatment with tibolone, there was no significant increase in the osteon density, cortical porosity, median canal diameter, or the markers of bone formation and resorption [17].
  • The results revealed a steady and equal increase in bone mineral density in both tibolone groups at the bone sites studied [18].
  • The apoptosis network was stimulated by the progestagenic properties of tibolone; in contrast, the estrogenic effect of tibolone suppressed the apoptosis network [19].
  • The objective was to compare the effects of L-HT and tibolone on lipid profile, vasodilation, and factors associated with inflammation and haemostasis [20].

Anatomical context of tibolone


Associations of tibolone with other chemical compounds


Gene context of tibolone


Analytical, diagnostic and therapeutic context of tibolone

  • The groups were tibolone [two doses were used, 0.05 mg/kg (LoTib) and 0.2 mg/kg (HiTib)], CEE (0.042 mg/kg), CEE (0.042 mg/kg) plus MPA (0.167 mg/kg given continuously), and a control group given no treatment for 2 yr [31].
  • Significant differential effects of lower doses of hormone therapy or tibolone on markers of cardiovascular disease in post-menopausal women: a randomized, double-blind, crossover study [20].
  • METHODS AND RESULTS: The OPAL study was a three-arm, randomized, placebo-controlled, double-blind study to determine the effect of tibolone (2.5 mg daily) and of CEE/MPA (0.625/2.5 mg daily) over 3 years on progression of carotid intima-media thickness (CIMT) in 866 healthy post-menopausal women [32].
  • In conclusion, within 2 yr of treatment, tibolone increases bone mass in the spine and prevents bone loss in the forearm in late postmenopausal women determined by densitometry and several biochemical parameters of bone turnover [18].
  • At baseline and after 3 months of tibolone administration (2.5 mg/day), glucose metabolism was evaluated in each subject using both an oral glucose tolerance test (75 g) and the minimal model method of a frequently sampled intravenous glucose tolerance test [23].


  1. Prevention of postmenopausal bone loss using tibolone or conventional peroral or transdermal hormone replacement therapy with 17beta-estradiol and dydrogesterone. Lippuner, K., Haenggi, W., Birkhaeuser, M.H., Casez, J.P., Jaeger, P. J. Bone Miner. Res. (1997) [Pubmed]
  2. Effect of 16 months of treatment with tibolone on bone mass, turnover, and biomechanical quality in mature ovariectomized rats. Ederveen, A.G., Spanjers, C.P., Quaijtaal, J.H., Kloosterboer, H.J. J. Bone Miner. Res. (2001) [Pubmed]
  3. Progestogenic effects of tibolone on human endometrial cancer cells. Blok, L.J., De Ruiter, P.E., Kühne, E.C., Hanekamp, E.E., Grootegoed, J.A., Smid-Koopman, E., Gielen, S.C., De Gooyer, M.E., Kloosterboer, H.J., Burger, C.W. J. Clin. Endocrinol. Metab. (2003) [Pubmed]
  4. Tibolone activates nitric oxide synthesis in human endothelial cells. Simoncini, T., Mannella, P., Fornari, L., Caruso, A., Varone, G., Garibaldi, S., Genazzani, A.R. J. Clin. Endocrinol. Metab. (2004) [Pubmed]
  5. Increased risk of breast cancer following different regimens of hormone replacement therapy frequently used in Europe. Stahlberg, C., Pedersen, A.T., Lynge, E., Andersen, Z.J., Keiding, N., Hundrup, Y.A., Obel, E.B., Ottesen, B. Int. J. Cancer (2004) [Pubmed]
  6. The effects of tibolone on mood and libido. Davis, S.R. Menopause (New York, N.Y.) (2002) [Pubmed]
  7. The influence of physical activity on the response of bone mineral density to 5 years tibolone. Brooke-Wavell, K., Prelevic, G.M., Bartram, C., Ginsburg, J. Maturitas. (2000) [Pubmed]
  8. Effects of physical activity and menopausal hormone replacement therapy on postural stability in postmenopausal women--a cross-sectional study. Brooke-Wavell, K., Prelevic, G.M., Bakridan, C., Ginsburg, J. Maturitas. (2001) [Pubmed]
  9. Tibolone: clinical recommendations and practical guidelines. A report of the International Tibolone Consensus Group. Kenemans, P., Speroff, L. Maturitas. (2005) [Pubmed]
  10. Effects of tibolone on the quality of life, anxiety-depression levels and cognitive functions in natural menopause: an observational follow-up study. Gülseren, L., Kalafat, D., Mandaci, H., Gülseren, S., Camli, L. The Australian & New Zealand journal of obstetrics & gynaecology. (2005) [Pubmed]
  11. Tibolone exerts its protective effect on trabecular bone loss through the estrogen receptor. Ederveen, A.G., Kloosterboer, H.J. J. Bone Miner. Res. (2001) [Pubmed]
  12. Tibolone, a steroid with a tissue-specific hormonal profile, completely prevents ovariectomy-induced bone loss in sexually mature rats. Ederveen, A.G., Kloosterboer, H.J. J. Bone Miner. Res. (1999) [Pubmed]
  13. Tibolone: influence on markers of cardiovascular disease. Bjarnason, N.H., Bjarnason, K., Haarbo, J., Bennink, H.J., Christiansen, C. J. Clin. Endocrinol. Metab. (1997) [Pubmed]
  14. Hormonal environment in the induction of breast cancer in castrated rats using dimethylbenzanthracene: influence of the presence or absence of ovarian activity and of treatment with estradiol, tibolone, and raloxifene. Callejo, J., Cano, A., Medina, M., Villaronga, M., Gonzalez-Bosquet, E., Sabria, J., Lailla, J.M. Menopause (New York, N.Y.) (2005) [Pubmed]
  15. The hormone replacement therapy drug tibolone acts very similar to medroxyprogesterone acetate in an estrogen-and progesterone-responsive endometrial cancer cell line. Hanifi-Moghaddam, P., Sijmons, B., Ott, M.C., van Ijcken, W.F., Nowzari, D., Kuhne, E.C., van der Spek, P., Kloosterboer, H.J., Burger, C.W., Blok, L.J. J. Mol. Endocrinol. (2006) [Pubmed]
  16. Use of leuprolide acetate plus tibolone in the treatment of severe premenstrual syndrome. Di Carlo, C., Palomba, S., Tommaselli, G.A., Guida, M., Di Spiezio Sardo, A., Nappi, C. Fertil. Steril. (2001) [Pubmed]
  17. Cortical remodeling following suppression of endogenous estrogen with analogs of gonadotrophin releasing hormone. Bell, K.L., Loveridge, N., Lindsay, P.C., Lunt, M., Garrahan, N., Compston, J.E., Reeve, J. J. Bone Miner. Res. (1997) [Pubmed]
  18. Tibolone: prevention of bone loss in late postmenopausal women. Bjarnason, N.H., Bjarnason, K., Haarbo, J., Rosenquist, C., Christiansen, C. J. Clin. Endocrinol. Metab. (1996) [Pubmed]
  19. Molecular portrait of the progestagenic and estrogenic actions of tibolone: behavior of cellular networks in response to tibolone. Hanifi-Moghaddam, P., Gielen, S.C., Kloosterboer, H.J., De Gooyer, M.E., Sijbers, A.M., van Gool, A.J., Smid, M., Moorhouse, M., van Wijk, F.H., Burger, C.W., Blok, L.J. J. Clin. Endocrinol. Metab. (2005) [Pubmed]
  20. Significant differential effects of lower doses of hormone therapy or tibolone on markers of cardiovascular disease in post-menopausal women: a randomized, double-blind, crossover study. Koh, K.K., Han, S.H., Shin, M.S., Ahn, J.Y., Lee, Y., Shin, E.K. Eur. Heart J. (2005) [Pubmed]
  21. Tibolone and its metabolites induce antimitogenesis in human coronary artery smooth muscle cells: role of estrogen, progesterone, and androgen receptors. Dubey, R.K., Gillespie, D.G., Grögli, M., Kloosterboer, H.J., Imthurn, B. J. Clin. Endocrinol. Metab. (2004) [Pubmed]
  22. The effect of tibolone on fat mass, fat-free mass, and total body water in postmenopausal women. Meeuwsen, I.B., Samson, M.M., Duursma, S.A., Verhaar, H.J. Endocrinology (2001) [Pubmed]
  23. Effect of tibolone on glucose and lipid metabolism in postmenopausal women. Cagnacci, A., Mallus, E., Tuveri, F., Cirillo, R., Setteneri, A.M., Melis, G.B. J. Clin. Endocrinol. Metab. (1997) [Pubmed]
  24. Clinical evaluation of the Serum CrossLaps One Step ELISA, a new assay measuring the serum concentration of bone-derived degradation products of type I collagen C-telopeptides. Christgau, S., Rosenquist, C., Alexandersen, P., Bjarnason, N.H., Ravn, P., Fledelius, C., Herling, C., Qvist, P., Christiansen, C. Clin. Chem. (1998) [Pubmed]
  25. Effect of estrogen suppression on the mineralization density of iliac crest biopsies in young women as assessed by backscattered electron imaging. Boyde, A., Compston, J.E., Reeve, J., Bell, K.L., Noble, B.S., Jones, S.J., Loveridge, N. Bone (1998) [Pubmed]
  26. Mammographic changes associated with raloxifene and tibolone therapy in postmenopausal women: a prospective study. Christodoulakos, G.E., Lambrinoudaki, I.V., Vourtsi, A.D., Panoulis, K.P., Kelekis, D.A., Creatsas, G.C. Menopause (New York, N.Y.) (2002) [Pubmed]
  27. Tibolone is metabolized by the 3alpha/3beta-hydroxysteroid dehydrogenase activities of the four human isozymes of the aldo-keto reductase 1C subfamily: inversion of stereospecificity with a delta5(10)-3-ketosteroid. Steckelbroeck, S., Jin, Y., Oyesanmi, B., Kloosterboer, H.J., Penning, T.M. Mol. Pharmacol. (2004) [Pubmed]
  28. Effect of tibolone and its metabolites on vascular endothelial growth factor isoforms 121 and 165 and thrombospondin-1 mRNA in Ishikawa cells. Mirkin, S., Mahony, M.C., Archer, D.F. Menopause (New York, N.Y.) (2004) [Pubmed]
  29. Tibolone metabolism in human liver is catalyzed by 3alpha/3beta-hydroxysteroid dehydrogenase activities of the four isoforms of the aldo-keto reductase (AKR)1C subfamily. Steckelbroeck, S., Oyesanmi, B., Jin, Y., Lee, S.H., Kloosterboer, H.J., Penning, T.M. J. Pharmacol. Exp. Ther. (2006) [Pubmed]
  30. Sulfation of tibolone metabolites by human postmenopausal liver and small intestinal sulfotransferases (SULTs). Wang, M., Ebmeier, C.C., Olin, J.R., Anderson, R.J. Steroids (2006) [Pubmed]
  31. A comparison of tibolone and conjugated equine estrogens effects on coronary artery atherosclerosis and bone density of postmenopausal monkeys. Clarkson, T.B., Anthony, M.S., Wagner, J.D. J. Clin. Endocrinol. Metab. (2001) [Pubmed]
  32. The effect of tibolone and continuous combined conjugated equine oestrogens plus medroxyprogesterone acetate on progression of carotid intima-media thickness: the Osteoporosis Prevention and Arterial effects of tiboLone (OPAL) study. Bots, M.L., Evans, G.W., Riley, W., McBride, K.H., Paskett, E.D., Helmond, F.A., Grobbee, D.E. Eur. Heart J. (2006) [Pubmed]
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