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Chemical Compound Review

Lentaron     (8R,9S,10R,13S,14S)-4- hydroxy-10,13...

Synonyms: SaveCream, formestane, formestano, formestanum, Lentaron(R), ...
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Disease relevance of formestane


High impact information on formestane


Chemical compound and disease context of formestane


Biological context of formestane


Anatomical context of formestane


Associations of formestane with other chemical compounds


Gene context of formestane


Analytical, diagnostic and therapeutic context of formestane

  • Although treatment with 4-hydroxyandrostenedione did not significantly alter the uptake of 3H-androstenedione or 14C-oestrone into breast tissues, in situ formation of 3H-oestrone was only detected in one tumour sample after treatment [31].
  • Formestane has been generally well tolerated in the relatively small clinical trials conducted to date with adverse effects reported in approximately 13% of patients following intramuscular administration [2].
  • Local side effects due to intramuscular injection of formestane were mild and transient [32].
  • Time to treatment failure was 120 days in the formestane arm and 111 days in the MGA arm [4].
  • In a phase II study, 91 women with advanced breast cancer received formestane (Lentaron) 500 mg intramuscularly every 2 weeks for 6 weeks, and then 250 mg every 2 weeks thereafter; all were either postmenopausal or surgically oophorectomized, and most had received previous hormonal treatment and/or chemotherapy [33].


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  8. Expression and mitogenic effect of fibroblast growth factor-9 in human endometriotic implant is regulated by aberrant production of estrogen. Wing, L.Y., Chuang, P.C., Wu, M.H., Chen, H.M., Tsai, S.J. J. Clin. Endocrinol. Metab. (2003) [Pubmed]
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  11. Quality of life in postmenopausal patients with breast cancer after failure of tamoxifen: formestane versus megestrol acetate as second-line hormonal treatment. Swiss Group for Clinical Cancer Research (SAKK). Bernhard, J., Castiglione-Gertsch, M., Schmitz, S.F., Thürlimann, B., Cavalli, F., Morant, R., Fey, M.F., Bonnefoi, H., Goldhirsch, A., Hürny, C. Eur. J. Cancer (1999) [Pubmed]
  12. Anastrozole shows evidence of activity in postmenopausal patients who have responded or stabilised on formestane therapy. Harper-Wynne, C., Coombes, R.C. Eur. J. Cancer (1999) [Pubmed]
  13. Structure-function studies of human aromatase by site-directed mutagenesis: kinetic properties of mutants Pro-308----Phe, Tyr-361----Phe, Tyr-361----Leu, and Phe-406----Arg. Zhou, D.J., Pompon, D., Chen, S.A. Proc. Natl. Acad. Sci. U.S.A. (1991) [Pubmed]
  14. Structure-activity relationships of new A,D-ring modified steroids as aromatase inhibitors: design, synthesis, and biological activity evaluation. Cepa, M.M., Tavares da Silva, E.J., Correia-da-Silva, G., Roleira, F.M., Teixeira, N.A. J. Med. Chem. (2005) [Pubmed]
  15. A multicentre, randomized, pharmacokinetic, endocrine and clinical study to evaluate formestane in breast cancer patients at first relapse: endocrine and clinical results. The Italian Trials in Medical Oncology (I.T.M.O.) group. Bajetta, E., Zilembo, N., Barni, S., Noberasco, C., Martinetti, A., Ferrari, L., Schieppati, G., Buzzoni, R., Jirillo, A., Amichetti, M., D'Aprile, M., Comella, G., Bichisao, E., Bolelli, G.F., Attili, A., Bombardieri, E. Ann. Oncol. (1997) [Pubmed]
  16. Equine cytochrome P450 aromatase exhibits an estrogen 2-hydroxylase activity in vitro. Almadhidi, J., Moslemi, S., Drosdowsky, M.A., Séralini, G.E. J. Steroid Biochem. Mol. Biol. (1996) [Pubmed]
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  18. Brain estradiol content in newborn rats: sex differences, regional heterogeneity, and possible de novo synthesis by the female telencephalon. Amateau, S.K., Alt, J.J., Stamps, C.L., McCarthy, M.M. Endocrinology (2004) [Pubmed]
  19. Gastric parietal cells: potent endocrine role in secreting estrogen as a possible regulator of gastro-hepatic axis. Ueyama, T., Shirasawa, N., Numazawa, M., Yamada, K., Shelangouski, M., Ito, T., Tsuruo, Y. Endocrinology (2002) [Pubmed]
  20. 4-Hydroxyandrostenedione is not an aromatase inhibitor in the neonatal guinea pig. Sumida, C., Gelly, C., Pasqualini, J.R. Biochem. Pharmacol. (1987) [Pubmed]
  21. Comparison of the effect of 4-hydroxy-4-androstene-3,17-dione on aromatase activity in granulosa cells from preovulatory follicles of rats, rabbits, and humans. Koos, R.D., LeMaire, W.J., Hung, T.T., Brodie, A.M. Steroids (1985) [Pubmed]
  22. Angiotensin-II stimulates estradiol secretion from human placental explants through AT1 receptor activation. Kalenga, M.K., De Gasparo, M., Thomas, K., De Hertogh, R. J. Clin. Endocrinol. Metab. (1995) [Pubmed]
  23. Chemopreventive effects of the aromatase inhibitors vorozole (R-83842) and 4-hydroxyandrostenedione in the methylnitrosourea (MNU)-induced mammary tumor model in Sprague-Dawley rats. Lubet, R.A., Steele, V.E., Casebolt, T.L., Eto, I., Kelloff, G.J., Grubbs, C.J. Carcinogenesis (1994) [Pubmed]
  24. Regulation of progesterone formation by human placental cells in culture. Wunsch, D.M., Anderson, L.D., Pepe, G.J., Albrecht, E.D. Endocrinology (1986) [Pubmed]
  25. Aromatase inhibition in the treatment of advanced breast cancer: is there a relationship between potency and clinical efficacy? Sainsbury, R. Br. J. Cancer (2004) [Pubmed]
  26. Formestane: effective therapy in postmenopausal women with advanced breast cancer. Bajetta, E., Zilembo, N., Buzzoni, R., Noberasco, C., Martinetti, A., Ferrari, L., Bartoli, C., Sacchini, V., Attili, A., Lepera, P. Ann. Oncol. (1994) [Pubmed]
  27. Cyclooxygenase-2 directly regulates gene expression of P450 Cyp19 aromatase promoter regions pII, pI.3 and pI.7 and estradiol production in human breast tumor cells. Prosperi, J.R., Robertson, F.M. Prostaglandins Other Lipid Mediat. (2006) [Pubmed]
  28. The aromatase inhibitor, 4-hydroxyandrostenedione, restores immune responses following trauma-hemorrhage in males and decreases mortality from subsequent sepsis. Schneider, C.P., Nickel, E.A., Samy, T.S., Schwacha, M.G., Cioffi, W.G., Bland, K.I., Chaudry, I.H. Shock (2000) [Pubmed]
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  31. In situ oestrone synthesis in normal breast and breast tumour tissues: effect of treatment with 4-hydroxyandrostenedione. Reed, M.J., Owen, A.M., Lai, L.C., Coldham, N.G., Ghilchik, M.W., Shaikh, N.A., James, V.H. Int. J. Cancer (1989) [Pubmed]
  32. Comparison of the selective aromatase inhibitor formestane with tamoxifen as first-line hormonal therapy in postmenopausal women with advanced breast cancer. Pérez Carrión, R., Alberola Candel, V., Calabresi, F., Michel, R.T., Santos, R., Delozier, T., Goss, P., Mauriac, L., Feuilhade, F., Freue, M. Ann. Oncol. (1994) [Pubmed]
  33. Formestane in the treatment of advanced postmenopausal breast cancer. Possinger, K., Jonat, W., Höffken, K. Ann. Oncol. (1994) [Pubmed]
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