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Chemical Compound Review

ATAMESTANE     (8R,9S,10R,13S,14S)-1,10,13- trimethyl-7,8...

Synonyms: Atamestano, Atamestanum, Biomed-777, SureCN59128, CCRIS 6528, ...
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Disease relevance of ATAMESTANE


High impact information on ATAMESTANE

  • Inhibition experiments with atamestane, an inhibitor of aromatase cytochrome P450, revealed specific, dose-responsive, and competitive inhibition of both brain and placental aromatase activities [2].
  • METHODS: Two hundred and ninety-two patients with clinical symptoms of BPH were randomly allocated to one of the following treatments for 48 weeks: placebo or the selective aromatase inhibitor, atamestane, at a daily dose of 100 mg or 300 mg [3].
  • CONCLUSIONS: The conclusion from this study is that the reduction in estrogen concentration using the selective aromatase inhibitor atamestane has no effect on clinically established BPH [3].
  • Comparison of the effects of the irreversible aromatase inhibitor exemestane with atamestane and MDL 18962 in rats with DMBA-induced mammary tumours [4].
  • Anti-androgen effects of the aromatase inhibitor, atamestane [5].

Chemical compound and disease context of ATAMESTANE


Biological context of ATAMESTANE


Anatomical context of ATAMESTANE


Associations of ATAMESTANE with other chemical compounds


Gene context of ATAMESTANE


Analytical, diagnostic and therapeutic context of ATAMESTANE

  • MATERIALS AND METHODS: In a double-blind study 160 patients from 14 centers were randomized between 2 groups to receive either placebo or the aromatase inhibitor atamestane (1-methyl-androsin-1,4 diene-3 17-dione, 400 mg. daily for 48 weeks) [1].
  • In an open multicenter study 49 men (mean age 70.1 years, range 55 to 84) with obstructive BPH were treated with atamestane (3 x 200 mg/day) for 3 months [12].
  • Since recent studies in animal models and in men have shown that estrogens might be causally linked to the onset and maintenance of BPH, we examined the effect of 1-methyl-androsta-1,4-diene-3,17-dione (Atamestane), a newly developed aromatase inhibitor, in men with BPH [12].
  • In this study, the efficacy of atamestane in suppressing tumor growth was evaluated in comparing with that of a non-steroidal aromatase inhibitor (CGS 16949A, Ciba-Geigy) and ovariectomy [10].


  1. Placebo controlled double-blind study to test the efficacy of the aromatase inhibitor atamestane in patients with benign prostatic hyperplasia not requiring operation. The Schering 90.062 Study Group. Gingell, J.C., Knönagel, H., Kurth, K.H., Tunn, U.W. J. Urol. (1995) [Pubmed]
  2. Characterization of aromatase cytochrome P450 activity in the human temporal lobe. Steckelbroeck, S., Heidrich, D.D., Stoffel-Wagner, B., Hans, V.H., Schramm, J., Bidlingmaier, F., Klingmüller, D. J. Clin. Endocrinol. Metab. (1999) [Pubmed]
  3. Estrogen reduction by aromatase inhibition for benign prostatic hyperplasia: results of a double-blind, placebo-controlled, randomized clinical trial using two doses of the aromatase-inhibitor atamestane. Atamestane Study Group. Radlmaier, A., Eickenberg, H.U., Fletcher, M.S., Fourcade, R.O., Reis Santos, J.M., van Aubel, O.G., Bono, A.V. Prostate (1996) [Pubmed]
  4. Comparison of the effects of the irreversible aromatase inhibitor exemestane with atamestane and MDL 18962 in rats with DMBA-induced mammary tumours. Zaccheo, T., Giudici, D., Ornati, G., Panzeri, A., di Salle, E. Eur. J. Cancer (1991) [Pubmed]
  5. Anti-androgen effects of the aromatase inhibitor, atamestane. Shao, T.C., Marcelli, M., Kong, A., Cunningham, G.R. J. Androl. (1995) [Pubmed]
  6. Atamestane, a new aromatase inhibitor for the management of benign prostatic hyperplasia. el Etreby, M.F., Nishino, Y., Habenicht, U.F., Henderson, D. J. Androl. (1991) [Pubmed]
  7. Metabolism of the steroidal aromatase inhibitor atamestane in rats, cynomolgus monkeys and humans. Isolation and identification of the major metabolites. Kuhnz, W., Hoyer, G.A., Backhus, S., Jakobs, U. European journal of drug metabolism and pharmacokinetics. (1994) [Pubmed]
  8. Further evidence of increased aromatase activity in granulosa luteal cells from polycystic ovary. Pierro, E., Andreani, C.L., Lazzarin, N., Cento, R., Lanzone, A., Caruso, A., Mancuso, S. Hum. Reprod. (1997) [Pubmed]
  9. Rationale for using aromatase inhibitors to manage benign prostatic hyperplasia. Experimental studies. Habenicht, U.F., el Etreby, M.F. J. Androl. (1991) [Pubmed]
  10. Antitumor effect of a specific aromatase inhibitor, 1-methyl-androsta-1,4-diene-3,17-dione (atamestane), in female rats bearing DMBA-induced mammary tumors. Nishino, Y., Schneider, M.R., Michna, H., el Etreby, M.F. J. Steroid Biochem. (1989) [Pubmed]
  11. Atamestane: an aromatase inhibitor for the treatment of benign prostatic hyperplasia. A short review. el Etreby, M.F. J. Steroid Biochem. Mol. Biol. (1993) [Pubmed]
  12. Effects of estrogen deprivation on human benign prostatic hyperplasia. Schweikert, H.U., Tunn, U.W., Habenicht, U.F., Arnold, J., Senge, T., Schulze, H., Schröder, F.H., Blom, J.H., Ennemoser, O., Horniger, W. J. Steroid Biochem. Mol. Biol. (1993) [Pubmed]
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