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Chemical Compound Review

Arimidex     2-[3-(2-cyanopropan-2-yl)-5- (1,2,4-triazol...

Synonyms: Anastrole, Asiolex, Anastrozol, AstraZeneca, anastrazole, ...
 Boeddinghaus,  Rubagotti,  Puntoni,  Comeri,  Buzzi,  Hills,  Cuzick,  Restuccia,  Dowsett,  Skene,  Liu,  Makovitzky,  Roselli,  Jones,  Macchiarella,  Diaz-Cruz,  Hayes,  Ferraris,  Cella,  Dowsett,  Griffith,  Mylonas,  Boccardo,  Howell,  Hurn,  Sismondi,  Distante,  Howell,  Massidda,  Webster,  Jonat,  Cuzick,  Guglielmini,  Hackett,  Boeddinghaus,  Azab,  Galassi,  Mokbel,  Romeo,  Blohmer,  Adams,  Ashley,  Eastell,  Walsh,  Fini,  Howell,  Ebbs,  Francis,  Ashley,  Di Tonno,  Skene,  Boccardo,  Sharpe,  Scali,  Rinaldini,  Detre,  Jou,  Gerber,  Siragusa,  Amoroso,  Vogel,  Manganelli,  Backeljauw, Massimo Cristofanilli, Vicente Valero, Aroop Mangalik, Melanie Royce, Ian Rabinowitz, Francis P. Arena, Joan F. Kroener, Elizabeth Curcio, Claire Watkins, Sarah Bacus, Elsa M. Cora, Elizabeth Anderson, Patrick J. Magill,  Bertaccini,  Boepple,  Buzdar,  Diamond,  Seminara,  Mesiti,  Cella,  Potenzoni,  Blomqvist,  Selvaggi,  Krause,  Kundt,  Muscas,  Montefiore,  DeCruz,  Walsh,  Dowsett,  Porpiglia,  Alkayed,  Fallowfield,  Battaglia,  Francis,  Reimer,  Amadori,  Fallowfield,  Smith,  Brueggemeier,  Zattoni,  Hannon,  Turner,  Dixon,  Durand,  Barker,  Dixon,  Reiter,  Atanassova,  Janni,  Francis,  Locker,  Crowley,  Benedetto,  Clack,  Plourde,  Plourde,  Conti,  Franchi,  Swanston,  Paladini,  Salter,  Desrochers,  Martorana,  Wolter,  Bercu,  Eiermann,  Locker,  Ebbs,  Smith,  Rubin,  Ingle,  Cuzick,  Rubagotti,  Morley,  
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Disease relevance of Anastrole


Psychiatry related information on Anastrole


High impact information on Anastrole


Chemical compound and disease context of Anastrole


Biological context of Anastrole


Anatomical context of Anastrole


Associations of Anastrole with other chemical compounds


Gene context of Anastrole

  • Dixon plots used to determine the Ki values for the inhibition of CYP1A2 and CYP3A activities by anastrozole were biphasic, indicating additional lower affinity Ki values [33].
  • Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase [33].
  • The anastrozole-induced changes in IGFs and IGFBP-1 appeared to be different in the patients receiving a clinical benefit from those observed in non-responders [34].
  • Furthermore, the preliminary results of the Arimidex, Tamoxifen, Alone and in Combination (ATAC) study have shown that adjuvant anastrozole is superior to tamoxifen in terms of disease-free survival (DFS), non-musculoskeletal adverse effects and prevention of contralateral breast cancer in postmenopausal women with early, ER-positive breast cancer [35].
  • There was a significantly greater suppression of Ki67 in the anastrozole-treated group than in the tamoxifen- or combination-treated groups, which is parallel to the greater efficacy seen for anastrozole over these two treatments in the Arimidex, Tamoxifen, Alone or in Combination adjuvant trial [14].

Analytical, diagnostic and therapeutic context of Anastrole


  1. Questions about anastrozole for early breast cancer. Thornton, H. Lancet (2002) [Pubmed]
  2. Anastrozole, a potent and selective aromatase inhibitor, versus megestrol acetate in postmenopausal women with advanced breast cancer: results of overview analysis of two phase III trials. Arimidex Study Group. Buzdar, A., Jonat, W., Howell, A., Jones, S.E., Blomqvist, C., Vogel, C.L., Eiermann, W., Wolter, J.M., Azab, M., Webster, A., Plourde, P.V. J. Clin. Oncol. (1996) [Pubmed]
  3. Evaluation of tamoxifen and anastrozole in the prevention of gynecomastia and breast pain induced by bicalutamide monotherapy of prostate cancer. Boccardo, F., Rubagotti, A., Battaglia, M., Di Tonno, P., Selvaggi, F.P., Conti, G., Comeri, G., Bertaccini, A., Martorana, G., Galassi, P., Zattoni, F., Macchiarella, A., Siragusa, A., Muscas, G., Durand, F., Potenzoni, D., Manganelli, A., Ferraris, V., Montefiore, F. J. Clin. Oncol. (2005) [Pubmed]
  4. Quality of life of postmenopausal women in the Arimidex, Tamoxifen, Alone or in Combination (ATAC) Adjuvant Breast Cancer Trial. Fallowfield, L., Cella, D., Cuzick, J., Francis, S., Locker, G., Howell, A. J. Clin. Oncol. (2004) [Pubmed]
  5. Safety and efficacy of anastrozole for the treatment of pubertal gynecomastia: a randomized, double-blind, placebo-controlled trial. Plourde, P.V., Reiter, E.O., Jou, H.C., Desrochers, P.E., Rubin, S.D., Bercu, B.B., Diamond, F.B., Backeljauw, P.F. J. Clin. Endocrinol. Metab. (2004) [Pubmed]
  6. A randomised trial comparing two doses of the new selective aromatase inhibitor anastrozole (Arimidex) with megestrol acetate in postmenopausal patients with advanced breast cancer. Jonat, W., Howell, A., Blomqvist, C., Eiermann, W., Winblad, G., Tyrrell, C., Mauriac, L., Roche, H., Lundgren, S., Hellmund, R., Azab, M. Eur. J. Cancer (1996) [Pubmed]
  7. Quality of Life of Postmenopausal Women in the ATAC ("Arimidex", Tamoxifen, Alone or in Combination) Trial after Completion of 5 years' Adjuvant Treatment for Early Breast Cancer. Cella, D., Fallowfield, L., Barker, P., Cuzick, J., Locker, G., Howell, A. Breast Cancer Res. Treat. (2006) [Pubmed]
  8. Anastrozole is cost-effective vs tamoxifen as initial adjuvant therapy in early breast cancer: Canadian perspectives on the ATAC completed-treatment analysis. Rocchi, A., Verma, S. Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer. (2006) [Pubmed]
  9. Aromatase inhibitors in the treatment of breast cancer. Brueggemeier, R.W., Hackett, J.C., Diaz-Cruz, E.S. Endocr. Rev. (2005) [Pubmed]
  10. Anastrozole as a preventive agent in breast cancer. Thornton, H. Lancet (2003) [Pubmed]
  11. Anastrozole alone or in combination with tamoxifen versus tamoxifen alone for adjuvant treatment of postmenopausal women with early breast cancer: first results of the ATAC randomised trial. Baum, M., Budzar, A.U., Cuzick, J., Forbes, J., Houghton, J.H., Klijn, J.G., Sahmoud, T. Lancet (2002) [Pubmed]
  12. Testosterone attenuates expression of vascular cell adhesion molecule-1 by conversion to estradiol by aromatase in endothelial cells: implications in atherosclerosis. Mukherjee, T.K., Dinh, H., Chaudhuri, G., Nathan, L. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  13. Neoadjuvant treatment of postmenopausal breast cancer with anastrozole, tamoxifen, or both in combination: the Immediate Preoperative Anastrozole, Tamoxifen, or Combined with Tamoxifen (IMPACT) multicenter double-blind randomized trial. Smith, I.E., Dowsett, M., Ebbs, S.R., Dixon, J.M., Skene, A., Blohmer, J.U., Ashley, S.E., Francis, S., Boeddinghaus, I., Walsh, G. J. Clin. Oncol. (2005) [Pubmed]
  14. Biomarker changes during neoadjuvant anastrozole, tamoxifen, or the combination: influence of hormonal status and HER-2 in breast cancer--a study from the IMPACT trialists. Dowsett, M., Ebbs, S.R., Dixon, J.M., Skene, A., Griffith, C., Boeddinghaus, I., Salter, J., Detre, S., Hills, M., Ashley, S., Francis, S., Walsh, G., Smith, I.E. J. Clin. Oncol. (2005) [Pubmed]
  15. Influence of letrozole and anastrozole on total body aromatization and plasma estrogen levels in postmenopausal breast cancer patients evaluated in a randomized, cross-over study. Geisler, J., Haynes, B., Anker, G., Dowsett, M., Lønning, P.E. J. Clin. Oncol. (2002) [Pubmed]
  16. Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment. Howell, A., Robertson, J.F., Quaresma Albano, J., Aschermannova, A., Mauriac, L., Kleeberg, U.R., Vergote, I., Erikstein, B., Webster, A., Morris, C. J. Clin. Oncol. (2002) [Pubmed]
  17. Endocrine therapy trials of aromatase inhibitors for breast cancer in the adjuvant and prevention settings. Ingle, J.N. Clin. Cancer Res. (2005) [Pubmed]
  18. Are differences in the available aromatase inhibitors and inactivators significant? Johnson, P.E., Buzdar, A. Clin. Cancer Res. (2001) [Pubmed]
  19. The role of growth factor receptor pathways in human breast cancer cells adapted to long-term estrogen deprivation. Sabnis, G.J., Jelovac, D., Long, B., Brodie, A. Cancer Res. (2005) [Pubmed]
  20. Aromatase inhibitors in human lung cancer therapy. Weinberg, O.K., Marquez-Garban, D.C., Fishbein, M.C., Goodglick, L., Garban, H.J., Dubinett, S.M., Pietras, R.J. Cancer Res. (2005) [Pubmed]
  21. Effect of an aromatase inhibitor on bmd and bone turnover markers: 2-year results of the Anastrozole, Tamoxifen, Alone or in Combination (ATAC) trial (18233230). Eastell, R., Hannon, R.A., Cuzick, J., Dowsett, M., Clack, G., Adams, J.E. J. Bone Miner. Res. (2006) [Pubmed]
  22. Gene expression profiling of breast cancer in relation to estrogen receptor status and estrogen-metabolizing enzymes: clinical implications. Kristensen, V.N., Sørlie, T., Geisler, J., Langerød, A., Yoshimura, N., Kåresen, R., Harada, N., Lønning, P.E., Børresen-Dale, A.L. Clin. Cancer Res. (2005) [Pubmed]
  23. Role of P450 aromatase in sex-specific astrocytic cell death. Liu, M., Hurn, P.D., Roselli, C.E., Alkayed, N.J. J. Cereb. Blood Flow Metab. (2007) [Pubmed]
  24. Anastrozole versus tamoxifen treatment in postmenopausal women with endocrine-responsive breast cancer and tamoxifen-induced endometrial pathology. Gerber, B., Krause, A., Reimer, T., Mylonas, I., Makovitzky, J., Kundt, G., Janni, W. Clin. Cancer Res. (2006) [Pubmed]
  25. Aromatase inhibitors for male infertility. Raman, J.D., Schlegel, P.N. J. Urol. (2002) [Pubmed]
  26. Anastrozole (Arimidex)--an aromatase inhibitor for the adjuvant setting? Buzdar, A.U. Br. J. Cancer (2001) [Pubmed]
  27. Effect of chronic administration of an aromatase inhibitor to adult male rats on pituitary and testicular function and fertility. Turner, K.J., Morley, M., Atanassova, N., Swanston, I.D., Sharpe, R.M. J. Endocrinol. (2000) [Pubmed]
  28. Effects of aromatase inhibition on in vitro follicle and oocyte development analyzed by early preantral mouse follicle culture. Hu, Y., Cortvrindt, R., Smitz, J. Mol. Reprod. Dev. (2002) [Pubmed]
  29. Differential regulation of gonadotropin secretion by testosterone in the human male: absence of a negative feedback effect of testosterone on follicle-stimulating hormone secretion. Hayes, F.J., DeCruz, S., Seminara, S.B., Boepple, P.A., Crowley, W.F. J. Clin. Endocrinol. Metab. (2001) [Pubmed]
  30. The role of aromatase inhibitors in the treatment of metastatic breast cancer. Mouridsen, H., Gershanovich, M. Semin. Oncol. (2003) [Pubmed]
  31. Randomized biomarker trial of anastrozole or low-dose tamoxifen or their combination in subjects with breast intraepithelial neoplasia. Bonanni, B., Serrano, D., Gandini, S., Guerrieri-Gonzaga, A., Johansson, H., Macis, D., Cazzaniga, M., Luini, A., Cassano, E., Oldani, S., Lien, E.A., Pelosi, G., Decensi, A. Clin. Cancer Res. (2009) [Pubmed]
  32. Phase II, randomized trial to compare anastrozole combined with gefitinib or placebo in postmenopausal women with hormone receptor-positive metastatic breast cancer. Cristofanilli, M., Valero, V., Mangalik, A., Royce, M., Rabinowitz, I., Arena, F.P., Kroener, J.F., Curcio, E., Watkins, C., Bacus, S., Cora, E.M., Anderson, E., Magill, P.J. Clin. Cancer Res. (2010) [Pubmed]
  33. Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase. Grimm, S.W., Dyroff, M.C. Drug Metab. Dispos. (1997) [Pubmed]
  34. Short-term effects of anastrozole treatment on insulin-like growth factor system in postmenopausal advanced breast cancer patients. Ferrari, L., Martinetti, A., Zilembo, N., Pozzi, P., Buzzoni, R., La Torre, I., Gattinoni, L., Catena, L., Vitali, M., Celio, L., Seregni, E., Bombardieri, E., Bajetta, E. J. Steroid Biochem. Mol. Biol. (2002) [Pubmed]
  35. Focus on anastrozole and breast cancer. Mokbel, K. Current medical research and opinion. (2003) [Pubmed]
  36. Anastrozole is superior to tamoxifen as first-line therapy for advanced breast cancer in postmenopausal women: results of a North American multicenter randomized trial. Arimidex Study Group. Nabholtz, J.M., Buzdar, A., Pollak, M., Harwin, W., Burton, G., Mangalik, A., Steinberg, M., Webster, A., von Euler, M. J. Clin. Oncol. (2000) [Pubmed]
  37. Switching to anastrozole versus continued tamoxifen treatment of early breast cancer: preliminary results of the Italian Tamoxifen Anastrozole Trial. Boccardo, F., Rubagotti, A., Puntoni, M., Guglielmini, P., Amoroso, D., Fini, A., Paladini, G., Mesiti, M., Romeo, D., Rinaldini, M., Scali, S., Porpiglia, M., Benedetto, C., Restuccia, N., Buzzi, F., Franchi, R., Massidda, B., Distante, V., Amadori, D., Sismondi, P. J. Clin. Oncol. (2005) [Pubmed]
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