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Atamestane

Description of Atamestane: Atamestane is a synthetic steroidal substance with antineoplastic activity. Atamestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:     Intarcia Therapeutics

 Publications related to this agent:

1. Carlsson, Lars; Helgee, Ernst Ahlberg; Boyer, Scott. Interpretation of Nonlinear QSAR Models Applied to Ames Mutagenicity Data. Journal of Chemical Information and Modeling (2009), 49(11), 2551-2558. CODEN: JCISD8 ISSN:1549-9596. CAN 151:522096 AN 2009:1253379

2. Goss, Paul E.; Qi, Shangle; Hu, Haiqing. Comparing the effects of atamestane, toremifene and tamoxifen alone and in combination, on bone, serum lipids and uterus in ovariectomized rats. Journal of Steroid Biochemistry and Molecular Biology (2009), 113(3-5), 233-240. CODEN: JSBBEZ ISSN:0960-0760. CAN 150:487195 AN 2009:284838

3. Sabnis, Gauri J.; Macedo, Luciana; Goloubeva, Olga; Schayowitz, Adam; Zhu, Yue; Brodie, Angela. Toremifene-atamestane; alone or in combination: Predictions from the preclinical intratumoral aromatase model. Journal of Steroid Biochemistry and Molecular Biology (2008), 108(1-2), 1-7. CODEN: JSBBEZ ISSN:0960-0760. CAN 148:509535 AN 2008:158434

4. Goss, Paul; Bondarenko, Igor N.; Manikhas, Georgiy N.; Pendergrass, Kelly B.; Miller, Wilson H., Jr.; Langecker, Peter; Blanchett, Dennis. Phase III, double-blind, controlled trial of atamestane plus toremifene compared with letrozole in postmenopausal women with advanced receptor-positive breast cancer. Journal of Clinical Oncology (2007), 25(31), 4961-4966. CODEN: JCONDN ISSN:0732-183X. CAN 148:182683 AN 2007:1372795

5. Santen, Richard J.; Demers, Lawrence; Ohorodnik, Susan; Settlage, J.; Langecker, Peter; Blanchett, D.; Goss, Paul E.; Wang, Shuping. Superiority of gas chromatography/tandem mass spectrometry assay (GC/MS/MS) for estradiol for monitoring of aromatase inhibitor therapy. Steroids (2007), 72(8), 666-671. CODEN: STEDAM ISSN:0039-128X. CAN 147:314050 AN 2007:716257

6. Goss, Paul E.; Qi, Shangle; Hu, Haiqing; Cheung, Angela M. The effects of atamestane and toremifene alone and in combination compared with letrozole on bone, serum lipids and the uterus in an ovariectomized rat model. Breast Cancer Research and Treatment (2007), 103(3), 293-302. CODEN: BCTRD6 ISSN:0167-6806. CAN 147:378302 AN 2007:647089

7. Muller, Majon; van den Beld, Annewieke W.; van der Schouw, Yvonne T.; Grobbee, Diederick E.; Lamberts, Steven W. J. Effects of dehydroepiandrosterone and atamestane supplementation on frailty in elderly men. Journal of Clinical Endocrinology and Metabolism (2006), 91(10), 3988-3991. CODEN: JCEMAZ ISSN:0021-972X. CAN 145:389621 AN 2006:1100727

8. Khastgir, Jay; Arya, Manit; Shergill, Iqbal S.; Kalsi, Jas S.; Minhas, Sux; Mundy, Anthony R. Current concepts in the pharmacotherapy of benign prostatic hyperplasia. Expert Opinion on Pharmacotherapy (2002), 3(12), 1727-1737. CODEN: EOPHF7 ISSN:1465-6566. CAN 139:206753 AN 2003:8976

9. Steckelbroeck, Stephan; Heidrich, Dagmar D.; Stoffel-Wagner, Birgit; Hans, Volkmar H. J.; Schramm, Johannes; Bidlingmaier, Frank; Klingmuller, Dietrich. Characterization of aromatase cytochrome P450 activity in the human temporal lobe. Journal of Clinical Endocrinology and Metabolism (1999), 84(8), 2795-2801. CODEN: JCEMAZ ISSN:0021-972X. CAN 131:252714 AN 1999:514654

10. Harada, N.; Honda, S-I.; Hatano, O. Aromatase inhibitors and enzyme stability. Endocrine-Related Cancer (1999), 6(2), 211-218. CODEN: ERCAE9 ISSN:1351-0088. CAN 131:223171 AN 1999:408370

11. Harada, N.; Hatano, O. Inhibitors of aromatase prevent degradation of the enzyme in cultured human tumor cells. British Journal of Cancer (1998), 77(4), 567-572. CODEN: BJCAAI ISSN:0007-0920. CAN 129:225346 AN 1998:455986

12. Kelloff, Gary J.; Lubet, Ronald A.; Lieberman, Ronald; Eisenhauer, Karen; Steele, Vernon E.; Crowell, James A.; Hawk, Ernest T.; Boone, Charles W.; Sigman, Caroline C. Aromatase inhibitors as potential cancer chemopreventives. Cancer Epidemiology, Biomarkers & Prevention (1998), 7(1), 65-78. CODEN: CEBPE4 ISSN:1055-9965. CAN 128:212474 AN 1998:93581

13. Radlmaier, Albert; Eickenberg, Hans U.; Fletcher, Matthew S.; Fourcade, Richard O.; Santos, Jose M. Reis; Van Aubel, Olav G. J. M.; Bono, Aldo V. 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. Prostate (New York) (1996), 29(4), 199-208. CODEN: PRSTDS ISSN:0270-4137. CAN 126:1382 AN 1996:696180

14. Reimann, Roland; Kalweit, Sabine; Lang, Rainer. Studies for a genotoxic potential of some endogenous and exogenous sex steroids. II. Communication: examination for the induction of cytogenetic damage using the chromosomal aberration assay on human lymphocytes in vitro and the mouse bone marrow micronucleus test in vivo. Environmental and Molecular Mutagenesis (1996), 28(2), 133-144. CODEN: EMMUEG ISSN:0893-6692. CAN 125:317767 AN 1996:634195

15. Geldof, A. A.; Dijkstra, I.; Newling, D. W. W.; Rao, B. R. Inhibition of 3 -hydroxysteroid dehydrogenase: An approach for prostate cancer treatment? Anticancer Research (1995), 15(4), 1349-54. CODEN: ANTRD4 ISSN:0250-7005. CAN 123:330266 AN 1995:866004

16. Lourdusamy, Mettilda; Labrie, Fernand; Singh, Shankar M. Synthesis of atamestane (SH 489): an aromatase inhibitor. Synthetic Communications (1995), 25(22), 3655-62. CODEN: SYNCAV ISSN:0039-7911. CAN 123:286375 AN 1995:827633

17. Shao, Tsang C.; Marcellj, Marco; Kong, Ann; Cunningham, Glenn R. Anti-androgen effects of the aromatase inhibitor, atamestane. Journal of Andrology (1995), 16(2), 100-7. CODEN: JOAND3 ISSN:0196-3635. CAN 123:74820 AN 1995:645749

18. Guarna, A.; Marrucci, A.; Danza, G.; Serio, M. Relationship between structure and activity of 5 -reductase inhibitors. International Congress Series (1994), 1064(Sex Hormones and Antihormones in Endocrine Dependent Pathology), 93-108. CODEN: EXMDA4 ISSN:0531-5131. CAN 123:102007 AN 1995:423802

19. Kunhz, W.; Hoyer, G.-A.; Backhus, S.; Jakobs, U. Metabolism of the steroidal aromatase inhibitor atamestane in rats, cynomolgus monkeys and humans. Isolation and identification of the major metabolites. European Journal of Drug Metabolism and Pharmacokinetics (1994), 19(2), 137-50. CODEN: EJDPD2 ISSN:0378-7966. CAN 121:291913 AN 1994:691913

20. Benten, W. P. M.; Wunderlich, F.; Herrmann, R.; Kuehn-Velten, W. N. Testosterone-induced compared with estradiol-induced immunosuppression against Plasmodium chabaudi malaria. Journal of Endocrinology (1993), 139(3), 487-94. CODEN: JOENAK ISSN:0022-0795. CAN 120:154124 AN 1994:154124

21. Lang, Rainer; Reimann, Roland. Studies for a genotoxic potential of some endogenous and exogenous sex steroids. I. Communication: Examination for the induction of gene mutations using the Ames Salmonella/microsome test and the HGPRT test in V79 cells. Environmental and Molecular Mutagenesis (1993), 21(3), 272-304. CODEN: EMMUEG ISSN:0893-6692. CAN 119:63431 AN 1993:463431

22. El Etreby, M. Fathy. Atamestane: An aromatase inhibitor for the treatment of benign prostatic hyperplasia. A short review. Journal of Steroid Biochemistry and Molecular Biology (1993), 44(4-6), 565-72. CODEN: JSBBEZ ISSN:0960-0760. CAN 119:41065 AN 1993:441065

23. Schweikert, H. U.; Tunn, U. W.; Habenicht, U. F.; Arnold, J.; Senge, T.; Schulze, H.; Schroder, F. H.; Blom, J. H. M.; Ennemoser, O.; et al. Effects of estrogen deprivation on human benign prostatic hyperplasia. Journal of Steroid Biochemistry and Molecular Biology (1993), 44(4-6), 573-6. CODEN: JSBBEZ ISSN:0960-0760. CAN 119:1231 AN 1993:401231

24. Habenicht, U. F.; Tunn, U. W.; Senge, T.; Schroder, F. H.; Schweikert, H. U.; Bartsch, G.; El Etreby, M. F. Management of benign prostatic hyperplasia with particular emphasis on aromatase inhibitors. Journal of Steroid Biochemistry and Molecular Biology (1993), 44(4-6), 557-63. CODEN: JSBBEZ ISSN:0960-0760. CAN 119:1230 AN 1993:401230

25. Lombardo, Michael E.; Hakky, Said I.; Hudson, Perry B. In vitro studies on the inhibition of testosterone synthesis in the human testis by atamestane. Journal of Steroid Biochemistry and Molecular Biology (1993), 44(3), 287-90. CODEN: JSBBEZ ISSN:0960-0760. CAN 118:225986 AN 1993:225986

26. Kuenzer, H.; Sauer, G.; Wiechert, R. A-Ring aromatic 9,10-secosteroids by radical-induced fragmentation of 3-oxo-1,4-diene derivatives. Tetrahedron Letters (1991), 32(49), 7247-50. CODEN: TELEAY ISSN:0040-4039. CAN 116:59722 AN 1992:59722

27. Zaccheo, Tiziana; Giudici, Donata; Ornati, Giorgio; Panzeri, Achille; Di Salle, Enrico. Comparison of the effects of the irreversible aromatase inhibitor exemestane with atamestane and MDL 18962 in rats with DMBA-induced mammary tumors. European Journal of Cancer (1991), 27(9), 1145-50. CODEN: EJCAEL ISSN:0959-8049. CAN 116:317 AN 1992:317

28. Di Salle, E.; Giudici, D.; Briatico, G.; Ornati, G. Novel irreversible aromatase inhibitors. Annals of the New York Academy of Sciences (1990), 595(Steroid Form., Degrad., Action Peripher. Tissues), 357-67. CODEN: ANYAA9 ISSN:0077-8923. CAN 114:699 AN 1991:699

29. Kuenzer, H.; Stahnke, M.; Sauer, G.; Wiechert, R. Regio- and stereoselective 1,4-reductions of methylated, cross-conjugated steroidal cyclohexadienones. Tetrahedron Letters (1990), 31(27), 3859-62. CODEN: TELEAY ISSN:0040-4039. CAN 113:231761 AN 1990:631761

30. Kuenzer, Hermann; Sauer, Gerhard; Wiechert, Rudolf. Regioselective synthesis of ring A polymethylated steroids in the androstane series. Tetrahedron (1989), 45(20), 6409-26. CODEN: TETRAB ISSN:0040-4020. CAN 113:6667 AN 1990:406667

31. Di Salle, E.; Briatico, G.; Giudici, D.; Ornati, G.; Zaccheo, T. Aromatase inhibition and experimental antitumor activity of FCE 24304, MDL 18962 and SH 489. Journal of Steroid Biochemistry (1989), 34(1-6), 431-4. CODEN: JSTBBK ISSN:0022-4731. CAN 112:171866 AN 1990:171866

32. Nishino, Y.; Schneider, M. R.; Michna, H.; El Etreby, M. F. 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. Journal of Steroid Biochemistry (1989), 34(1-6), 435-7. CODEN: JSTBBK ISSN:0022-4731. CAN 112:152023 AN 1990:152023

33. Lehmann, R. R.; Berges, R.; Richter, K. D.; Senge, T. Effect of the aromatase inhibitor 1-methylandrostadienedione on human BPH tissue after xenotransplantation into thymusaplastic nude mice: a light and an electron microscopic study. Klinische und Experimentelle Urologie (1989), 20(New Aspects Regul. Prostatic Funct.), 104-19. CODEN: KEURDM ISSN:0174-2752. CAN 112:112259 AN 1990:112259

34. Habenicht, Ursula F.; El Etreby, M. Fathy. Selective inhibition of androstenedione-induced prostate growth in intact beagle dogs by a combined treatment with the antiandrogen cyproterone acetate and the aromatase inhibitor 1-methyl-androsta-1,4-diene-3,17-dione (1-methyl-ADD). Prostate (New York, NY, United States) (1989), 14(4), 309-22. CODEN: PRSTDS ISSN:0270-4137. CAN 111:127229 AN 1989:527229

35. Deckers, G. H.; Schuurs, A. H. W. M. Aromatase inhibition in hypophysectomized female rats: a novel animal model for in vivo screening. Journal of Steroid Biochemistry (1989), 32(5), 625-31. CODEN: JSTBBK ISSN:0022-4731. CAN 111:109190 AN 1989:509190

36. Bohl, Martin; Simon, Zeno; Lochmann, Jens Reiner. Theoretical investigations on the role of steroid-skeleton C4 = C5 unsaturation in competitive aromatase inhibition. Zeitschrift fuer Naturforschung, C: Journal of Biosciences (1989), 44(3-4), 217-25. CODEN: ZNCBDA ISSN:0341-0382. CAN 111:50522 AN 1989:450522

37. Schroeder, Helmut; Ziegler, Marianne; El Etreby, M. Fathy. Aromatase-inhibitors of the androstenedione-type activate the 17 -hydroxysteroid-dehydrogenase in the rat testis tissue suspension model. Journal of Steroid Biochemistry (1988), 31(4B), 685-90. CODEN: JSTBBK ISSN:0022-4731. CAN 110:88846 AN 1989:88846

38. Klein, Hartmut; Bartsch, Wilfried; Niemand, Anette; Stuerenburg, Hans Joerg; Voigt, Klaus Dieter. Inhibition of human placental aromatase in a perfusion model. Comparison with kinetic, cell-free experiments. Journal of Steroid Biochemistry (1988), 29(2), 161-9. CODEN: JSTBBK ISSN:0022-4731. CAN 108:198558 AN 1988:198558

39. Aumueller, G.; Habenicht, U. F.; El Etreby, M. F. Pharmacologically induced ultrastructural and immunohistochemical changes in the prostate of the castrated dog. Prostate (New York, NY, United States) (1987), 11(3), 211-18. CODEN: PRSTDS ISSN:0270-4137. CAN 108:49492 AN 1988:49492

40. Habenicht, Ursula F.; El Etreby, M. Fathy. Synergic inhibitory effects of the aromatase inhibitor 1-methyl-androsta-1,4-diene-3,17-dione and the antiandrogen cyproterone acetate on androstenedione-induced hyperplastic effects in the prostates of castrated dogs. Prostate (New York, NY, United States) (1987), 11(2), 133-43. CODEN: PRSTDS ISSN:0270-4137. CAN 108:49482 AN 1988:49482

41. Nishino, Y.; Kerb, U.; Henderson, D. A.; Schillinger, E.; Beier, S.; Wiechert, R.; Neumann, F.; El Etreby, M. F. In vitro and in vivo evaluation of a new selective aromatase inhibitor. International Congress Series (1986), 683(Endocrinology '85), 443-6. CODEN: EXMDA4 ISSN:0531-5131. CAN 106:44161 AN 1987:44161

42. Breiner, M.; Romalo, G.; Schweikert, H. U. Inhibition of androgen receptor binding by natural and synthetic steroids in cultured human genital skin fibroblasts. Klinische Wochenschrift (1986), 64(16), 732-7. CODEN: KLWOAZ ISSN:0023-2173. CAN 105:165312 AN 1986:565312

43. Henderson, D.; Norbisrath, G.; Kerb, U. 1-Methyl-1,4-androstadiene-3,17-dione (SH 489): characterization of an irreversible inhibitor of estrogen biosynthesis. Journal of Steroid Biochemistry (1986), 24(1), 303-6. CODEN: JSTBBK ISSN:0022-4731. CAN 105:18736 AN 1986:418736

44. Ito K; Fukabori Y; Shibata Y; Suzuki K; Mieda M; Gotanda K; Honma S; Yamanaka H Effects of a new steroidal aromatase inhibitor, TZA-2237, and/or chlormadinone acetate on hormone-induced and spontaneous canine benign prostatic hyperplasia. European journal of endocrinology / European Federation of Endocrine Societies (2000), 143(4), 543-54. Journal code: 9423848. ISSN:0804-4643. PubMed ID 11022202 AN 2001019668 MEDLINE (Copyright (C) 2010 U.S. National Library of Medicine on SciFinder (R))

45. Boehm S; Nirnberger G; Ferrari P Estrogen suppression as a pharmacotherapeutic strategy in the medical treatment of benign prostatic hyperplasia: evidence for its efficacy from studies with mepartricin. Wiener klinische Wochenschrift (1998), 110(23), 817-23. Journal code: 21620870R. ISSN:0043-5325. PubMed ID 10025034 AN 1999149173 MEDLINE (Copyright (C) 2010 U.S. National Library of Medicine on SciFinder (R))

46. Pierro E; Andreani C L; Lazzarin N; Cento R; Lanzone A; Caruso A; Mancuso S Further evidence of increased aromatase activity in granulosa luteal cells from polycystic ovary. Human reproduction (Oxford, England) (1997), 12(9), 1890-6. Journal code: 8701199. ISSN:0268-1161. PubMed ID 9363701 AN 1998028331 MEDLINE (Copyright (C) 2010 U.S. National Library of Medicine on SciFinder (R))

47. Ekman P Endocrine therapy for benign prostatic hyperplasia in the 90's. Journal d'urologie (1995), 101(1), 22-5. Journal code: 8006503. ISSN:0248-0018. PubMed ID 7545721 AN 1995404026 MEDLINE (Copyright (C) 2010 U.S. National Library of Medicine on SciFinder (R))

48. Gingell J C; Knonagel H; Kurth K H; Tunn U W 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. The Journal of urology (1995), 154(2 Pt 1), 399-401. Journal code: 0376374. ISSN:0022-5347. PubMed ID 7541854 AN 1995333326 MEDLINE (Copyright (C) 2010 U.S. National Library of Medicine on SciFinder (R))

49. Oesterling J E; el Etreby M F; Gormley G J; Imperato-McGinley J L; Roehrborn C G; Schroder F H; Tunn U W Endocrine therapies for BPH: scientific rationale, clinical results, and patient selection. Progress in clinical and biological research (1994), 386 231-50. Journal code: 7605701. ISSN:0361-7742. PubMed ID 7528391 AN 1995098843 MEDLINE (Copyright (C) 2010 U.S. National Library of Medicine on SciFinder (R))

50. el Etreby M F; Habenicht U F The function and the role of aromatase inhibitors in the treatment of BPH. Progress in clinical and biological research (1994), 386 209-30. Journal code: 7605701. ISSN:0361-7742. PubMed ID 7528389 AN 1995098841 MEDLINE (Copyright (C) 2010 U.S. National Library of Medicine on SciFinder (R))

Patents related to this agents:

1. Wang, Changjin; Wilson, Leland F. Methods and compositions for the treatment of estrogen-dependent hyperproliferative uterine disorders. U.S. Pat. Appl. Publ. (2010), 14pp. CODEN: USXXCO US 2010087402 A1 20100408 CAN 152:422282 AN 2010:442220

2. Dewitt, David M. Preparation of high throughput pharmaceutical nanoparticles. PCT Int. Appl. (2010), 26pp. CODEN: PIXXD2 WO 2010030763 A2 20100318 CAN 152:390074 AN 2010:330249

3. Henteman, Martin F.; Scott, William; Wood, Jill; Johnson, Jeffrey; Redman, Aniko; Bullion, Ann-Marie; Guernon, Leatte. Preparation of sulfonyldihydroimidazoquinazoline derivatives for use as PIK3 inhibitors. PCT Int. Appl. (2009), 133pp. CODEN: PIXXD2 WO 2009091550 A2 20090723 CAN 151:173483 AN 2009:887413

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5. Schwede, Wolfgnag; Moeller, Carsten; Schmidt, Anja; Fuhrmann, Ulrike; Rotgeri, Andrea; Kirkland, Thomas. Preparation of phenylcyclopropanes and related compounds as nonsteroidal progesterone receptor modulators. U.S. Pat. Appl. Publ. (2009), 110 pp. CODEN: USXXCO US 2009099147 A1 20090416 CAN 150:398171 AN 2009:456905

6. Schwede, Wolfgang; Moeller, Carsten; Schmidt, Anja; Fuhrmann, Ulrike; Rotgeri, Andrea; Kirkland, Thomas Andrew; Wyrwa, Ralf. Preparation of 1-benzoxazones and related compounds as nonsteroidal progesterone receptor modulators. U.S. Pat. Appl. Publ. (2009), 145 pp. CODEN: USXXCO US 2009075989 A1 20090319 CAN 150:306681 AN 2009:336276

7. Hoffmann, Jens; Korr, Daniel. Combination of progesterone-receptor antagonist together with an aromatase inhibitor for use in BRCA-mediated diseases. U.S. Pat. Appl. Publ. (2008), 7 pp. CODEN: USXXCO US 2008261929 A1 20081023 CAN 149:478716 AN 2008:1277610

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