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Volumn 76, Issue 11, 2016, Pages 3307-3318

AZD9496: An oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1-mutant breast tumors in preclinical models

Author keywords

[No Author keywords available]

Indexed keywords

AZD 9496; ESTROGEN RECEPTOR ANTAGONIST; FULVESTRANT; PROGESTERONE RECEPTOR; UNCLASSIFIED DRUG; AZD9496; CINNAMIC ACID DERIVATIVE; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR ALPHA, HUMAN; INDOLE DERIVATIVE; SELECTIVE ESTROGEN RECEPTOR MODULATOR;

EID: 84975060972     PISSN: 00085472     EISSN: 15387445     Source Type: Journal    
DOI: 10.1158/0008-5472.CAN-15-2357     Document Type: Article
Times cited : (148)

References (49)
  • 1
    • 85181122894 scopus 로고    scopus 로고
    • Relevance of breast cancer hormone receptors and other factors to the efficacy of adjuvant tamoxifen: Patient-level meta-analysis of randomised trials
    • Early Breast Cancer Trialists' Collaborative Group (EBCTCG), Davies C, Godwin J, Gray R, Clarke M, Cutter D, et al. Relevance of breast cancer hormone receptors and other factors to the efficacy of adjuvant tamoxifen: patient-level meta-analysis of randomised trials. Lancet 2011;378:771-84.
    • (2011) Lancet , vol.378 , pp. 771-784
    • Davies, C.1    Godwin, J.2    Gray, R.3    Clarke, M.4    Cutter, D.5
  • 2
    • 78649603622 scopus 로고    scopus 로고
    • Effect of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: 10-Year analysis of the ATAC trial
    • Cuzick J, Sestak I, Baum M, Buzdar A, Howell A, Dowsett M, et al. Effect of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: 10-year analysis of the ATAC trial. Lancet Oncol 2010;11:1135-41.
    • (2010) Lancet Oncol , vol.11 , pp. 1135-1141
    • Cuzick, J.1    Sestak, I.2    Baum, M.3    Buzdar, A.4    Howell, A.5    Dowsett, M.6
  • 4
    • 77957673898 scopus 로고    scopus 로고
    • Growth factor stimulation induces a distinct ER(alpha) cistrome underlying breast cancer endocrine resistance
    • Lupien M, Meyer CA, Bailey ST, Eeckhoute J, Cook J, Westerling T, et al. Growth factor stimulation induces a distinct ER(alpha) cistrome underlying breast cancer endocrine resistance. Genes Dev 2010;24:2219-27.
    • (2010) Genes Dev , vol.24 , pp. 2219-2227
    • Lupien, M.1    Meyer, C.A.2    Bailey, S.T.3    Eeckhoute, J.4    Cook, J.5    Westerling, T.6
  • 5
    • 33846869263 scopus 로고    scopus 로고
    • Resistance to endocrine therapy in breast cancer: Exploiting estrogen receptor/growth factor signaling crosstalk
    • Massarweh S, Schiff R. Resistance to endocrine therapy in breast cancer: exploiting estrogen receptor/growth factor signaling crosstalk. Endocr Relat Cancer 2006;13Suppl 1:S15-24.
    • (2006) Endocr Relat Cancer , vol.13 , pp. S15-S24
    • Massarweh, S.1    Schiff, R.2
  • 6
    • 0036488531 scopus 로고    scopus 로고
    • Endocrine-responsive breast cancer and strategies for combating resistance
    • Ali S, Coombes RC. Endocrine-responsive breast cancer and strategies for combating resistance. Nat Rev Cancer 2002;2:101-12.
    • (2002) Nat Rev Cancer , vol.2 , pp. 101-112
    • Ali, S.1    Coombes, R.C.2
  • 8
    • 84860322213 scopus 로고    scopus 로고
    • Dose-dependent change in biomarkers during neoadjuvant endocrine therapy with fulvestrant: Results from NEWEST, a randomized Phase II study
    • Kuter I, Gee JM, Hegg R, Singer CF, Badwe RA, Lowe ES, et al. Dose-dependent change in biomarkers during neoadjuvant endocrine therapy with fulvestrant: results from NEWEST, a randomized Phase II study. Breast Cancer Res Treat 2012;133:237-46.
    • (2012) Breast Cancer Res Treat , vol.133 , pp. 237-246
    • Kuter, I.1    Gee, J.M.2    Hegg, R.3    Singer, C.F.4    Badwe, R.A.5    Lowe, E.S.6
  • 10
    • 1842633460 scopus 로고    scopus 로고
    • Fulvestrant: Pharmacokinetics and pharmacology
    • Robertson JF, Harrison M. Fulvestrant: pharmacokinetics and pharmacology. Br J Cancer 2004;90Suppl 1:S7-10.
    • (2004) Br J Cancer , vol.90 , pp. S7-S10
    • Robertson, J.F.1    Harrison, M.2
  • 11
    • 80052736785 scopus 로고    scopus 로고
    • Fulvestrant revisited: Efficacy andsafetyof the 500-mg dose
    • Howell A, Sapunar F. Fulvestrant revisited: efficacy andsafetyof the 500-mg dose. Clin Breast Cancer 2011;11:204-10.
    • (2011) Clin Breast Cancer , vol.11 , pp. 204-210
    • Howell, A.1    Sapunar, F.2
  • 12
    • 34548241775 scopus 로고    scopus 로고
    • Fulvestrant (Faslodex) - How to make a good drug better
    • Robertson JF. Fulvestrant (Faslodex) - how to make a good drug better. Oncologist 2007;12:774-84.
    • (2007) Oncologist , vol.12 , pp. 774-784
    • Robertson, J.F.1
  • 13
    • 84884559238 scopus 로고    scopus 로고
    • Endocrine-therapy-resistant ESR1 variants revealed by genomic characterization of breastcancer-derived xenografts
    • Li S, Shen D, Shao J, Crowder R, Liu W, Prat A, et al. Endocrine-therapy-resistant ESR1 variants revealed by genomic characterization of breastcancer-derived xenografts. Cell Rep 2013;4:1116-30.
    • (2013) Cell Rep , vol.4 , pp. 1116-1130
    • Li, S.1    Shen, D.2    Shao, J.3    Crowder, R.4    Liu, W.5    Prat, A.6
  • 14
    • 84888391516 scopus 로고    scopus 로고
    • ESR1 ligand-binding domain mutations in hormone-resistant breast cancer
    • Toy W, Shen Y, Won H, Green B, Sakr RA, Will M, et al. ESR1 ligand-binding domain mutations in hormone-resistant breast cancer. Nat Genet 2013;45:1439-45.
    • (2013) Nat Genet , vol.45 , pp. 1439-1445
    • Toy, W.1    Shen, Y.2    Won, H.3    Green, B.4    Sakr, R.A.5    Will, M.6
  • 15
    • 84898717745 scopus 로고    scopus 로고
    • Emergence of constitutively active estrogen receptor-alpha mutations in pretreated advanced estrogen receptor-positive breast cancer
    • Jeselsohn R, Yelensky R, Buchwalter G, Frampton G, Meric-Bernstam F, Gonzalez-Angulo AM, et al. Emergence of constitutively active estrogen receptor-alpha mutations in pretreated advanced estrogen receptor-positive breast cancer. Clin Cancer Res 2014;20:1757-67.
    • (2014) Clin Cancer Res , vol.20 , pp. 1757-1767
    • Jeselsohn, R.1    Yelensky, R.2    Buchwalter, G.3    Frampton, G.4    Meric-Bernstam, F.5    Gonzalez-Angulo, A.M.6
  • 16
    • 0028263517 scopus 로고
    • 3-[4-(1,2-Diphenylbut-1-enyl)phenyl]acrylic acid: A non-steroidal estrogen with functional selectivity for bone over uterus in rats
    • Willson TM, Henke BR, Momtahen TM, Charifson PS, Batchelor KW, Lubahn DB, et al. 3-[4-(1,2-Diphenylbut-1-enyl)phenyl]acrylic acid: a non-steroidal estrogen with functional selectivity for bone over uterus in rats. J Med Chem 1994;37:1550-2.
    • (1994) J Med Chem , vol.37 , pp. 1550-1552
    • Willson, T.M.1    Henke, B.R.2    Momtahen, T.M.3    Charifson, P.S.4    Batchelor, K.W.5    Lubahn, D.B.6
  • 17
    • 10744226748 scopus 로고    scopus 로고
    • Characterization of new estrogen receptor destabilizing compounds: Effects on estrogen-sensitive and tamoxifen-resistant breast cancer
    • Hoffmann J, Bohlmann R, Heinrich N, Hofmeister H, Kroll J, Kunzer H, et al. Characterization of new estrogen receptor destabilizing compounds: effects on estrogen-sensitive and tamoxifen-resistant breast cancer. J Natl Cancer Inst 2004;96:210-8.
    • (2004) J Natl Cancer Inst , vol.96 , pp. 210-218
    • Hoffmann, J.1    Bohlmann, R.2    Heinrich, N.3    Hofmeister, H.4    Kroll, J.5    Kunzer, H.6
  • 19
    • 78650611572 scopus 로고    scopus 로고
    • Anti-breast cancer potential of SS5020, a novel benzopyran antiestrogen
    • Suzuki N, Liu X, Laxmi YR, Okamoto K, Kim HJ, Zhang G, et al. Anti-breast cancer potential of SS5020, a novel benzopyran antiestrogen. Int J Cancer 2011;128:974-82.
    • (2011) Int J Cancer , vol.128 , pp. 974-982
    • Suzuki, N.1    Liu, X.2    Laxmi, Y.R.3    Okamoto, K.4    Kim, H.J.5    Zhang, G.6
  • 20
    • 84933059419 scopus 로고    scopus 로고
    • Identification of GDC-0810 (ARN-810), an orally bioavailable Selective Estrogen Receptor Degrader (SERD) that demonstrates robust activity in tamoxifen-resistant breast cancer xenografts
    • Lai A, Kahraman M, Govek S, Nagasawa J, Bonnefous C, Julien J, et al. Identification of GDC-0810 (ARN-810), an orally bioavailable Selective Estrogen Receptor Degrader (SERD) that demonstrates robust activity in tamoxifen-resistant breast cancer xenografts. J Med Chem 2015;58:4888-904.
    • (2015) J Med Chem , vol.58 , pp. 4888-4904
    • Lai, A.1    Kahraman, M.2    Govek, S.3    Nagasawa, J.4    Bonnefous, C.5    Julien, J.6
  • 21
    • 84940933249 scopus 로고    scopus 로고
    • RAD1901: A novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumour activity in breast cancer xenograft models
    • Garner F, Shomali M, Paquin D, Lyttle R, Hattersley G. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumour activity in breast cancer xenograft models. Anti-Cancer Drugs 2015;26:948-956.
    • (2015) Anti-Cancer Drugs , vol.26 , pp. 948-956
    • Garner, F.1    Shomali, M.2    Paquin, D.3    Lyttle, R.4    Hattersley, G.5
  • 22
    • 79953311521 scopus 로고    scopus 로고
    • A gene expression signature from human breast cancer cells with acquired hormone independence identifies MYC as a mediator of antiestrogen resistance
    • Miller TW, Balko JM, Ghazoui Z, Dunbier A, Anderson H, Dowsett M, et al. A gene expression signature from human breast cancer cells with acquired hormone independence identifies MYC as a mediator of antiestrogen resistance. Clin Cancer Res 2011;17:2024-34.
    • (2011) Clin Cancer Res , vol.17 , pp. 2024-2034
    • Miller, T.W.1    Balko, J.M.2    Ghazoui, Z.3    Dunbier, A.4    Anderson, H.5    Dowsett, M.6
  • 23
    • 84931301519 scopus 로고    scopus 로고
    • A screening assay cascade to identify and characterize novel selective estrogen receptor downregulators (SERDs)
    • Callis R, Rabow A, Tonge M, Bradbury R, Challinor M, Roberts K, et al. A screening assay cascade to identify and characterize novel selective estrogen receptor downregulators (SERDs). J Biomol Screen 2015;20:748-59.
    • (2015) J Biomol Screen , vol.20 , pp. 748-759
    • Callis, R.1    Rabow, A.2    Tonge, M.3    Bradbury, R.4    Challinor, M.5    Roberts, K.6
  • 24
    • 84928485170 scopus 로고    scopus 로고
    • Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic acids as oral selective estrogen receptor down-regulators
    • Degorce SL, Bailey A, Callis R, De Savi C, Ducray R, Lamont G, et al. Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic acids as oral selective estrogen receptor down-regulators. J Med Chem 2015;58:3522-33.
    • (2015) J Med Chem , vol.58 , pp. 3522-3533
    • Degorce, S.L.1    Bailey, A.2    Callis, R.3    De Savi, C.4    Ducray, R.5    Lamont, G.6
  • 27
  • 28
    • 0035788101 scopus 로고    scopus 로고
    • Implementation of molecular replacement in AMoRe
    • Navaza J. Implementation of molecular replacement in AMoRe. Acta Crystallogr D Biol Crystallogr 2001;57:1367-72.
    • (2001) Acta Crystallogr D Biol Crystallogr , vol.57 , pp. 1367-1372
    • Navaza, J.1
  • 30
    • 34247396011 scopus 로고    scopus 로고
    • A practical recipe for stable isotope labeling by amino acids in cell culture (SILAC)
    • Ong S, Mann M. A practical recipe for stable isotope labeling by amino acids in cell culture (SILAC). Nat Protoc 2007;1:2650-60.
    • (2007) Nat Protoc , vol.1 , pp. 2650-2660
    • Ong, S.1    Mann, M.2
  • 31
    • 0021091890 scopus 로고
    • Comparison of the biological effects of tamoxifen and a new antioestrogen (LY 117018) on the immature rat uterus
    • Wakeling AE, O'Connor KM, Newboult E. Comparison of the biological effects of tamoxifen and a new antioestrogen (LY 117018) on the immature rat uterus. J Endocrinol 1983;99:447-53.
    • (1983) J Endocrinol , vol.99 , pp. 447-453
    • Wakeling, A.E.1    O'Connor, K.M.2    Newboult, E.3
  • 32
    • 84945381593 scopus 로고    scopus 로고
    • Optimization of a novel binding motif to (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic acid (AZD9496), a potent and orally bioavailable selective estrogen receptor downregulator and antagonist
    • Bradbury R, De Savi C, Rabow A, Norman R, de Almeida C, Andrews D. Optimization of a novel binding motif to (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic acid (AZD9496), a potent and orally bioavailable selective estrogen receptor downregulator and antagonist. J Med Chem 2015;58:8128-40.
    • (2015) J Med Chem , vol.58 , pp. 8128-8140
    • Bradbury, R.1    De Savi, C.2    Rabow, A.3    Norman, R.4    De Almeida, C.5    Andrews, D.6
  • 33
  • 34
    • 0018138071 scopus 로고
    • Estrogen control of progesterone receptor in human breast cancer. Correlation with nuclear processing of estrogen receptor
    • Horwitz KB, McGuire WL. Estrogen control of progesterone receptor in human breast cancer. Correlation with nuclear processing of estrogen receptor. J Biol Chem 1978;253:2223-8.
    • (1978) J Biol Chem , vol.253 , pp. 2223-2228
    • Horwitz, K.B.1    McGuire, W.L.2
  • 36
    • 0033198735 scopus 로고    scopus 로고
    • Structure of the ligand-binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist
    • Pike AC, Brzozowski AM, Hubbard RE, Bonn T, Thorsell AG, Engstrom O, et al. Structure of the ligand-binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist. EMBO J 1999;18:4608-18.
    • (1999) EMBO J , vol.18 , pp. 4608-4618
    • Pike, A.C.1    Brzozowski, A.M.2    Hubbard, R.E.3    Bonn, T.4    Thorsell, A.G.5    Engstrom, O.6
  • 38
    • 0033638393 scopus 로고    scopus 로고
    • The 26S proteasome is required for estrogen receptor-alpha and coactivator turnover and for efficient estrogen receptor-alpha transactivation
    • Lonard DM, Nawaz Z, Smith CL, O'Malley BW. The 26S proteasome is required for estrogen receptor-alpha and coactivator turnover and for efficient estrogen receptor-alpha transactivation. Mol Cell 2000;5:939-48.
    • (2000) Mol Cell , vol.5 , pp. 939-948
    • Lonard, D.M.1    Nawaz, Z.2    Smith, C.L.3    O'Malley, B.W.4
  • 39
    • 0037351881 scopus 로고    scopus 로고
    • Cyclic, proteosome-mediated turnover of unliganded and liganded ERα on responsive promoters is an integral feature of estrogen signaling
    • Reid G, Hübner MR, Métivier R, Brand H, Denger S, Manu D, et al. Cyclic, proteosome-mediated turnover of unliganded and liganded ERα on responsive promoters is an integral feature of estrogen signaling. Mol Cell 2003;11:695-707.
    • (2003) Mol Cell , vol.11 , pp. 695-707
    • Reid, G.1    Hübner, M.R.2    Métivier, R.3    Brand, H.4    Denger, S.5    Manu, D.6
  • 40
    • 0033677086 scopus 로고    scopus 로고
    • PDZK1 and GREB1 are estrogen-regulated genes expressed in hormone-responsive breast cancer
    • Ghosh MG, Thompson DA, Weigel RJ. PDZK1 and GREB1 are estrogen-regulated genes expressed in hormone-responsive breast cancer. Cancer Res 2000;60:6367-75.
    • (2000) Cancer Res , vol.60 , pp. 6367-6375
    • Ghosh, M.G.1    Thompson, D.A.2    Weigel, R.J.3
  • 41
    • 67651005771 scopus 로고    scopus 로고
    • Positive feedback activation of estrogen receptors by the CXCL12-CXCR4 pathway
    • Sauve K, Lepage J, Sanchez M, Heveker N, Tremblay A. Positive feedback activation of estrogen receptors by the CXCL12-CXCR4 pathway. Cancer Res 2009;69:5793-800.
    • (2009) Cancer Res , vol.69 , pp. 5793-5800
    • Sauve, K.1    Lepage, J.2    Sanchez, M.3    Heveker, N.4    Tremblay, A.5
  • 42
    • 2342526570 scopus 로고    scopus 로고
    • Estrogen regulation in human breast cancer cells of new downstream gene targets involved in estrogen metabolism, cell proliferation and cell transformation
    • Vendrell JA, Magnino F, Danis E, Duchesne MJ, Pinloche S, Pons S, et al. Estrogen regulation in human breast cancer cells of new downstream gene targets involved in estrogen metabolism, cell proliferation and cell transformation. J Mol Endocrinol 2004;32:397-414.
    • (2004) J Mol Endocrinol , vol.32 , pp. 397-414
    • Vendrell, J.A.1    Magnino, F.2    Danis, E.3    Duchesne, M.J.4    Pinloche, S.5    Pons, S.6
  • 43
    • 84896259336 scopus 로고    scopus 로고
    • The emergence of targeted drugs in breast cancer to prevent resistance to endocrine treatment and chemotherapy
    • Austreid E, Lonning PE, Eikesdal HP. The emergence of targeted drugs in breast cancer to prevent resistance to endocrine treatment and chemotherapy. Expert Opin Pharmacother 2014;15:681-700.
    • (2014) Expert Opin Pharmacother , vol.15 , pp. 681-700
    • Austreid, E.1    Lonning, P.E.2    Eikesdal, H.P.3
  • 44
    • 0037088656 scopus 로고    scopus 로고
    • Structure-function relationship of the raloxifene-estrogen receptor-α complex for regulating transforming growth factor-α in breast cancer cells
    • Liu H, Park W, Bentrem DJ, McKian KP, De Los Reyes A, Loweth JA, et al. Structure-function relationship of the raloxifene-estrogen receptor-α complex for regulating transforming growth factor-α in breast cancer cells. J Biol Chem 2002;277:9189-98.
    • (2002) J Biol Chem , vol.277 , pp. 9189-9198
    • Liu, H.1    Park, W.2    Bentrem, D.J.3    McKian, K.P.4    De Los Reyes, A.5    Loweth, J.A.6
  • 45
    • 84874745627 scopus 로고    scopus 로고
    • Long-term effects of continuing adjuvant tamoxifen to 10 years versus stopping at 5 years after diagnosis of oestrogen receptor-positive breast cancer: ATLAS, a randomised trial
    • Davies C, Pan H, Godwin J, Gray R, Arriagada R, Raina V, et al. Long-term effects of continuing adjuvant tamoxifen to 10 years versus stopping at 5 years after diagnosis of oestrogen receptor-positive breast cancer: ATLAS, a randomised trial. Lancet 2013;381:805-16.
    • (2013) Lancet , vol.381 , pp. 805-816
    • Davies, C.1    Pan, H.2    Godwin, J.3    Gray, R.4    Arriagada, R.5    Raina, V.6
  • 47
    • 84884715444 scopus 로고    scopus 로고
    • Sex hormones and breast cancer risk and prognosis
    • Folkerd E, Dowsett M. Sex hormones and breast cancer risk and prognosis. Breast 2013;22Suppl 2:S38-43.
    • (2013) Breast , vol.22 , pp. S38-S43
    • Folkerd, E.1    Dowsett, M.2
  • 48
    • 84975034261 scopus 로고    scopus 로고
    • Patient-derived xenograft study reveals the pharmacology and the role of ESR1 gene aberrations in endocrine therapy resistance of ER positive breast cancer
    • Sen T, Li S, Shao J, Crowder R, Kitchen R, Ellis MJ. Patient-derived xenograft study reveals the pharmacology and the role of ESR1 gene aberrations in endocrine therapy resistance of ER positive breast cancer. Can Res 2014;74:5544.
    • (2014) Can Res , vol.74 , pp. 5544
    • Sen, T.1    Li, S.2    Shao, J.3    Crowder, R.4    Kitchen, R.5    Ellis, M.J.6
  • 49
    • 84921807735 scopus 로고    scopus 로고
    • Everolimus plus exemestane for hormone-receptor-positive, human epidermal growth factor receptor-2-negative advanced breast cancer: Overall survival results from BOLERO-2†
    • Piccart M, Hortobagyi GN, Campone M, Pritchard KI, Lebrun F, Ito Y, et al. Everolimus plus exemestane for hormone-receptor-positive, human epidermal growth factor receptor-2-negative advanced breast cancer: overall survival results from BOLERO-2†. Ann Oncol 2014;25:2357-62.
    • (2014) Ann Oncol , vol.25 , pp. 2357-2362
    • Piccart, M.1    Hortobagyi, G.N.2    Campone, M.3    Pritchard, K.I.4    Lebrun, F.5    Ito, Y.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.