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Volumn 15, Issue 2, 2013, Pages 69-75

Enzalutamide, a second generation androgen receptor antagonist: Development and clinical applications in prostate cancer

Author keywords

Abiraterone; Androgen receptor; Antiandrogen; ARN 509; Castration resistant; Enzalutamide; MDV3100; ODM 201; Prostate cancer

Indexed keywords

ABIRATERONE; ANDROGEN RECEPTOR; ANDROGEN RECEPTOR ANTAGONIST; ANDROSTANOLONE; ANTINEOPLASTIC AGENT; ARN 509; BICALUTAMIDE; CABAZITAXEL; CYTOCHROME P450 2C19; CYTOCHROME P450 2C9; CYTOCHROME P450 3A4; DOCETAXEL; DUTASTERIDE; ENZALUTAMIDE; FLUORO 5 ALPHA DIHYDROTESTOSTERONE; FLUORODEOXYGLUCOSE; HALOPERIDOL; ITRACONAZOLE; MITOXANTRONE; ODM 201; PLACEBO; PREDNISONE; PROSTATE SPECIFIC ANTIGEN; RADIOISOTOPE; RADIUM 223; RD 162; RU 59603; SIPULEUCEL T; TESTOSTERONE; UNCLASSIFIED DRUG;

EID: 84879601455     PISSN: 15233790     EISSN: 15346269     Source Type: Journal    
DOI: 10.1007/s11912-013-0293-9     Document Type: Article
Times cited : (14)

References (31)
  • 1
    • 84928580276 scopus 로고
    • Studies on prostatic cancer.1. The effect of castration, of estrogen and of androgen injections on serum phosphatases in metastatic carcinoma of the prostate
    • 1:CAS:528:DyaH3MXkvVCrtw%3D%3D
    • Huggins CB, Hodges CV. Studies on prostatic cancer.1. The effect of castration, of estrogen and of androgen injections on serum phosphatases in metastatic carcinoma of the prostate. Cancer Res. 1941;1:293-7.
    • (1941) Cancer Res , vol.1 , pp. 293-297
    • Huggins, C.B.1    Hodges, C.V.2
  • 2
    • 0003964363 scopus 로고    scopus 로고
    • American Cancer Society American Cancer Society Atlanta
    • American Cancer Society. Cancer facts & figures 2012. Atlanta: American Cancer Society; 2012.
    • (2012) Cancer Facts & Figures 2012
  • 3
    • 41149138104 scopus 로고    scopus 로고
    • Efficacy of androgen deprivation therapy (ADT) in patients with advanced prostate cancer: Association between Gleason score, prostate-specific antigen level, and prior ADT exposure with duration of ADT effect
    • 18293426 10.1002/cncr.23304
    • Ross RW, Xie W, Regan MM, Pomerantz M, et al. Efficacy of androgen deprivation therapy (ADT) in patients with advanced prostate cancer: association between Gleason score, prostate-specific antigen level, and prior ADT exposure with duration of ADT effect. Cancer. 2008;112(6):1247-53.
    • (2008) Cancer , vol.112 , Issue.6 , pp. 1247-1253
    • Ross, R.W.1    Xie, W.2    Regan, M.M.3    Pomerantz, M.4
  • 4
    • 0034652723 scopus 로고    scopus 로고
    • Androgen receptor mutations in prostate cancer
    • 10706109 1:CAS:528:DC%2BD3cXhs1Shs78%3D
    • Marcelli M, Ittmann M, Mariani S, et al. Androgen receptor mutations in prostate cancer. Cancer Res. 2000;60:944-9.
    • (2000) Cancer Res , vol.60 , pp. 944-949
    • Marcelli, M.1    Ittmann, M.2    Mariani, S.3
  • 5
    • 0029011116 scopus 로고
    • Mutation of the androgen-receptor gene in metastatic androgen-independent prostate cancer
    • 7723794 10.1056/NEJM199505253322101 1:CAS:528:DyaK2MXmvVWnsbs%3D
    • Taplin ME, et al. Mutation of the androgen-receptor gene in metastatic androgen-independent prostate cancer. N Engl J Med. 1995;332:1393-8.
    • (1995) N Engl J Med , vol.332 , pp. 1393-1398
    • Taplin, M.E.1
  • 6
    • 15644368237 scopus 로고    scopus 로고
    • Androgen receptor gene amplification: A possible molecular mechanism for androgen deprivation therapy failure in prostate cancer
    • 9000575 1:CAS:528:DyaK2sXntFKhug%3D%3D
    • Koivisto P, et al. Androgen receptor gene amplification: a possible molecular mechanism for androgen deprivation therapy failure in prostate cancer. Cancer Res. 1997;57:314-9.
    • (1997) Cancer Res , vol.57 , pp. 314-319
    • Koivisto, P.1
  • 7
    • 0028944138 scopus 로고
    • In vivo amplification of the androgen receptor gene and progression of human prostate cancer
    • 7795646 10.1038/ng0495-401 1:CAS:528:DyaK2MXkvV2jurc%3D
    • Visakorpi T, et al. In vivo amplification of the androgen receptor gene and progression of human prostate cancer. Nat Genet. 1995;9:401-6.
    • (1995) Nat Genet , vol.9 , pp. 401-406
    • Visakorpi, T.1
  • 8
    • 1842612441 scopus 로고    scopus 로고
    • Molecular determinants of resistance to antiandrogen therapy
    • 14702632 10.1038/nm972
    • Chen CD, Welsbie DS, Tran C, et al. Molecular determinants of resistance to antiandrogen therapy. Nat Med. 2004;10:33-9.
    • (2004) Nat Med , vol.10 , pp. 33-39
    • Chen, C.D.1    Welsbie, D.S.2    Tran, C.3
  • 9
    • 49249119358 scopus 로고    scopus 로고
    • Maintenance of intratumoral androgens in metastatic prostate cancer: A mechanism for castration-resistant tumor growth
    • 18519708 10.1158/0008-5472.CAN-08-0249 1:CAS:528:DC%2BD1cXmsFKlsr8%3D This study demonstrated that intracrine steroidogenesis maintained intratumoral androgens at levels that could activate AR genes and stimulate tumor growth in CRPC
    • • Montgomery RB, Mostaghel EA, Vessella R, et al. Maintenance of intratumoral androgens in metastatic prostate cancer: a mechanism for castration-resistant tumor growth. Cancer Res. 2008;68(11):4447-54. This study demonstrated that intracrine steroidogenesis maintained intratumoral androgens at levels that could activate AR genes and stimulate tumor growth in CRPC.
    • (2008) Cancer Res , vol.68 , Issue.11 , pp. 4447-4454
    • Montgomery, R.B.1    Mostaghel, E.A.2    Vessella, R.3
  • 10
    • 38349167518 scopus 로고    scopus 로고
    • Docetaxel plus prednisone or mitoxantrone plus prednisone for advanced prostate cancer: Updated survival in the TAX 327 study
    • 18182665 10.1200/JCO.2007.12.4008 1:CAS:528:DC%2BD1cXitVWitLs%3D
    • Berthold DR, Pond GR, Soban F, et al. Docetaxel plus prednisone or mitoxantrone plus prednisone for advanced prostate cancer: updated survival in the TAX 327 study. J Clin Oncol. 2008;26:242.
    • (2008) J Clin Oncol , vol.26 , pp. 242
    • Berthold, D.R.1    Pond, G.R.2    Soban, F.3
  • 11
    • 77955066199 scopus 로고    scopus 로고
    • Sipuleucel-T immunotherapy for castration-resistant prostate cancer
    • 20818862 10.1056/NEJMoa1001294 1:CAS:528:DC%2BC3cXhtVGlurrN
    • Kantoff PW, Higano CS, Shore ND, et al. Sipuleucel-T immunotherapy for castration-resistant prostate cancer. N Engl J Med. 2010;363:411.
    • (2010) N Engl J Med , vol.363 , pp. 411
    • Kantoff, P.W.1    Higano, C.S.2    Shore, N.D.3
  • 12
    • 77957682309 scopus 로고    scopus 로고
    • Prednisone plus cabazitaxel or mitoxantrone for metastatic castration-resistant prostate cancer progressing after docetaxel treatment: A randomized open-label trial
    • 20888992 10.1016/S0140-6736(10)61389-X
    • de Bono JS, Oudard S, Ozguroglu M, et al. Prednisone plus cabazitaxel or mitoxantrone for metastatic castration-resistant prostate cancer progressing after docetaxel treatment: a randomized open-label trial. Lancet. 2010;376:1147.
    • (2010) Lancet , vol.376 , pp. 1147
    • De Bono, J.S.1    Oudard, S.2    Ozguroglu, M.3
  • 13
    • 84866948935 scopus 로고    scopus 로고
    • Abiraterone acetate for treatment of metastatic castration-resistant prostate cancer: Final overall survival analysis of the COU-AA-301 randomised, double-blind, placebo-controlled phase 3 study
    • Fizazi K, Scher HI, Molina A, et al. Abiraterone acetate for treatment of metastatic castration-resistant prostate cancer: final overall survival analysis of the COU-AA-301 randomised, double-blind, placebo-controlled phase 3 study. Lancet Oncol. 2013;13(10):983-92.
    • (2013) Lancet Oncol , vol.13 , Issue.10 , pp. 983-992
    • Fizazi, K.1    Scher, H.I.2    Molina, A.3
  • 14
    • 84872078210 scopus 로고    scopus 로고
    • Abiraterone in metastatic prostate cancer without previous chemotherapy
    • Ryan CJ, Smith MR, de Bono JS, et al. Abiraterone in metastatic prostate cancer without previous chemotherapy. N Engl J Med. 2013;368(2):138-48.
    • (2013) N Engl J Med , vol.368 , Issue.2 , pp. 138-148
    • Ryan, C.J.1    Smith, M.R.2    De Bono, J.S.3
  • 15
    • 0035148171 scopus 로고    scopus 로고
    • Flutamide versus prednisone in patients with prostate cancer symptomatically progressing after androgen-ablative therapy: A phase III study of the European organization for research and treatment of cancer genitourinary group
    • 11134196
    • Fosså SD, Slee PH, Brausi M, et al. Flutamide versus prednisone in patients with prostate cancer symptomatically progressing after androgen-ablative therapy: a phase III study of the European organization for research and treatment of cancer genitourinary group. J Clin Oncol. 2001;19(1):62-71.
    • (2001) J Clin Oncol , vol.19 , Issue.1 , pp. 62-71
    • Fosså, S.D.1    Slee, P.H.2    Brausi, M.3
  • 16
    • 68149098902 scopus 로고    scopus 로고
    • Combined androgen blockade with bicalutamide for advanced prostate cancer: Long-term follow-up of a phase 3, double-blind, randomized study for survival
    • 19536889 10.1002/cncr.24395 1:CAS:528:DC%2BD1MXpslOntbk%3D
    • Akaza H, Hinotsu S, Usami M. Combined androgen blockade with bicalutamide for advanced prostate cancer: long-term follow-up of a phase 3, double-blind, randomized study for survival. Cancer. 2009;115(15):3437-45.
    • (2009) Cancer , vol.115 , Issue.15 , pp. 3437-3445
    • Akaza, H.1    Hinotsu, S.2    Usami, M.3
  • 17
    • 0024324367 scopus 로고
    • A controlled trial of leuprolide with and without flutamide in prostatic carcinoma
    • 2503724 10.1056/NEJM198908173210702 1:STN:280:DyaL1MzksVWgtw%3D%3D
    • Crawford ED, Eisenberger MA, McLeod DG, et al. A controlled trial of leuprolide with and without flutamide in prostatic carcinoma. N Engl J Med. 1989;321(7):419-24.
    • (1989) N Engl J Med , vol.321 , Issue.7 , pp. 419-424
    • Crawford, E.D.1    Eisenberger, M.A.2    McLeod, D.G.3
  • 18
    • 0000428935 scopus 로고    scopus 로고
    • Receptor affinity and potency of non-steroidal antiandrogens: Translation of preclinical findings into clinical activity
    • 12496872 10.1038/sj.pcan.4500262 1:CAS:528:DyaK1MXkt1Smuw%3D%3D
    • Kolvenbag GJ, Furr BJ, Blackledge GR. Receptor affinity and potency of non-steroidal antiandrogens: translation of preclinical findings into clinical activity. Prostate Cancer Prostatic Dis. 1998;1(6):307-14.
    • (1998) Prostate Cancer Prostatic Dis , vol.1 , Issue.6 , pp. 307-314
    • Kolvenbag, G.J.1    Furr, B.J.2    Blackledge, G.R.3
  • 19
    • 65649090203 scopus 로고    scopus 로고
    • Development of a second-generation antiandrogen for treatment of advanced prostate cancer
    • 19359544 10.1126/science.1168175 1:CAS:528:DC%2BD1MXlsVeksro%3D This article describes how enzalutamide was designed, reviews the detailed in vitro and in vivo preclinical data, and shows early evidence of clinical efficacy in the first 30 patients who were treated with enzalutamide
    • • Tran C, Ouk S, Clegg NJ, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009;324(5928):787-90. This article describes how enzalutamide was designed, reviews the detailed in vitro and in vivo preclinical data, and shows early evidence of clinical efficacy in the first 30 patients who were treated with enzalutamide.
    • (2009) Science , vol.324 , Issue.5928 , pp. 787-790
    • Tran, C.1    Ouk, S.2    Clegg, N.J.3
  • 20
    • 77952105685 scopus 로고    scopus 로고
    • Antitumour activity of MDV3100 in castration-resistant prostate cancer: A phase 1-2 study
    • 20398925 10.1016/S0140-6736(10)60172-9 1:CAS:528:DC%2BC3cXltFOmsL0%3D The efficacy data for 140 patients treated with enzalutamide on the phase 1-2 trial are reported in this paper. Significant PSA responses were seen in patients who were treated either before or after receiving chemotherapy. The results of this trial formed the rationale for the two phase 3 trials, AFFIRM (post chemotherapy) and PREVAIL (pre chemotherapy)
    • • Scher HI, Beer TM, Higano CS, et al. Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet. 2010;375(9724):1437-46. The efficacy data for 140 patients treated with enzalutamide on the phase 1-2 trial are reported in this paper. Significant PSA responses were seen in patients who were treated either before or after receiving chemotherapy. The results of this trial formed the rationale for the two phase 3 trials, AFFIRM (post chemotherapy) and PREVAIL (pre chemotherapy).
    • (2010) Lancet , vol.375 , Issue.9724 , pp. 1437-1446
    • Scher, H.I.1    Beer, T.M.2    Higano, C.S.3
  • 21
    • 84876225299 scopus 로고    scopus 로고
    • Antitumor activity of MDV3100 in pre- and post docetaxel advanced prostate cancer: Long-term follow up of the phase 1-2 study
    • (abstr 1342011)
    • Higano CS, Beer TM, Yu EY, et al. Antitumor activity of MDV3100 in pre- and post docetaxel advanced prostate cancer: Long-term follow up of the phase 1-2 study. J Clin Oncol. 2011;29 suppl 7 (abstr 1342011).
    • (2011) J Clin Oncol , vol.29 , Issue.SUPPL. 7
    • Higano, C.S.1    Beer, T.M.2    Yu, E.Y.3
  • 22
    • 79951518634 scopus 로고    scopus 로고
    • Drug safety is a barrier to the discovery of new androgen receptor antagonist drugs
    • 20878947 10.1002/pros.21263
    • Foster WR, Car BD, Shi H, et al. Drug safety is a barrier to the discovery of new androgen receptor antagonist drugs. Prostate. 2010;71:480-8.
    • (2010) Prostate , vol.71 , pp. 480-488
    • Foster, W.R.1    Car, B.D.2    Shi, H.3
  • 23
    • 84866770294 scopus 로고    scopus 로고
    • Increased survival with Enzalutamide in prostate cancer after chemotherapy
    • The results of the AFFIRM trial, the first of the two phase 3 trials with enzalutamide, are reported in this paper. This trial was conducted in men who had previously been treated with chemotherapy. The results of the phase 3 PREVAIL trial in men with metastatic CRPC who have not yet received chemotherapy have not yet matured at the time of this writing (November 2012)
    • • Scher HI, Fizazi K, Saad F, et al. Increased survival with Enzalutamide in prostate cancer after chemotherapy. N Engl J Med. 2012;367:118-97. The results of the AFFIRM trial, the first of the two phase 3 trials with enzalutamide, are reported in this paper. This trial was conducted in men who had previously been treated with chemotherapy. The results of the phase 3 PREVAIL trial in men with metastatic CRPC who have not yet received chemotherapy have not yet matured at the time of this writing (November 2012).
    • (2012) N Engl J Med , vol.367 , pp. 118-197
    • Scher, H.I.1    Fizazi, K.2    Saad, F.3
  • 24
    • 84879606321 scopus 로고    scopus 로고
    • Accessed 29 Oct 2012
    • http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm317997.htm. Accessed 29 Oct 2012.
  • 25
    • 84879606497 scopus 로고    scopus 로고
    • Accessed 30 Nov 2012
    • http://www.accessdata.fda.gov/drugsatfda-docs/label/2012/203415lbl.pdf. Accessed 30 Nov 2012.
  • 26
    • 84863230424 scopus 로고    scopus 로고
    • ARN-509, a novel antiandrogen for prostate cancer treatment
    • 10.1158/0008-5472.CAN-11-3948
    • Clegg NJ, Wongvipat J, Joseph JD, et al. ARN-509, a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012;72(6):1-10.
    • (2012) Cancer Res , vol.72 , Issue.6 , pp. 1-10
    • Clegg, N.J.1    Wongvipat, J.2    Joseph, J.D.3
  • 27
    • 84873804151 scopus 로고    scopus 로고
    • ARN-509 in men with metastatic castration-resistant prostate cancer (CRPC)
    • Abstract 984TiP.DE
    • Rathkopf D, Antonarakis ES, Shore ND, et al. ARN-509 in men with metastatic castration-resistant prostate cancer (CRPC). Ann Oncol. 2012;23:ix317. Abstract 984TiP.DE.
    • (2012) Ann Oncol , vol.23 , pp. 317
    • Rathkopf, D.1    Antonarakis, E.S.2    Shore, N.D.3
  • 28
    • 84873847379 scopus 로고    scopus 로고
    • ARN 509 in high-risk patients with non-metastatic castration resistant prostate cancer
    • Abstract 920P
    • Smith MR, Antonarakis ES, Ryan CJ, et al. ARN 509 in high-risk patients with non-metastatic castration resistant prostate cancer. Ann Oncol. 2012;23:ix303. Abstract 920P.
    • (2012) Ann Oncol , vol.23 , pp. 303
    • Smith, M.R.1    Antonarakis, E.S.2    Ryan, C.J.3
  • 29
    • 84879606850 scopus 로고    scopus 로고
    • ARADES trial: A first-in-man, open-label, phaseI/II safety, pharmacokinetic, and proof-of-concept study of ODM-201 in patients with progressive, metastatic castration-resistant prostate cancer
    • LBA25-PR
    • Massard C, James N, Culine S, Jones R, Vuorela A, Mustonen M, Fizazi K. ARADES trial: a first-in-man, open-label, phaseI/II safety, pharmacokinetic, and proof-of-concept study of ODM-201 in patients with progressive, metastatic castration-resistant prostate cancer. Ann Oncol. 2012;23 Suppl 9. LBA25-PR.
    • (2012) Ann Oncol , vol.23 , Issue.SUPPL. 9
    • Massard, C.1    James, N.2    Culine, S.3    Jones, R.4    Vuorela, A.5    Mustonen, M.6    Fizazi, K.7
  • 30
    • 4744366279 scopus 로고    scopus 로고
    • Docetaxel plus Prednisone or Mitoxantrone plus Prednisone for advanced prostate cancer
    • 15470213 10.1056/NEJMoa040720 1:CAS:528:DC%2BD2cXot1Kmu7s%3D
    • Tannock IF, DeWit D, Berry WR, Horti J, et al. Docetaxel plus Prednisone or Mitoxantrone plus Prednisone for advanced prostate cancer. N Engl J Med. 2004;351:1502-12.
    • (2004) N Engl J Med , vol.351 , pp. 1502-1512
    • Tannock, I.F.1    Dewit, D.2    Berry, W.R.3    Horti, J.4
  • 31
    • 84860854128 scopus 로고    scopus 로고
    • Overall survival benefit and safety profile of radium-223 chloride, a first-in-class alpha-pharmaceutical: Results from a phase III randomized trial (ALSYMPCA) in patients with castration-resistant prostate cancer (CRPC) with bone metastases
    • (abstr 8)
    • Parker C, Heinrich D, O'Sullivan JM, et al. Overall survival benefit and safety profile of radium-223 chloride, a first-in-class alpha-pharmaceutical: Results from a phase III randomized trial (ALSYMPCA) in patients with castration-resistant prostate cancer (CRPC) with bone metastases. J Clin Oncol. 2012;30 suppl 5 (abstr 8).
    • (2012) J Clin Oncol , vol.30 , Issue.SUPPL. 5
    • Parker, C.1    Heinrich, D.2    O'Sullivan, J.M.3


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