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Drug Profile

The safety and efficacy of enzalutamide in the treatment of advanced prostate cancer

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Pages 681-696 | Received 08 Mar 2016, Accepted 18 May 2016, Published online: 07 Jun 2016

References

  • Eisenberger MA, Walsh PC. Early androgen deprivation for prostate cancer? N Engl J Med. 1999;341:1837–1838.
  • Chen CD, Welsbie DS, Tran C, et al. Molecular determinants of resistance to antiandrogen therapy. Nat Med. 2004;10(1):33–39.
  • Visakorpi T, Hyytinen E, Koivisto P, et al. In vivo amplification of the androgen receptor gene and progression of human prostate cancer. Nat Genet. 1995;9:401–406.
  • Koivisto P, Kononen J, Palmberg C, et al. Androgen receptor gene amplification: a possible molecular mechanism for androgen deprivation therapy failure in prostate cancer. Cancer Res. 1997;57:314–319.
  • Grasso CS, Wu YM, Robinson DR, et al. The mutational landscape of lethal castration-resistant prostate cancer. Nature. 2012;487:239–243.
  • Taplin ME, Bubley GJ, Shuster TD, et al. Mutation of the androgen-receptor gene in metastatic androgen-independent prostate cancer. N Engl J Med. 1995;332:1393–1398.
  • Hara T, Miyazaki J, Araki H, et al. Novel mutations of androgen receptor: a possible mechanism of bicalutamide withdrawal syndrome. Cancer Res. 2003;63:149–153.
  • Jenster G, van der Korput HA, van Vroonhoven C, et al. Domains of the human androgen receptor involved in steroid binding, transcriptional activation, and subcellular localization. Mol Endocrinol. 1991;5:1396–1404.
  • Locke JA, Guns ES, Lubik AA, et al. Androgen levels increase by intratumoral de novo steroidogenesis during progression of castration-resistant prostate cancer. Cancer Res. 2008;68:6407–6415.
  • Titus MA, Schell MJ, Lih FB, et al. Testosterone and dihydrotestosterone tissue levels in recurrent prostate cancer. Clin Cancer Res. 2005;11:4653–4657.
  • Guo Z, Dai B, Jiang T, et al. Regulation of androgen receptor activity by tyrosine phosphorylation. Cancer Cell. 2006;10:309–319.
  • Lin HK, Hu YC, Yang L, et al. Suppression versus induction of androgen receptor functions by the phosphatidylinositol 3-kinase/Akt pathway in prostate cancer LNCaP cells with different passage numbers. J Biol Chem. 2003;278:50902–50907.
  • Tran C, Ouk S, Clegg NJ, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009;324(5928):787–790.
  • Van Dort ME, Robins DM, Wayburn B. Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile as a high-affinity nonsteroidal androgen receptor ligand. J Med Chem. 2000;43(17):3344–3347.
  • Guerrero J, Alfaro IE, Gómez F, et al. Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer. Prostate. 2013;73(12):1291–1305.
  • Scher HI, Beer TM, Higano CS, et al. Prostate Cancer Foundation/Department of Defense Prostate Cancer Clinical Trials Consortium. Antitumor activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet. 2010;375(9724):1437–1446.
  • Scher HI, Fizazi K, Saad F, et al. Increased survival with enzalutamide in prostate cancer after chemotherapy. N Engl J Med. 2012;367(13):1187–1197.
  • Fizazi K, Scher HI, Miller K, et al. Effect of enzalutamide on time to first skeletal-related event, pain, and quality of life in men with castration-resistant prostate cancer: results from the randomised, phase 3 AFFIRM trial. Lancet Oncol. 2014;15(10):1147–1156.
  • Cella D, Ivanescu C, Holmstrom S, et al. Impact of enzalutamide on quality of life in men with metastatic castration-resistant prostate cancer after chemotherapy: additional analyses from the AFFIRM randomized clinical trial. Ann Oncol. 2015;26(1):179–185.
  • Sternberg CN, De Bono JS, Chi KN, et al. Improved outcomes in elderly patients with metastatic castration-resistant prostate cancer treated with the androgen receptor inhibitor enzalutamide: results from the phase III AFFIRM trial. Ann Oncol. 2014;25(2):429–434.
  • Richards J, Lim AC, Hay CW, et al. Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100. Cancer Res. 2012;72(9):2176–2182.
  • Scher HI, Fizazi K, Saad F, et al. Association of baseline corticosteroid with outcomes in a multivariate analysis of the phase 3 affirm study of enzalutamide (ENZA), an androgen receptor signaling inhibitor (ARSI). Ann Oncol. 2012;23(suppl9):Abstr 899PD.
  • Scher HI, Fizazi K, Saad F, et al. Impact of on-study corticosteroid use on efficacy and safety in the phase III AFFIRM study of enzalutamide (ENZA), an androgen receptor inhibitor. J Clin Oncol. 2013;31(suppl 6):abstr 6.
  • Beer TM, Armstrong AJ, Rathkopf DE, et al. Enzalutamide in metastatic prostate cancer before chemotherapy. N Engl J Med. 2014;371(5):424–433.
  • Loriot Y, Miller K, Sternberg CN, et al. Effect of enzalutamide on health-related quality of life, pain, and skeletal-related events in asymptomatic and minimally symptomatic, chemotherapy-naive patients with metastatic castration-resistant prostate cancer (PREVAIL): results from a randomised, phase 3 trial. Lancet Oncol. 2015;16(5):509–521.
  • Higano C, Alumkal J, Chowdhury S, et al. Response rates and outcomes with enzalutamide for patients with metastatic castration resistant prostate cancer and visceral disease in the prevail trial. Ann Oncol. 2014;25(Suppl4):Abstr 767P.
  • Graff JN, Baciarello G, Armstrong AJ, et al. Efficacy and safety of enzalutamide in patients 75 years or older with chemotherapy-naive metastatic castration-resistant prostate cancer: results from PREVAIL. Ann Oncol. 2016;27(2):286–294.
  • Kucuk O, Fisher E, Moinpour CM, et al. Phase II trial of bicalutamide in patients with advanced prostate cancer in whom conventional hormonal therapy failed: a Southwest Oncology Group study (SWOG 9235). Urology. 2001;58(1):53–58.
  • Manikandan R, Srirangam SJ, Pearson E, et al. Diethylstilboestrol versus bicalutamide in hormone refractory prostate carcinoma: a prospective randomized trial. Urol Int. 2005;75(3):217–221.
  • Small EJ, Srinivas S. The antiandrogen withdrawal syndrome. Experience in a large cohort of unselected patients with advanced prostate cancer. Cancer. 1995;76(8):1428–1434.
  • Shore ND, Chowdhury S, Villers A, et al. Efficacy and safety of enzalutamide versus bicalutamide for patients with metastatic prostate cancer (TERRAIN): a randomised, double-blind, phase 2 study. Lancet Oncol. 2016;17(2):153–163.
  • Penson DF, Armstrong AJ, Concepcion R, et al. Enzalutamide versus bicalutamide in castration-resistant prostate cancer: the STRIVE trial. J Clin Oncol. 2016. pii: JCO649285. [Epub ahead of print].
  • De Bono JS, Logothetis CJ, Molina A, et al. Abiraterone and increased survival in metastatic prostate cancer. N Engl J Med. 2011;364(21):1995–2005.
  • 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 randomised open-label trial. Lancet. 2010;376(9747):1147–1154.
  • Tannock IF, De Wit R, Berry WR, et al. Docetaxel plus prednisone or mitoxantrone plus prednisone for advanced prostate cancer. N Engl J Med. 2004;351(15):1502–1512.
  • Parker C, Nilsson S, Heinrich D, et al. Alpha emitter radium-223 and survival in metastatic prostate cancer. N Engl J Med. 2013;369(3):213–223.
  • Kantoff PW, Higano CS, Shore ND, et al. Sipuleucel-T immunotherapy for castration-resistant prostate cancer. N Engl J Med. 2010;363(5):411–422.
  • Ryan CJ, Smith MR, De Bono JS, et al. Abiraterone in metastatic prostate cancer without previous chemotherapy. N Engl J Med. 2013;368(2):138–148.
  • Ryan CJ, Smith MR, Fizazi K, et al. Abiraterone acetate plus prednisone versus placebo plus prednisone in chemotherapy-naive men with metastatic castration-resistant prostate cancer (COU-AA-302): final overall survival analysis of a randomised, double-blind, placebo-controlled phase 3 study. Lancet Oncol. 2015;16(2):152–160.
  • Modena A, Ciccarese C, Fantinel E, et al. Metastatic castration-resistant prostate cancer: targeting the mechanisms of resistance to abiraterone acetate and enzalutamide. Expert Rev Anticancer Ther. 2015;15(9):1037–1048.
  • Buttigliero C, Tucci M, Bertaglia V, et al. Understanding and overcoming the mechanisms of primary and acquired resistance to abiraterone and enzalutamide in castration resistant prostate cancer. Cancer Treat Rev. 2015;41(10):884–892.
  • Hu R, Lu C, Mostaghel EA, et al. Distinct transcriptional programs mediated by the ligand-dependent full-length androgen receptor and its splice variants in castration-resistant prostate cancer. Cancer Res. 2012;72(14):3457–3462.
  • Mostaghel EA, Marck BT, Plymate SR, et al. Resistance to CYP17A1 inhibition with abiraterone in castration-resistant prostate cancer: induction of steroidogenesis and androgen receptor splice variants. Clin Cancer Res. 2011;17(18):5913–5925.
  • Li Y, Chan SC, Brand LJ, et al. Androgen receptor splice variants mediate enzalutamide resistance in castration-resistant prostate cancer cell lines. Cancer Res. 2013;73(2):483–489.
  • Cai C, Chen S, Ng P, et al. Intratumoral de novo steroid synthesis activates androgen receptor in castration-resistant prostate cancer and is upregulated by treatment with CYP17A1 inhibitors. Cancer Res. 2011;71(20):6503–6513.
  • Noonan KL, North S, Bitting RL, et al. Clinical activity of abiraterone acetate in patients with metastatic castration-resistant prostate cancer progressing after enzalutamide. Ann Oncol. 2013;24(7):1802–1807.
  • Loriot Y, Bianchini D, Ileana E, et al. Antitumour activity of abiraterone acetate against metastatic castration-resistant prostate cancer progressing after docetaxel and enzalutamide (MDV3100). Ann Oncol. 2013;24(7):1807–1812.
  • Balbas MD, Evans MJ, Hosfield DJ, et al. Overcoming mutation-based resistance to antiandrogens with rational drug design. Elife. 2013;2:e00499.
  • Schrader AJ, Boegemann M, Ohlmann CH, et al. Enzalutamide in castration-resistant prostate cancer patients progressing after docetaxel and abiraterone. Eur Urol. 2014;65(1):30–36.
  • Bianchini D, Lorente D, Rodriguez-Vida A, et al. Antitumour activity of enzalutamide (MDV3100) in patients with metastatic castration-resistant prostate cancer (CRPC) pre-treated with docetaxel and abiraterone. Eur J Cancer. 2014;50(1):78–84.
  • Schmid SC, Geith A, Böker A, et al. Enzalutamide after docetaxel and abiraterone therapy in metastatic castration-resistant prostate cancer. Adv Ther. 2014;31(2):234–241.
  • Thomson D, Charnley N, Parikh O. Enzalutamide after failure of docetaxel and abiraterone in metastatic castrate-resistant prostate cancer. Eur J Cancer. 2014;50(5):1040–1041.
  • Badrising S, van der Noort V, van Oort IM, et al. Clinical activity and tolerability of enzalutamide (MDV3100) in patients with metastatic, castration-resistant prostate cancer who progress after docetaxel and abiraterone treatment. Cancer. 2014;120(7):968–975.
  • Thomsen FB, Røder MA, Rathenborg P, et al. Enzalutamide treatment in patients with metastatic castration-resistant prostate cancer progressing after chemotherapy and abiraterone acetate. Scand J Urol. 2014;48(3):268–275.
  • Brasso K, Thomsen FB, Schrader AJ, et al. Enzalutamide antitumour activity against metastatic castration-resistant prostate cancer previously treated with docetaxel and abiraterone: a multicentre analysis. Eur Urol. 2015;68(2):317–324.
  • Vera-Badillo FE, Leibowitz-Amit R, Templeton A, et al. Clinical activity of enzalutamide against metastatic castration-resistant prostate cancer (mCRPC) in patients who have progressed on abiraterone acetate: the Princess Margaret experience. J Clin Oncol. 2014;32(suppl 4):abstr 159.
  • Petrelli F, Coinu A, Borgonovo K, et al. Enzalutamide after docetaxel and abiraterone acetate treatment in prostate cancer: a pooled analysis of 10 case series. Clin Genitourin Cancer. 2015;13(3):193–198.
  • Caffo O, De Giorgi U, Fratino L, et al. Clinical outcomes of castration-resistant prostate cancer treatments administered as third or fourth line following failure of docetaxel and other second-line treatment: results of an Italian Multicentre Study. Eur Urol. 2015;68(1):147–153.
  • Scholz MC, Lam RY, Turner JS, et al. Enzalutamide in men with prostate cancer resistant to docetaxel and abiraterone. J Clin Oncol. 2014;32(suppl 4):abstr 247.
  • Cheng HH, Gulati R, Azad A, et al. Activity of enzalutamide in men with metastatic castration-resistant prostate cancer is affected by prior treatment with abiraterone and/or docetaxel. Prostate Cancer Prostatic Dis. 2015;18(2):122–127.
  • Azad AA, Eigl BJ, Murray RN, et al. Efficacy of enzalutamide following abiraterone acetate in chemotherapy-naive metastatic castration-resistant prostate cancer patients. Eur Urol. 2015;67(1):23–29.
  • Sandhu GS, Parikh RA, Appleman LJ, et al. Enzalutamide after abiraterone in patients with metastatic castrate-resistant prostate cancer (mCRPC). J Clin Oncol. 2014;32(suppl 4):abstr 240.
  • Zhang T, Dhawan MS, Healy P, et al. Exploring the clinical benefit of docetaxel or enzalutamide after disease progression during abiraterone acetate and prednisone treatment in men with metastatic castration-resistant prostate cancer. Clin Genitourin Cancer. 2015;13(4):392–399.
  • Rodriguez-Vida A, Galazi M, Rudman S, et al. Enzalutamide for the treatment of metastatic castration-resistant prostate cancer. Drug Des Devel Ther. 2015;9:3325–3339.
  • Suzman DL, Luber B, Schweizer MT, et al. Clinical activity of enzalutamide versus docetaxel in men with castration-resistant prostate cancer progressing after abiraterone. Prostate. 2014;74(13):1278–1285.
  • Nadal R, Zhang Z, Rahman H, et al. Clinical activity of enzalutamide in Docetaxel-naïve and Docetaxel-pretreated patients with metastatic castration-resistant prostate cancer. Prostate. 2014;74(15):1560–1568.
  • Morris MJ, Rathkopf DE, Novotny W, et al. Phase Ib study of enzalutamide in combination with docetaxel in men with metastatic castration-resistant prostate cancer. Clin Cancer Res. 2016. pii: clincanres.2638.2015. [Epub ahead of print].
  • Petrylak DP, Quinn DI, Dreicer R, et al. STRIDE, a randomized, phase 2, open-label study of sipuleucel-T with concurrent vs sequential enzalutamide in metastatic castration-resistant prostate cancer (mCRPC). Ann Oncol. 2014;25(suppl 4):Abstr 774P.
  • Ciccarese C, Santoni M, Brunelli M, et al. AR-V7 and prostate cancer: the watershed for treatment selection? Cancer Treat Rev. 2016;43:27–35.
  • Antonarakis ES, Lu C, Wang H, et al. AR-V7 and resistance to enzalutamide and abiraterone in prostate cancer. N Engl J Med. 2014;371:1028–1038.

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