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Expert Opinion on Investigational Drugs Volume 17, 2008 - Issue 8
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Drug Evaluation

ZD4054: a specific endothelin A receptor antagonist with promising activity in metastatic castration-resistant prostate cancer

Ruth Warren University of Wisconsin School of Medicine and Public Health, Health Sciences Learning Center, 750 Highland Avenue, Madison, WI 53705, USA
, DO &
Glenn Liu University of Wisconsin Paul P. Carbone Comprehensive Cancer Center, Genitourinary Oncology and Experimental Therapeutics Group, Section of Hematology/Oncology, 600 Highland Avenue, K6/534 Clinical Science Center, Madison, WI 53792, USA +1 608 265 8689; +1 608 265 8133; [email protected]
, MD
Pages 1237-1245 | Published online: 10 Jul 2008

Bibliography

  • Jemal A, Siegel R, Ward E, et al. Cancer statistics, 2007. CA Cancer J Clin 2007;57(1):43-66
  • Kantoff PW, Halabi S, Conaway M, et al. Hydrocortisone with or without mitoxantrone in men with hormone-refractory prostate cancer: results of the cancer and leukemia group B 9182 study. J Clin Oncol 1999;17(8):2506-13
  • Tannock IF, Osoba D, Stockler MR, et al. Chemotherapy with mitoxantrone plus prednisone or prednisone alone for symptomatic hormone-resistant prostate cancer: a Canadian randomized trial with palliative end points. J Clin Oncol 1996;14(6):1756-64
  • 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):1502-12
  • Saitoh H, Hida M, Shimbo T, et al. Metastatic patterns of prostatic cancer. Correlation between sites and number of organs involved. Cancer 1984;54(12):3078-84
  • Daniell HW, Dunn SR, Ferguson DW, et al. Progressive osteoporosis during androgen deprivation therapy for prostate cancer. J Urol 2000;163(1):181-6
  • Stoch SA, Parker RA, Chen L, et al. Bone loss in men with prostate cancer treated with gonadotropin-releasing hormone agonists. J Clin Endocrinol Metab 2001;86(6):2787-91
  • Saad F, Gleason DM, Murray R, et al. A randomized, placebo-controlled trial of zoledronic acid in patients with hormone-refractory metastatic prostate carcinoma. J Natl Cancer Inst 2002;94(19):1458-68
  • Scher HI, Heller G. Clinical states in prostate cancer: toward a dynamic model of disease progression. Urology 2000;55(3):323-7
  • Morris MJ, Scher HI. Clinical approaches to osseous metastases in prostate cancer. Oncologist 2003;8(2):161-73
  • Armstrong AJ, Garrett-Mayer E, Ou Yang YC, et al. Prostate-specific antigen and pain surrogacy analysis in metastatic hormone-refractory prostate cancer. J Clin Oncol 2007;25(25):3965-70
  • Prentice R. Surrogate end points in clinical trials: definition and operational criteria. Stat Med 1989;8:431-40
  • Rubanyi GM, Polokoff MA. Endothelins: molecular biology, biochemistry, pharmacology, physiology, and pathophysiology. Pharmacol Rev 1994;46(3):325-415
  • Levin ER. Endothelins. N Engl J Med 1995;333(6):356-63
  • Bagnato A, Catt KJ. Endothelins as Autocrine Regulators of Tumor Cell Growth. Trends Endocrinol Metab 1998;9(9):378-83
  • Goldie RG. Endothelins in health and disease: an overview. Clin Exp Pharmacol Physiol 1999;26(2):145-8
  • Nelson J, Bagnato A, Battistini B, Nisen P. The endothelin axis: emerging role in cancer. Nat Rev Cancer 2003;3(2):110-6
  • Bagnato A, Natali PG. Endothelin receptors as novel targets in tumor therapy. J Transl Med 2004;2(1):16
  • Lalich M, McNeel DG, Wilding G, Liu G. Endothelin receptor antagonists in cancer therapy. Cancer Invest 2007;25(8):785-94
  • Nelson JB, Chan-Tack K, Hedican SP, et al. Endothelin-1 production and decreased endothelin B receptor expression in advanced prostate cancer. Cancer Res 1996;56(4):663-8
  • Nelson JB, Nabulsi AA, Vogelzang NJ, et al. Suppression of prostate cancer induced bone remodeling by the endothelin receptor A antagonist atrasentan. J Urol 2003;169(3):1143-9
  • Daub H, Weiss FU, Wallasch C, Ullrich A. Role of transactivation of the EGF receptor in signalling by G-protein-coupled receptors. Nature 1996;379(6565):557-60
  • Vacca F, Bagnato A, Catt KJ, Tecce R. Transactivation of the epidermal growth factor receptor in endothelin-1-induced mitogenic signaling in human ovarian carcinoma cells. Cancer Res 2000;60(18):5310-7
  • Bagnato A, Tecce R, Di Castro V, Catt KJ. Activation of mitogenic signaling by endothelin 1 in ovarian carcinoma cells. Cancer Res 1997;57(7):1306-11
  • Del Bufalo D, Di Castro V, Biroccio A, et al. Endothelin-1 protects ovarian carcinoma cells against paclitaxel-induced apoptosis: requirement for Akt activation. Mol Pharmacol 2002;61(3):524-32
  • Rosano L, Spinella F, Salani D, et al. Therapeutic targeting of the endothelin a receptor in human ovarian carcinoma. Cancer Res 2003;63(10):2447-53
  • Nelson JB, Hedican SP, George DJ, et al. Identification of endothelin-1 in the pathophysiology of metastatic adenocarcinoma of the prostate. Nat Med 1995;1(9):944-9
  • Bagnato A, Tecce R, Moretti C, et al. Autocrine actions of endothelin-1 as a growth factor in human ovarian carcinoma cells. Clin Cancer Res 1995;1(9):1059-66
  • Drimal J, Drimal J Jr, Drimal D. Enhanced endothelin ET(B) receptor down-regulation in human tumor cells. Eur J Pharmacol 2000;396(1):19-22
  • Bagnato A, Cirilli A, Salani D, et al. Growth inhibition of cervix carcinoma cells in vivo by endothelin A receptor blockade. Cancer Res 2002;62(22):6381-4
  • Grimshaw MJ, Naylor S, Balkwill FR. Endothelin-2 is a hypoxia-induced autocrine survival factor for breast tumor cells. Mol Cancer Ther 2002;1(14):1273-81
  • Lahav R, Heffner G, Patterson PH. An endothelin receptor B antagonist inhibits growth and induces cell death in human melanoma cells in vitro and in vivo. Proc Natl Acad Sci USA 1999;96(20):11496-500
  • Gohji K, Kitazawa S, Tamada H, et al. Expression of endothelin receptor a associated with prostate cancer progression. J Urol 2001;165(3):1033-6
  • Godara G, Cannon GW, Cannon GM Jr, et al. Role of endothelin axis in progression to aggressive phenotype of prostate adenocarcinoma. Prostate 2005;65(1):27-34
  • Nelson JB, Lee WH, Nguyen SH, et al. Methylation of the 5′ CpG island of the endothelin B receptor gene is common in human prostate cancer. Cancer Res 1997;57(1):35-7
  • Kopetz ES, Nelson JB, Carducci MA. Endothelin-1 as a target for therapeutic intervention in prostate cancer. Invest New Drugs 2002;20(2):173-82
  • Chiao JW, Moonga BS, Yang YM, et al. Endothelin-1 from prostate cancer cells is enhanced by bone contact which blocks osteoclastic bone resorption. Br J Cancer 2000;83(3):360-5
  • Curtis N, Howard Z, Brooks N, Curwen J. ZD4054 specifically inhibits endothelin A receptor-mediated anti-apoptotic effects, but not endothelin B receptor-medicated pro-apoptotic effects. Eur J Cancer Suppl 2004;2(8):27
  • Dreicer R, Curtis N, Morris CD, et al. ZD4054 specifically inhibits endothelin A receptor-mediated effects but not endothelin B receptor-mediated effects. ASCO Multidisciplinary Prostate Cancer Symposium; February 17 – 19, 2005, Orlando, FL, USA
  • Okazawa M, Shiraki T, Ninomiya H, et al. Endothelin-induced apoptosis of A375 human melanoma cells. J Biol Chem 1998;273(20):12584-92
  • Lassiter LK, Carducci MA. Endothelin receptor antagonists in the treatment of prostate cancer. Semin Oncol 2003;30(5):678-88
  • Bagnato A, Salani D, Di Castro V, et al. Expression of endothelin 1 and endothelin A receptor in ovarian carcinoma: evidence for an autocrine role in tumor growth. Cancer Res 1999;59(3):720-7
  • Salani D, Taraboletti G, Rosano L, et al. Endothelin-1 induces an angiogenic phenotype in cultured endothelial cells and stimulates neovascularization in vivo. Am J Pathol 2000;157(5):1703-11
  • Spinella F, Rosano L, Di Castro V, et al. Endothelin-1 induces vascular endothelial growth factor by increasing hypoxia-inducible factor-1alpha in ovarian carcinoma cells. J Biol Chem 2002;277(31):27850-5
  • Salani D, Di Castro V, Nicotra MR, et al. Role of endothelin-1 in neovascularization of ovarian carcinoma. Am J Pathol 2000;157(5):1537-47
  • Strohmeyer D, Rossing C, Bauerfeind A, et al. Vascular endothelial growth factor and its correlation with angiogenesis and p53 expression in prostate cancer. Prostate 2000;45(3):216-24
  • Rosano L, Salani D, Di Castro V, et al. Endothelin-1 promotes proteolytic activity of ovarian carcinoma. Clin Sci (Lond) 2002;103(Suppl 48):306S-309S
  • Rosano L, Varmi M, Salani D, et al. Endothelin-1 induces tumor proteinase activation and invasiveness of ovarian carcinoma cells. Cancer Res 2001;61(22):8340-66
  • Spinella F, Rosano L, Di Castro V, et al. Endothelin-1 decreases gap junctional intercellular communication by inducing phosphorylation of connexin 43 in human ovarian carcinoma cells. J Biol Chem 2003;278(42):41294-301
  • Carducci MA, Nelson JB, Bowling MK, et al. Atrasentan, an endothelin-receptor antagonist for refractory adenocarcinomas: safety and pharmacokinetics. J Clin Oncol 2002;20(8):2171-80
  • Zonnenberg BA, Groenewegen G, Janus TJ, et al. Phase I dose-escalation study of the safety and pharmacokinetics of atrasentan: an endothelin receptor antagonist for refractory prostate cancer. Clin Cancer Res 2003;9(8):2965-72
  • Ryan CW, Vogelzang NJ, Vokes EE, et al. Dose-ranging study of the safety and pharmacokinetics of atrasentan in patients with refractory malignancies. Clin Cancer Res 2004;10(13):4406-11
  • Nelson JB, Nguyen SH, Wu-Wong JR, et al. New bone formation in an osteoblastic tumor model is increased by endothelin-1 overexpression and decreased by endothelin A receptor blockade. Urology 1999;53(5):1063-9
  • Morris CD, Rose A, Curwen J, et al. Specific inhibition of the endothelin A receptor with ZD4054: clinical and pre-clinical evidence. Br J Cancer 2005;92(12):2148-52
  • Logothetis CJ, Lin SH. Osteoblasts in prostate cancer metastasis to bone. Nat Rev Cancer 2005;5(1):21-8
  • Curtis N, Anderson E, Brooks J, Curwen J. ZD4054 blocks ET-1-stimulated phosphorylation of p44/42 mitogen-activated protein kinase and proliferation of osteoblast cells. Proceedings American Association of Cancer Research; April 16 – 20, 2005, Anaheim, CA, USA
  • Dahlof B, Gustafsson D, Hedner T, et al. Regional haemodynamic effects of endothelin-1 in rat and man: unexpected adverse reaction. J Hypertens 1990;8(9):811-7
  • Pomonis JD, Rogers SD, Peters CM, et al. Expression and localization of endothelin receptors: implications for the involvement of peripheral glia in nociception. J Neurosci 2001;21(3):999-1006
  • Khodorova A, Navarro B, Jouaville LS, et al. Endothelin-B receptor activation triggers an endogenous analgesic cascade at sites of peripheral injury. Nat Med 2003;9(8):1055-61
  • Yuyama H, Koakutsu A, Fujiyasu N, et al. Effects of selective endothelin ET(A) receptor antagonists on endothelin-1-induced potentiation of cancer pain. Eur J Pharmacol 2004;492(2-3):177-82
  • Yuyama H, Sanagi M, Koakutsu A, et al. Pharmacological characterization of YM598, an orally active and highly potent selective endothelin ET(A) receptor antagonist. Eur J Pharmacol 2003;478(1):61-71
  • Opgenorth TJ, Adler AL, Calzadilla SV, et al. Pharmacological characterization of A-127722: an orally active and highly potent ETA-selective receptor antagonist. J Pharmacol Exp Ther 1996;276(2):473-81
  • Carducci MA, Padley RJ, Breul J, et al. Effect of endothelin-A receptor blockade with atrasentan on tumor progression in men with hormone-refractory prostate cancer: a randomized, phase II, placebo-controlled trial. J Clin Oncol 2003;21(4):679-89
  • Nelson JB. Endothelin inhibition: novel therapy for prostate cancer. J Urol 2003;170(6 Pt 2):S65-7; discussion S7-8
  • Michaelson MD, Kaufman DS, Kantoff P, et al. Randomized phase II study of atrasentan alone or in combination with zoledronic acid in men with metastatic prostate cancer. Cancer 2006;107(3):530-5
  • Carducci MA, Saad F, Abrahamsson PA, et al. A phase 3 randomized controlled trial of the efficacy and safety of atrasentan in men with metastatic hormone-refractory prostate cancer. Cancer 2007;110(9):1959-66
  • Stensland B, Roberts R. N-3-methoxy-5-methylpyrazine-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl] phenyl) pyridine-3-sulfonamide (ZD4054 form1). Struct Rep 2004;60(10):1817-9
  • Clarkson-Jones J, Kenyon A, Kemp J, et al. Metabolism of [14 C]-ZD4054 in healthy volunteers [poster]. 14th European Conference on Clinical Oncology; September 23 – 27, 2007, Barcelona, Spain
  • Swaisland H, Oliver S, Morris T, et al. Clinical drug interactions with ZD4054 in healthy, male volunteers [poster]. European Multidisciplinary Meeting on Urological Cancers; November 2 – 4, 2007, Barcelona, Spain
  • Ranson M, Usami M, Maruoka M, et al. The pharmacokinetics and tolerability profile of once-daily oral ZD4054 in Japanese and caucasian patients wtih hormone-resistant prostate cancer [poster]. 14th European Conference on Clinical Oncology; September 23 – 27, 2007, Barcelona, Spain
  • Liu G, Dreicer R, Hou J, et al. Tolerability profile of ZD4054 is consistent with the effects of endothelin A receptor-specific antagonism. J Clin Oncol 2005;23(16S):4628
  • James ND, Borre M, Zonnenberg BA, et al. ZD4054, a potent, specific endothelin A receptor antagonist, improves overall survival in pain-free or mildly symptomatic patients with hormone-resistant prostate cancer (HRPC) and bone metastases [abstract # 3LB]. European Conference of Clinical Oncologists; September 23 – 27, 2007, Barcelona, Spain
  • Dawson N, Phung D, Morris M, et al. Impact of the specific endothelin A receptor antagonist ZD4054 onoverall survival and bone metastasis in patients with hormone-resistant prostate cancer: results of a phase II trial. 2008 Genitourinary Cancers Symposium; 2008; San Fransisco, California
  • Scher HI, Morris MJ, Kelly WK, et al. Prostate cancer clinical trial end points: “RECIST”ing a step backwards. Clin Cancer Res 2005;11(14):5223-32

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