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Expert Opinion on Investigational Drugs Volume 17, 2008 - Issue 7
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Drug Evaluation

Apaziquone for non-muscle invasive bladder cancer: a critical review

J Alfred Witjes Radboud University Nijmegen Medical Centre, Department of Urology (659), PO Box 9101, 6500 H.B Nijmegen, The Netherlands +31 24 361 6712; +31 24 354 1031; [email protected]
&
Prasad S Kolli Spectrum Pharmaceuticals, Department of biopharmaceuticals, Irvine, California, USA
Pages 1085-1096 | Published online: 12 Jun 2008

Bibliography

  • Oosterlinck W, van der Meijden AP, Sylvester R, et al. Guidelines on TaT1 (non-muscle invasive) bladder Cancer. In: Guidelines, european association of urology. Arnhem: Drukkerij Gelderland bv; 2006. p. 3-17
  • Kirkali Z, Chan T, Manoharan M, et al. Bladder cancer: epidemiology, staging and grading, and diagnosis. Urology 2005;66:4-34
  • Sylvester RJ, van der Meijden AP, Oosterlinck W, et al. Predicting recurrence and progression in individual patients with stage Ta T1 bladder cancer using EORTC risk tables: a combined analysis of 2596 patients from seven EORTC trials. Eur Urol 2006;49:466-77
  • Oosterlinck W, Lobel B, Jakse G, et al. Guidelines on bladder cancer. Eur Urol 2002;41:105-12
  • Sylvester RJ, Oosterlinck W, van der Meijden AP. A single immediate postoperative instillation of chemotherapy decreases the risk of recurrence in patients with stage Ta T1 bladder cancer: a meta-analysis of published results of randomized clinical trials. J Urol 2004;171:2186-90
  • Kaasinen E, Rintala E, Hellstrom P, et al. Factors explaining recurrence in patients undergoing chemoimmunotherapy regimens for frequently recurring superficial bladder carcinoma. Eur Urol 2002;42:167-74
  • Jakse G, Algaba F, Malmström PU, Oosterlinck W. A second-look TUR in T1 transitional cell carcinoma: why? Eur Urol 2004;45:539-46
  • Herr HW. The value of a second transurethral resection in evaluating patients with bladder tumors. J Urol 1999;162:74-6
  • Dutta SC, Smith JA Jr, Shappell SB, et al. Clinical under staging of high risk nonmuscle invasive urothelial carcinoma treated with radical cystectomy. J Urol 2001;166:490-3
  • Sylvester RJ, van der Meijden AP, Lamm DL. Intravesical bacillus Calmette-Guerin reduces the risk of progression in patients with superficial bladder cancer: a meta-analysis of the published results of randomized clinical trials. J Urol 2002;168:1964-70
  • Witjes JA. Management of BCG failures in superficial bladder cancer: a review. Eur Urol 2006;49:790-7
  • Pawinski A, Sylvester R, Kurth KH, et al. A combined analysis of EORTC and MRC randomized clinical trials for the prophylactic treatment of stage TaT1 bladder cancer. J Urol 1996;156:1934-40
  • Sylvester RJ, Oosterlinck W, Witjes JA. The schedule and duration of intravesical chemotherapy in patients with non muscle invasive bladder cancer: a systematic review of the published results of randomized clinical trials. Eur Urol 2008;53:709-19
  • Murta-Nascimento C, Schmitz-Dräger BJ, Zeegers MP, et al. Epidemiology of urinary bladder cancer: from tumour development to patient's death. World J Urol 2007;25:285-95
  • IARC. GLOBOCAN 2002. Available from: http://www-dep.iarc.fr [Accessed 6 December 2007]
  • Botteman M, Pashos C, Redaelli A, et al. The health economics of bladder cancer: a comprehensive review of the published literature. Pharmacoeconomics 2003;21:1315-30
  • Avritscher E, Cooksley CD, Grossman HB, et al. Clinical model of lifetime cost of treating bladder cancer and associated complications. Urology 2006;68:549-53
  • Hendricksen K, Witjes WPJ, Idema JG, et al. Comparison of three schedules of intravesical epirubicin in patients with non-muscle invasive bladder cancer. Eur Urol 2008;53(5):984-91
  • Witjes JA, van der Heijden AG, Vriesema JL, et al. Intravesical gemcitabine: a phase 1 and pharmacokinetic study. Eur Urol 2004;45:182-6
  • Laufer M, Ramalingam S, Schoenberg MP, et al. Intravesical gemcitabine therapy for superficial transitional cell carcinoma of the bladder: a phase I and pharmacokinetic study. J Clin Oncol 2003;21:697-703
  • Gontero P, Casetta G, Maso G, et al. Phase II study to investigate the ablative efficacy of intravesical administration of gemcitabine in intermediate-risk superficial bladder cancer (SBC). Eur Urol 2004;46:339-43
  • Dalbagni G, Russo P, Sheinfeld J, et al. Phase I trial of intravesical gemcitabine in bacillus Calmette-Guerin-refractory transitional-cell carcinoma of the bladder. J Clin Oncol 2002;20:3193-8
  • Dalbagni G, Russo P, Bochner B, et al. Phase II trial of intravesical gemcitabine in bacille Calmette-Guerin-refractory transitional cell carcinoma of the bladder. J Clin Oncol 2006;24:2729-34
  • Palou J, Carcas A, Segarra J, et al. Phase I pharmacokinetic study of a single intravesical instillation of gemcitabine administered immediately after transurethral resection plus multiple random biopsies in patients with superficial bladder cancer. J Urol 2004;172:485-8
  • Gardmark T, Carringer M, Beckman E, Malmstrom PU. Randomized phase II marker lesion study evaluating effect of scheduling on response to intravesical gemcitabine in recurrent Stage Ta urothelial cell carcinoma of the bladder. Urology 2005;66:527-30
  • Bartoletti R, Cai T, Gacci M, et al. Intravesical gemcitabine therapy for superficial transitional cell carcinoma: results of a phase II prospective multicenter study. Urology 2005;66:726-31
  • Colombo R, Da Pozzo LF, Lev A, et al. Neoadjuvant combined microwave induced local hyperthermia and topical chemotherapy versus chemotherapy alone for superficial bladder cancer. J Urol 1996;155:1227-32
  • Colombo R, Da Pozzo LF, Salonia A, et al. Multicentric study comparing intravesical chemotherapy alone and with local microwave hyperthermia for prophylaxis of recurrence of superficial transitional cell carcinoma. J Clin Oncol 2003;21:4270-6
  • Gofrit ON, Shapiro A, Pode D, et al. Combined local bladder hyperthermia and intravesical chemotherapy for the treatment of high-grade superficial bladder cancer. Urology 2004;63:466-71
  • van der Heijden AG, Kiemeney LA, Gofrit ON, et al. Preliminary European results of local microwave hyperthermia and chemotherapy treatment in intermediate or high risk superficial transitional cell carcinoma of the bladder. Eur Urol 2004;46:65-71
  • Brausi M, Campo B, Pizzocaro G, et al. Intravesical electromotive administration of drugs for treatment of superficial bladder cancer: a comparative phase II study. Urology 1998;51:506-9
  • Colombo R, Brausi M, Da Pozzo L, et al. Thermo-chemotherapy and electromotive drug administration of mitomycin C in superficial bladder cancer eradication. a pilot study on marker lesion. Eur Urol 2001;39:95-100
  • Di Stasi SM, Giannantoni A, Stephen RL, et al. Intravesical electromotive mitomycin C versus passive transport mitomycin C for high risk superficial bladder cancer: a prospective randomized study. J Urol 2003;170:777-82
  • Di Stasi SM, Giannantoni A, Giurioli A, et al. Sequential BCG and electromotive mitomycin versus BCG alone for high-risk superficial bladder cancer: a randomised controlled trial. Lancet Oncol 2006;7:43-51
  • Oostveen EA, Speckamp WN. Mitomycin analogs I. Indoloquinones as (potential) bisalkylating agents. Tetrahedron 1987;43:255-62
  • Hendriks HR, Pizao PE, Berger DP, et al. apaziquone, a novel bioreductive alkylating indoloquinone with preferential solid tumor activity and lack of bone marrow toxicity in preclinical models. Eur J Cancer 1993;29A:897-906
  • Loadman PM, Phillips RM, Lim LE, et al. Pharmacological properties of a new aziridinylbenzoquinone, RH1 (2,5-diaziridinyl-3-(hydroxymethyl)-6-methyl-1,4-benzoquinone), in mice. Biochem Pharmacol 2000;59:831-7
  • Choudry GA, Stewart PA, Double JA, et al. A novel strategy for NQO1 (NAD(P)H:quinone oxidoreductase, EC 1.6.99.2) mediated therapy of bladder cancer based on the pharmacological properties of apaziquone. Br J Cancer 2001;85:1137-46
  • Hoskin PJ, Sibtain A, Daley FM, et al. GLUT1 and CAIX as intrinsic markers of hypoxia in bladder cancer: relationship with vascularity and proliferation as predictors of outcome of ARCON. Br J Cancer 2003;89:1290-7
  • Cummings J, Spanswick VJ, Tomasz M, et al. Enzymology of mitomycin C metabolic activation in tumor tissue. Biochem Pharmacol 1998;56:405-14
  • Smitskamp-Wilms E, Hendriks HR, Peters GJ. Development, pharmacology, role of DT-diaphorase and prospects of the indoloquinone apaziquone. Gen Pharmacol 1996;27:421-9
  • Walton MI, Bibby MC, Double JA, et al. DT-diaphorase activity correlates with sensitivity to the indoloquinone apaziquone in mouse and human colon carcinomas. Eur J Cancer 1992;28A:1597-600
  • Plumb JA, Gerritsen M, Workman P. DT-Diaphorase protects cells from the hypoxic cytotoxicity of indoloquinone apaziquone. Br J Cancer 1994;70:1136-43
  • Workman P. Keynote address: bioreductive mechanisms. Int J Rad Oncol Biol Phys 1992;22:631-7
  • Bailey SM, Lewis AD, Patterson LH, et al. Involvement of NADPH: cytochrome P450 reductase in the activation of indoloquinone apaziquone to free radical and DNA damaging species. Biochem Pharmacol 2001;62:461-8
  • Jaffar M, Naylor MA, Lockyer SD, et al. 5-Substituted analogues of 3-hydroxymethyl-5-aziridinyl-1-methyl-2[1H-indole-4,7-dione]prop-2-en-1-ol (apaziquone, NSC 382459) and their regioisomers as hypoxia-selective agents: structure-cytotoxicity in vitro. Anticancer Drug Des 1998;13:105-23
  • Phillips RM, Naylor MA, Jaffar M, et al. Bioreductive activation of a series of indolequinones by human DT-diaphorase: Structure-activity relationships. J Med Chem 1999;42:4071-80
  • Bailey SM, Wyatt M, Friedlos F, et al. Involvement of DT-diaphorase in the DNA cross-linking and sequence selectivity of the indoloquinone bioreductive antitumor agent apaziquone. Br J Cancer 1997;76:1596-603
  • Maliepaard M, Wolfs A, Groot SE, et al. Indoloquinone apaziquone: DNA interstrand cross-linking upon reduction by DT-diaphorase or xanthine oxidase. Br J Cancer 1995;71:836-9
  • Walton MI, Smith PJ, Workman P. The role of NAD(P)H: quinone reductase (EC1.6.99.2,DT-diaphorase) in the reductive bioactivation of the novel indoloquinone antitumor agent apaziquone. Cancer Commun 1991;3:199-206
  • Siegel D, Gibson NW, Preusch PC, et al. Metabolism of mitomycin C by DT-diaphorase: role in mitomycin C-induced DNA damage and cytotoxicity in human colon carcinoma cells. Cancer Res 1990;50:7483-9
  • Workman P, Walton MI, Powis G, et al. DT-diaphorase: questionable role in Mitomycin resistance, but a target for novel bioreductive drugs? Br J Cancer 1989;60:800-2
  • Schlager JJ, Powis G. Mitomycin C is not metabolized by but is an inhibitor of human kidney NAD(P)H: (quinone-acceptor) oxidoreductase. Cancer Chemother Pharmacol 1988;22:126-30
  • Bailey SM, Suggett N, Walton MI, et al. Structure-activity relationships for DT-Diaphorase reduction of hypoxic cell directed agents: indoloquinones and diaziridinyl benzoquinones. Int J Rad Oncol Biol Phys 1992;22:649-53
  • Bailey SM, Friedlos F, Knox RJ, et al. Bioreductive activation of indoloquinone apaziquone: involvement of DT-diaphorase and DNA cross-linking. Ann Oncol 1992;3(Suppl 1):185
  • Robertson N, Stratford IJ, Houlbrook S, et al. The sensitivity of human tumor cells to quinone bioreductive drugs: What role for DT-diaphorase? Biochem Pharmacol 1992;44:409-12
  • Fitzsimmons SA, Workman P, Grever M, et al. Reductase enzyme expression across the National Cancer Institute tumor cell line panel – correlation with sensitivity to mitomycin C and apaziquone. J Natl Cancer Inst 1996;88:259-69
  • Phillips RM, Hulbert PB, Bibby MC, et al. In vitro activity of the novel indoloquinone EO-9 and the influence of pH on cytotoxicity. Br J Cancer 1992;65:359-64
  • Plumb JA, Gerritsen M, Milroy R, et al. Relative importance of DT-diaphorase and hypoxia in the bioactivation of apaziquone by human lung tumor cell lines. Int J Radiat Oncol Biol Phys 1994;29:295-9
  • Stratford IJ, Adams GE, Bremner JCM, et al. The assessment of bioreductive drug toxicity in vitro and in experimental tumors in vivo. In: Adams GE, Breccia A, Fielden EM, Wardman P, editors, Selective activation of drugs by redox processes. New York: Plenum Press; 1990. p. 203-12
  • Adams GE, Stratford IJ, Edwards HS, et al. Bioreductive drugs as post-irradiation sensitizers: comparison of dual function agents with SR 4233 and the mitomycin C analogue apaziquone. Int J Rad Oncol Biol Phys 1992;22:717-20
  • Bibby MC, Sleigh NR, Loadman PM, et al. Potentiation of apaziquone anti-tumor activity by hydralazine. Eur J Cancer 1993;29A:1033-5
  • Developmental Therapeutics Program, NCI. Available from: http://dtp.nci.nih.gov/dtpstandard/servlet/MeanGraphSummary?searchtype=NSC&chemnameboolean=and&outputformat=htmL& searchlist=26980%2C+382459 [accessed 29 February 2008]
  • Workman P, Binger M, Kooistra KL. Pharmacokinetics, distribution, and metabolism of the novel bioreductive alkylating indoloquinone apaziquone in rodents. Int J Radiat Oncol Biol Phys 1992;22:713-6
  • Spectrum Pharmaceuticals, pers. Commun.
  • Verweij J, Aamdal S, Schellens J, et al. Clinical studies with apaziquone, a new indoloquinone bioreductive alkylating cytotoxic agent. EORTC Early Clinical Trials Group. Oncol Res 1994;6:519-23
  • Vainchtein LD, Rosing H, Mirejovsky D, et al. Quantitative analysis of EO9 (apaziquone) and its metabolite EO5a in human plasma by high-performance liquid chromatography under basic conditions coupled to electrospray tandem mass spectrometry. J Mass Spectrom 2006;41:1268-76
  • Puri R, Palit V, Loadman PM, Flannigan M, et al. Phase I/II pilot study of intravesical apaziquone (apaziquone) for superficial bladder cancer. J Urol 2006;176:1344-8
  • Schellens JHM, Planting AST, van Acker BAC, et al. Phase I and pharmacologic study of the novel indoloquinone bioreductive alkylating cytotoxic drug apaziquone. J Natl Cancer Inst 1994;86:906-12
  • van der Heijden AG, Verhaegh G, Jansen CF, et al. Effect of hyperthermia on the cytotoxicity of 4 chemotherapeutic agents currently used for the treatment of transitional cell carcinoma of the bladder: an in vitro study. J Urol 2005;173:1375-80
  • van der Heijden AG, Moonen PM, Cornel EB, et al. Phase II marker lesion study with intravesical instillation of apaziquone for superficial bladder cancer: toxicity and marker response. J Urol 2006;176:1349-53
  • McLeod HL, Graham MA, Aamdal S, et al. Phase I pharmacokinetics and limited sampling strategies for the bioreductive alkylating drug apaziquone. EORTC Early Clinical Trials Group. Eur J Cancer 1996;32A:1518-22
  • Li D, Gan Y, Wientjes MG, et al. Distribution of DT-diaphorase and reduced nicotinamide adenine dinucleotide phosphate: cytochrome p450 oxidoreductase in bladder tissues and tumors. J Urol 2001;166:2500-5

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