178
Views
24
CrossRef citations to date
0
Altmetric
Drug Evaluations

Diflomotecan, a promising homocamptothecin for cancer therapy

&
Pages 69-75 | Published online: 21 Nov 2008

Bibliography

  • Pizzolato JF, Saltz LB. The camptothecins. Lancet 2003;361:2235-42
  • Hsiang YH, Liu LF. Identification of mammalian DNA topoisomerase I as an intracellular target of the anticancer drug camptothecin. Cancer Res 1988;48:1722-6
  • Hertzberg RP, Caranfa MJ, Hecht SM. On the mechanism of topoisomerase I inhibition by camptothecin: evidence for binding to an enzyme-DNA complex. Biochemistry 1989;28:4629-38
  • Kjeldsen E, Svejstrup JQ, Gromova II, et al. Camptothecin inhibits both the cleavage and religation reactions of eukaryotic DNA topoisomerase I. J Mol Biol 1992;228:1025-30
  • Giovanella BC, Stehlin JS, Wall ME, et al. DNA topoisomerase I–targeted chemotherapy of human colon cancer in xenografts. Science 1989;246:1046-8
  • Husain I, Mohler JL, Seigler HF, Besterman JM. Elevation of topoisomerase I messenger RNA, protein, and catalytic activity in human tumors: demonstration of tumor-type specificity and implications for cancer chemotherapy. Cancer Res 1994;54:539-46
  • Moertel CG, Schutt AJ, Reitemeier RJ, Hahn RG. Phase II study of camptothecin (NSC-100880) in the treatment of advanced gastrointestinal cancer. Cancer Chemother Rep 1972;56:95-101
  • ten Bokkel HW, Gore M, Carmichael J, et al. Topotecan versus paclitaxel for the treatment of recurrent epithelial ovarian cancer. J Clin Oncol 1997;15:2183-93
  • Long HJ 3rd, Bundy BN, Grendys EC Jr, et al. Randomized Phase III trial of cisplatin with or without topotecan in carcinoma of the uterine cervix: a Gynecologic Oncology Group Study. J Clin Oncol 2005;23:4626-33
  • Noda K, Nishiwaki Y, Kawahara M, et al. Irinotecan plus cisplatin compared with etoposide plus cisplatin for extensive small-cell lung cancer. N Engl J Med 2002;346:85-91
  • Cunningham D, Pyrhonen S, James RD, et al. Randomised trial of irinotecan plus supportive care versus supportive care alone after fluorouracil failure for patients with metastatic colorectal cancer. Lancet 1998;352:1413-8
  • Perez EA, Hillman DW, Mailliard JA, et al. Randomized Phase II study of two irinotecan schedules for patients with metastatic breast cancer refractory to an anthracycline, a taxane, or both. J Clin Oncol 2004;22:2849-55
  • Vredenburgh JJ, Desjardins A, Herndon JE, et al. Bevacizumab plus irinotecan in recurrent glioblastoma multiforme. J Clin Oncol 2007;25:4722-9
  • Burkart C, Bokemeyer C, Klump B, et al. A Phase II trial of weekly irinotecan in cisplatin-refractory esophageal cancer. Anticancer Res 2007;27:2845-8
  • Burke TG. Chemistry of the camptothecins in the bloodstream. Drug stabilization and optimization of activity. Ann NY Acad Sci 1996;803:29-31
  • Burke TG, Mi Z. Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin. J Med Chem 1993;36:2580-2
  • Lavergne O, Lesueur-Ginot L, Pla Rodas F, et al. BN 80245: an E-ring modified camptothecin with potent antiproliferative and topoisomerase I inhibitory activities. Bioorg Med Chem Lett 1997;7:2235-8
  • Lesueur-Ginot L, Demarquay D, Kiss R, et al. Homocamptothecin, an E-ring modified camptothecin with enhanced lactone stability, retains topoisomerase I-targeted activity and antitumor properties. Cancer Res 1999;59:2939-43
  • Bailly C, Lansiaux A, Dassonneville L, et al. Homocamptothecin, an E-ring-modified camptothecin analogue, generates new topoisomerase I-mediated DNA breaks. Biochemistry 1999;38:15556-63
  • Chauvier D, Morjani H, Manfait M. Homocamptothecin-daunorubicin association overcomes multidrug-resistance in breast cancer MCF7 cells. Breast Cancer Res Treat 2002;73:113-25
  • Larsen AK, Gilbert C, Chyzak G, et al. Unusual potency of BN 80915, a novel fluorinated E-ring modified camptothecin, toward human colon carcinoma cells. Cancer Res 2001;61:2961-7
  • Demarquay D, Huchet M, Coulomb H, et al. The homocamptothecin BN 80915 is a highly potent orally active topoisomerase I poison. Anticancer Drugs 2001;12:9-19
  • Lavergne O, Demarquay D, Bailly C, et al. Topoisomerase I-mediated antiproliferative activity of enantiomerically pure fluorinated homocamptothecins. J Med Chem 2000;43:2285-9
  • Lavergne O, Lesueur-Ginot L, Pla RF, et al. Homocamptothecins: synthesis and antitumor activity of novel E-ring-modified camptothecin analogues. J Med Chem 1998;41:5410-9
  • Philippart P, Harper L, Chaboteaux C, et al. Homocamptothecin, an E-ring-modified camptothecin, exerts more potent antiproliferative activity than other topoisomerase I inhibitors in human colon cancers obtained from surgery and maintained in vitro under histotypical culture conditions. Clin Cancer Res 2000;6:1557-62
  • Lansiaux A, Facompre M, Wattez N, et al. Apoptosis induced by the homocamptothecin anticancer drug BN80915 in HL-60 cells. Mol Pharmacol 2001;60:450-61
  • Liao Z, Robey RW, Guirouilh-Barbat J, et al. Reduced expression of DNA topoisomerase I in SF295 human glioblastoma cells selected for resistance to homocamptothecin and diflomotecan. Mol Pharmacol 2008;73:490-7
  • Bates SE, Medina-Perez WY, Kohlhagen G, et al. ABCG2 mediates differential resistance to SN-38 (7-ethyl-10-hydroxycamptothecin) and homocamptothecins. J Pharmacol Exp Ther 2004;310:836-42
  • Lavergne O, Demarquay D, Kasprzyk PG, et al. Homocamptothecins: E-ring modified CPT analogues. Ann NY Acad Sci 2000;922:100-11
  • Lansiaux A, Bras-Goncalves RA, Rosty C, et al. Topoisomerase I-DNA covalent complexes in human colorectal cancer xenografts with different p53 and microsatellite instability status: relation with their sensitivity to CTP-11. Anticancer Res 2001;21:471-6
  • De Cesare M, Zunino F, Pace S, et al. Efficacy and toxicity profile of oral topotecan in a panel of human tumour xenografts. Eur J Cancer 2000;36:1558-64
  • Schaefer PL, Marks RS, Mahoney MR, et al. Randomized Phase II study of daily versus continuous-infusion schedules of topotecan in the treatment of extensive-stage small cell lung cancers. Am J Clin Oncol 2003;26:236-40
  • Gelderblom H, Salazar R, Verweij J, et al. Phase I pharmacological and bioavailability study of oral diflomotecan (BN80915), a novel E-ring-modified camptothecin analogue in adults with solid tumors. Clin Cancer Res 2003;9:4101-7
  • Troconiz IF, Garrido MJ, Segura C, et al. Phase I dose-finding study and a pharmacokinetic/pharmacodynamic analysis of the neutropenic response of intravenous diflomotecan in patients with advanced malignant tumours. Cancer Chemother Pharmacol 2006;57:727-35
  • Scott L, Soepenberg O, Verweij J, et al. A multicentre Phase I and pharmacokinetic study of BN80915 (diflomotecan) administered daily as a 20-min intravenous infusion for 5 days every 3 weeks to patients with advanced solid tumours. Ann Oncol 2007;18:569-75
  • Lesimple T, Fumoleau P, Lortholary A, et al. First results of diflomotecan, a new topoisomerase inhibitor, as oral soft-gel capsules in a Phase I dose escalation study in patients with advanced malignant solid tumours. Eur j cancer suppl 2004;153-4
  • Loos WJ, Gelderblom H, Sparreboom A, et al. Inter- and intrapatient variability in oral topotecan pharmacokinetics: implications for body-surface area dosage regimens. Clin Cancer Res 2000;6:2685-9
  • Xie R, Mathijssen RH, Sparreboom A, et al. Clinical pharmacokinetics of irinotecan and its metabolites: a population analysis. J Clin Oncol 2002;20:3293-301
  • Mathijssen RH, Verweij J, de Jonge MJ, et al. Impact of body-size measures on irinotecan clearance: alternative dosing recommendations. J Clin Oncol 2002;20:81-7
  • Mould DR, Holford NH, Schellens JH, et al. Population pharmacokinetic and adverse event analysis of topotecan in patients with solid tumors. Clin Pharmacol Ther 2002;71:334-48
  • Schellens JH, Heinrich B, Lehnert M, et al. Population pharmacokinetic and dynamic analysis of the topoisomerase I inhibitor lurtotecan in Phase II studies. Invest New Drugs 2002;20:83-93
  • Piscitelli SC, Rodvold KA, Rushing DA, et al. Pharmacokinetics and pharmacodynamics of doxorubicin in patients with small cell lung cancer. Clin Pharmacol Ther 1993;53:555-61
  • Gelderblom HA, de Jonge MJ, Sparreboom A, et al. Oral topoisomerase 1 inhibitors in adult patients: present and future. Invest New Drugs 1999;17:401-15
  • Sparreboom A, Gelderblom H, Marsh S, et al. Diflomotecan pharmacokinetics in relation to ABCG2 421C>A genotype. Clin Pharmacol Ther 2004;76:38-44
  • Ipsen, data on file. 2008. Ref Type: Personal Communication
  • Teicher BA. Next generation topoisomerase I inhibitors: Rationale and biomarker strategies. Biochem Pharmacol 2008;75:1262-71
  • Liu G, Franssen E, Fitch MI, et al. Patient preferences for oral versus intravenous palliative chemotherapy. J Clin Oncol 1997;15:110-5
  • Pommier Y. Topoisomerase I inhibitors: camptothecins and beyond. Nat Rev Cancer 2006;6:789-802

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.