119
Views
34
CrossRef citations to date
0
Altmetric
Antimicrobial Chemotherapy

Clinical Phase I and Pharmacology Study of Gemcitabine (2', 2'-Difluorodeoxycytidine) Administered in a Two-Weekly Schedule

Pages 212-221 | Published online: 18 Jul 2013

References

  • Hertel LW, Soder GB, Kroin JS, et al. Evaluation of the antitumor activity of a (2',2'-difluoro-2'-deoxycytidine). Cancer Res 1990; 50: 4417-4422.
  • Merriman RL, Hertel LW, Schultz RM, et al. Comparison of the antitumor activity of gemcitabine and ara-C in a panel of human breast, colon, lung and pancreatic xenograft models. Invest New Drugs 1996; 14: 243–247.
  • Braakhuis BJ, van Dongen GAMS, Vermorken JB, Snow GB. Preclinical in vivo activity of 2',2'-difluorodeoxycy-tidine (Gemcitabine) against head and neck cancer. Cancer Res. 1991; 51: 211–214.
  • Boven E, Schipper H, Erkelens CAM, Hatty SA, Pinedo HM. The influence of the schedule and the dose of gemcitabine on the anti-tumour efficacy in experimental human cancer. Br J Cancer 1993; 68: 52–56.
  • Braakhuis BJ, Ruiz van Haperen VW, Boven E, Veerman G, Peters GJ. Schedule-dependent antitumor effect of gemcitabine in in vivo model system. Semin Oncol 1995; 22: 42–46.
  • Heinemann V, Hertel LW, Grindey GB, Plunkett W. Comparison of the cellular pharmacokinetics and toxicity of 2',2'-difluorodeoxycytidine and 1 D arabinofuranosylcyto-sine. Cancer Res 1988; 48: 4024-4031.
  • Bergman AM, Pinedo HM, Peters GJ. Determinants of resistance to 2',2'-difluorodeoxycytidine (gemcitabine). DrugResist Updat 2002; 5: 19–33.
  • Mackey JR, Mani RS, Selner M, et al. Functional nucleo-side transporters are required for gemcitabine influx and mani-festation of toxicity in cancer cell lines. Cancer Res 1998; 58: 4349–4357.
  • Mackey JR, Yao SY, Smith KM, et al. Gemcitabine transport in xenopus oocytes expressing recombinant plasma membrane mammalian nucleoside transporters. J Natl Cancer Inst 1999; 91: 1876-1881.1°
  • Van Moorsel CJ, Bergman AM, Veerman G, et al. Differential effects of gemcitabine on ribonucleotide pools of twenty-one solid tumour and leukaemia cell lines. Biochim Biophys Acta 2000; 1474: 5–12.
  • Bergman AM, Pinedo HM, Jongsma AP, et al. Decreased resistance to gemcitabine (2',2'-difluorodeoxyciti-dine) of cytosine arabinoside-resistant myeloblastic murine and rat leukemia cell lines: role of altered activity and substrate specificity of deoxycytidine kinase. Biochem Pharmacol 1999; 57: 397-406.
  • Ruiz van Haperen VWT, Veerman G, Boven E, Noordhuis P, Vermorken JB, Peters GJ. Schedule depen-dence of sensitivity to 2',2'-difluorodeocytidine (Gemcitabine) in relation to accumulation and retention of its triphosphate in solid tumour cell lines and solid tumours. Biochem Pharmacol 1994; 48: 1327-1339.
  • Shewach DS, Hahn TM, Chang E, Hertel LW, Lawrence TS. Metabolism of 2',2'-difluoro-2'-deoxycytidine and radiation sensitization of human colon carcinoma cells. Cancer Res 1994; 54: 3218-3223.
  • Smitskamp-Wilms E, Pinedo HM, Veerman G, Ruiz van Haperen VW, Peters GJ. Postconfluent multilayered cell line cultures for selective screening of gemcitabine. Eur J Cancer 1994; 34 : 921–926.
  • Ruiz van Haperen VWT, Veerman G, Vermorken JB, Peters GJ. 2',2'- Difluoro-deoxycytidine incorporation into RNA and DNA of tumour cell lines. Biochem Pharmacol 1993; 46: 762–766.
  • Abbruzzese JL, Grunewald R, Weeks EA, et al. A Phase I clinical, plasma, and cellular pharmacology study of Gemcitabine. J Clin Oncol 1991; 9: 491–498.
  • Storniolo AM, Allerheiligen SR, Pearce HL. Preclinical, pharmacologic, and phase I studies of gemcitabine. Semin Oncol 1997; 24 (2 Suppl 7): 2-7.
  • Grunewald R, Abbruzzese JL, Tarassoff P, Plunkett W. Saturation of 2',2'-difluorodeoxycytidine 5'-triphosphate accu-mulation by mononuclear cells during a Phase I trial of gemc-itabine. Cancer Chemother Pharmacol 1991; 27: 258–262.
  • Grunewald R, Kantarjian H, Du M, Faucher K, Tarassoff P, Plunkett W. Gemcitabine in leukemia: A phase I clinical, plasma and cellular pharmacology study. J Clin Oncol 1992; 10: 406–413.
  • Vermorken JB, Guastalla JP, Hatty SR, et al. Phase I study of gemcitabine using a once every 2 weeks schedule. Br J Cancer 1997; 76: 1489-1493.
  • Rothenberg ML, Sharma A, Weiss GR, et al. Phase I trial of paclitaxel and gemcitabine administered every two weeks in patients with refractory solid tumors. Ann Oncol 1998; 9: 733–738.
  • Freeman KB, Anliker S, Hamilton M, et al. Validated assays for the determination of gemcitabine in human plasma and urine using high-performance liquid chromatography with ultraviolet detection. J Chromatogr B Biomed 1995; 665: 171–181.
  • Veerman G, Ruiz van Haperen VW, Vermorken JB, Noordhuis P, Braakhuis BJ, Pinedo HM, Peters GJ. Antitumor activity of prolonged as compared with bolus administration of 2',2'-difluorodeoxycytidne in vivo against murine colon tumors. Cancer Chemother Pharmacol 1996; 38: 335–342.
  • Edzes HT, Peters GJ, Noordhuis P, Vermorken JB. Determination of the antimetabolite Gemcitabine (2',2'-difluo-ro-2'-deoxycytidine) and of 2',2'-difluoro-2'- deoxyuridine by 19F nuclear magnetic resonance spectroscopy. Anal Biochem 1993; 214: 25–30.
  • Peters GJ, Schwartsmann G, Nadal JC, Laurensse EJ, Van Groeningen CJ, Van der Vijgh WJ, Pinedo HM. In vivo inhibition of the pyrimidine de novo enzyme dihydroorotic acid dehydrogenase by brequinar sodium (DUP-785; NSC 368390) in mice and patients. Cancer Res 1990; 50: 4644-4649.
  • Ruiz van Haperen VWT, Veerman G, Eriksson S, et al. Development and molecular characterization of a 2',2'-difluo-rodeoxycytidine-resistant variant of the human overian carci-noma cell line A2780. Cancer Res 1994; 54: 4138-4143.
  • Schwartsmann G, Van der Vijgh WJ, Van Hennik MB, et al. Pharmacokinetics of Brequinar sodium (NSC 368390) in patients with solid tumors during a phase I study. Eur J Cancer Clin Oncol 1989; 25 : 1675-1681.
  • Van der Wilt CL, Kroep JR, Loves WJ, Rots MG, Van Groeningen CJ, Kaspers GJ, Peters GJ. Expression of deoxy-cytidine kinase in leukaemic cells compared with solid tumour cell lines, liver metastases and normal liver. Eur J Cancer 2003; 39: 691–697.
  • Ruiz van Haperen VW, Veerman G, Braakhuis BJ, Vermorken JB, Boven E, Leyva A, Peters GJ. Deoxycytidine kinase and deoxycytidine deaminase activities in human tumour xenografts. Eur J Cancer 1993; 29A: 2132–2137.
  • Bengala C, Guarneri V, Giovannetti E, et al. Prolonged fixed doxe rate infusion of gemcitabine with autologous haemopoietic support in advanced pancreatic adenocarcino-ma. Br J Cancer 2005; 93: 35–40.
  • De Lange SM, Van der Born K, Kroep JR, et al. No evidence of gemcitabine accumulation during weekly adminis-tration. Eur J Clin Pharmacol 2005; 61: 843–849.
  • Periclou AP, Avramis VI. NONMEM population phar-macokinetic studies of cytosine arabinoside after high-dose and after loading bolus followed by continuous infusion of the drug in pediatric patients with leukemias. Cancer Chemother Pharmacol 1996; 39: 42–50.
  • Peters GJ, Schornagel JH, Milano GA. Clinical phar-macokinetics of anti-metabolites. Cancer Surv 1993; 17: 123–156.
  • Gilbert JA, Salavaggione OE, Ji Y, et al. Gemcitabine pharmacogenomics: Cytidine deaminase and deoxycytidylate deaminase gene resequencing and funtional genomics. Clin Cancer Res. 2006; 12: 1794–1803.
  • Van Groeningen CJ, Leyva A, O'Brien AM, Gall HE, Pinedo HM. Phase I and pharmacokinetic study of 5-aza-2'-deoxycytidine (NSC 127716) in cancer patients. Cancer Res 1986; 46: 4831-4836.
  • Liliemark J, Juliusson G. On the pharmacokinetics of 2-chloro-2'-deoxyadenosine in humans. Cancer Res 1991; 51: 5570-5572.
  • Bergman AM, Giaccone G, Van Moorsel CJ, Mauritz R, Noordhuis P, Pinedo HM, Peters GJ. Cross-resistance in the 2',2'-difluorodeoxycytidine (gemcitabine)-resistant human ovarian cancer cell line AG6000 to standard and investigation-al drugs. Eur J Cancer 2001; 36: 1974-1983.
  • Wang L, Munch-Petersen B, Herrstrom Sjoberg A, Hellman U, Bergman T, Jornvall H, Eriksson S. Human thymidine kinase 2: molecular cloning and characterisation of the enzyme activity with antiviral and cytostatic nucleoside sub-strates. FESS Lett 1999; 443: 170–174.
  • Arner ES, Eriksson S. Mammalian deoxyribonucleoside kinases. Pharmacol Ther 1995; 67: 155–186.
  • Ruiz van Haperen VWT, Veerman G, Vermorken JB, Pinedo HM, Peters GJ. Regulation of phosphorylation of deoxycytidine and 2',2'-difluorodeoxycytidine (Gemcitabine); effects of cytidine 5'-triphosphate and uridine 5'-triphosphate in relation to chemosensitivity for 2',2'-difluorodeoxycytidine.Biochem Pharmacol 1996; 51: 911–918.
  • Shewach DS, Reynolds KK, Hertel L. Nucleotide speci-ficity of human deoxycytidine kiinase. Mol Pharmacol 1992; 42: 518–524.
  • Kroep JR, Giaccone G, Voorn DA, et al. Gemcitabine and paclitaxel: pharmacokinetic and pharmacodynamic inter-actions in patients with non-small-cell lung cancer. J Clin Oncol 1999; 17: 2190–2197.
  • Van Moorsel CJ, Kroep JR, Pinedo HM, et al. Pharmacokinetic schedule finding study of the combination of gemcitabine and cisplatin in patients with solid tumors. Ann Oncol 1999; 10: 441–448.
  • Peters GJ, Veerkamp JH. Purine and pyrimidine metabolism in peripheral blood lymphocytes (Review). Int J Biochem 1983; 15: 115–123.
  • Bianchi V, Spychala J. Mammalian 5'-nucleotidases. J Biol Chem 2003; 278: 46195–46198.
  • Gandhi V, Plunkett W, Du M, Ayres M, Estey EH. Prolonged infusion of gemcitabine: clinical and pharmacody-namic studies during a phase I trial in relapsed acute myeloge-nous leukemia. J Clin Oncol 2002; 20: 665–673.
  • Tempero M, Plunkett W, Ruiz van Haperen V, Hainsworth J, Hochster H, Lenzi R, Abbruzzese J. Randomized phase II comparison of dose-intense gemcitabine: thirty-minute infusion and fixed dose rate infusion in patients with pancreatic adenocarcinoma. J Clin Oncol 2003; 21: 3402-3408.
  • Huang P, Chubb S, Hertel LW, Grindey GB, Plunkett W. Action of 2',2'-difluorodeoxycytidine on DNA Synthesis. Cancer Res 1991; 51: 6110-6117.

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.