2009
DOI: 10.1007/s00280-009-1201-8
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Antitumor activity and pharmacokinetics of oral gimatecan on pediatric cancer xenografts

Abstract: Purpose This study compared the antitumor activity and the pharmacological proWle of gimatecan given orally and irinotecan (CPT-11) on pediatric tumor xenografts. Experimental design Gimatecan was tested in two neuroblastoma cell lines (SK-N-DZ and SK-N-(BE)2c) and on TE-671 rhabdomyosarcoma cells using two diVerent schedules. We characterized its pharmacokinetic proWle in nude mice bearing human SK-N-DZ and TE-671 cell lines. Results Gimatecan appears to have high plasma disposition. The drug was present in p… Show more

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Cited by 6 publications
(4 citation statements)
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“…As described for Ewing sarcoma ( Section 2.4.1.5 ), namitecan produced RD/TE-671 RMS xenograft regression at low doses and additive effects with the antiangiogenic agents bevacizumab and sunitinib [252] , while Genz-644282 induced complete responses in Rh18 and Rh28 ARMS and Rh30 ERMS xenografts [216] . Prolonged daily treatment with low doses of gimatecan also produced significant tumor regression in RD/TE-671 RMS tumor xenografts [148] .…”
Section: Relevant Biomarkers In Childhood Malignancies and Novel Thermentioning
confidence: 88%
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“…As described for Ewing sarcoma ( Section 2.4.1.5 ), namitecan produced RD/TE-671 RMS xenograft regression at low doses and additive effects with the antiangiogenic agents bevacizumab and sunitinib [252] , while Genz-644282 induced complete responses in Rh18 and Rh28 ARMS and Rh30 ERMS xenografts [216] . Prolonged daily treatment with low doses of gimatecan also produced significant tumor regression in RD/TE-671 RMS tumor xenografts [148] .…”
Section: Relevant Biomarkers In Childhood Malignancies and Novel Thermentioning
confidence: 88%
“…Similarly, the combination of topotecan with vincristine and doxorubicin induced objective responses in a small cohort of 6 patients with refractory or recurrent RMS, and was well tolerated [282] . More recent in vivo studies also indicated that namitecan, Genz-644282 and gimatecan were highly active in a number of RMS xenograft models [148] , [216] , [252] . As described for Ewing sarcoma ( Section 2.4.1.5 ), namitecan produced RD/TE-671 RMS xenograft regression at low doses and additive effects with the antiangiogenic agents bevacizumab and sunitinib [252] , while Genz-644282 induced complete responses in Rh18 and Rh28 ARMS and Rh30 ERMS xenografts [216] .…”
Section: Relevant Biomarkers In Childhood Malignancies and Novel Thermentioning
confidence: 95%
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