Antitumor activity and pharmacokinetics of oral gimatecan on pediatric cancer xenografts

Massimo Zucchetti; Daniela Meco; Angela Maria Di Francesco; Tiziana Servidei; Valentina Patriarca; Gabriella Cusano; Maurizio D'Incalci; Daniele Forestieri; Claudio Pisano; Riccardo Riccardi

doi:10.1007/s00280-009-1201-8

Antitumor activity and pharmacokinetics of oral gimatecan on pediatric cancer xenografts

Massimo Zucchetti, Daniela Meco, Angela Maria Di Francesco, Tiziana Servidei, Valentina Patriarca, Gabriella Cusano, Maurizio D'Incalci, Daniele Forestieri, Claudio Pisano, Riccardo Riccardi

Università Cattolica del Sacro Cuore

Risultato della ricerca: Contributo in rivista › Articolo in rivista

7 Citazioni (Scopus)

Abstract

PURPOSE: This study compared the antitumor activity and the pharmacological profile 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 different schedules. We characterized its pharmacokinetic profile 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 plasma almost completely as the intact lactone form and showed substantial activity in all tumor models. Prolonged daily treatment with low doses of gimatecan produced significant tumor regression in all tumor xenografts. CONCLUSION: The antitumor activity and the promising pharmacological profile indicate gimatecan as an excellent candidate for clinical treatment of pediatric tumors.

Lingua originale	English
pagine (da-a)	635-641
Numero di pagine	7
Rivista	Cancer Chemotherapy and Pharmacology
Volume	66
DOI	https://doi.org/10.1007/s00280-009-1201-8
Stato di pubblicazione	Pubblicato - 2010

Keywords

antitumor activity
cancer xenografts
gimatecan
oral administration
pharmacokinetics

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title = "Antitumor activity and pharmacokinetics of oral gimatecan on pediatric cancer xenografts",

abstract = "PURPOSE: This study compared the antitumor activity and the pharmacological profile 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 different schedules. We characterized its pharmacokinetic profile 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 plasma almost completely as the intact lactone form and showed substantial activity in all tumor models. Prolonged daily treatment with low doses of gimatecan produced significant tumor regression in all tumor xenografts. CONCLUSION: The antitumor activity and the promising pharmacological profile indicate gimatecan as an excellent candidate for clinical treatment of pediatric tumors.",

keywords = "antitumor activity, cancer xenografts, gimatecan, oral administration, pharmacokinetics, antitumor activity, cancer xenografts, gimatecan, oral administration, pharmacokinetics",

author = "Massimo Zucchetti and Daniela Meco and {Di Francesco}, {Angela Maria} and Tiziana Servidei and Valentina Patriarca and Gabriella Cusano and Maurizio D'Incalci and Daniele Forestieri and Claudio Pisano and Riccardo Riccardi",

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doi = "10.1007/s00280-009-1201-8",

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journal = "Cancer Chemotherapy and Pharmacology",

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TY - JOUR

T1 - Antitumor activity and pharmacokinetics of oral gimatecan on pediatric cancer xenografts

AU - Zucchetti, Massimo

AU - Meco, Daniela

AU - Di Francesco, Angela Maria

AU - Servidei, Tiziana

AU - Patriarca, Valentina

AU - Cusano, Gabriella

AU - D'Incalci, Maurizio

AU - Forestieri, Daniele

AU - Pisano, Claudio

AU - Riccardi, Riccardo

PY - 2010

Y1 - 2010

N2 - PURPOSE: This study compared the antitumor activity and the pharmacological profile 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 different schedules. We characterized its pharmacokinetic profile 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 plasma almost completely as the intact lactone form and showed substantial activity in all tumor models. Prolonged daily treatment with low doses of gimatecan produced significant tumor regression in all tumor xenografts. CONCLUSION: The antitumor activity and the promising pharmacological profile indicate gimatecan as an excellent candidate for clinical treatment of pediatric tumors.

AB - PURPOSE: This study compared the antitumor activity and the pharmacological profile 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 different schedules. We characterized its pharmacokinetic profile 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 plasma almost completely as the intact lactone form and showed substantial activity in all tumor models. Prolonged daily treatment with low doses of gimatecan produced significant tumor regression in all tumor xenografts. CONCLUSION: The antitumor activity and the promising pharmacological profile indicate gimatecan as an excellent candidate for clinical treatment of pediatric tumors.

KW - antitumor activity

KW - cancer xenografts

KW - gimatecan

KW - oral administration

KW - pharmacokinetics

KW - antitumor activity

KW - cancer xenografts

KW - gimatecan

KW - oral administration

KW - pharmacokinetics

UR - http://hdl.handle.net/10807/16409

U2 - 10.1007/s00280-009-1201-8

DO - 10.1007/s00280-009-1201-8

M3 - Article

SN - 0344-5704

VL - 66

SP - 635

EP - 641

JO - Cancer Chemotherapy and Pharmacology

JF - Cancer Chemotherapy and Pharmacology

ER -

Antitumor activity and pharmacokinetics of oral gimatecan on pediatric cancer xenografts

Abstract

Keywords

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