Gimatecan - CAS 292618-32-7
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Not Intended for Therapeutic Use. For research use only.
Gimatecan  is an orally bioavailable, semi-synthetic lipophilic analogue of camptothecin, a quinoline alkaloid extracted from the Asian tree Camptotheca acuminate, with potential antineoplastic and antiangiogenic activities. Gimatecan binds to and inhibits the activity of topoisomerase I, stabilizing the cleavable complex of topoisomerase I-DNA, which inhibits the religation of single-stranded DNA breaks generated by topoisomerase I; lethal double-stranded DNA breaks occur when the topoisomerase I-DNA complex is encountered by the DNA replication machinery, DNA replication is disrupted, and the tumor cell undergoes apoptosis. Although the mechanism of its antiangiogenic activity has yet to be full elucidated, this agent may inhibit endothelial cell migration, tumor neovascularization, and the expression of proangiogenic basic fibroblast growth factor (bFGF).
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LBQ707; STI481;
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Novartis Pharmaceuticals and Sigma-Tau Research
1.Antitumor activity and pharmacokinetics of oral gimatecan on pediatric cancer xenografts.
Zucchetti M1, Meco D, Di Francesco AM, Servidei T, Patriarca V, Cusano G, D'Incalci M, Forestieri D, Pisano C, Riccardi R. Cancer Chemother Pharmacol. 2010 Sep;66(4):635-41. doi: 10.1007/s00280-009-1201-8. Epub 2009 Dec 20.
PURPOSE: This study compared the antitumor activity and the pharmacological profile of gimatecan given orally and irinotecan (CPT-11) on pediatric tumor xenografts.
2.Clinical pharmacokinetics of the new oral camptothecin gimatecan: the inter-patient variability is related to alpha1-acid glycoprotein plasma levels.
Frapolli R1, Zucchetti M, Sessa C, Marsoni S, Viganò L, Locatelli A, Rulli E, Compagnoni A, Bello E, Pisano C, Carminati P, D'Incalci M. Eur J Cancer. 2010 Feb;46(3):505-16. doi: 10.1016/j.ejca.2009.11.006. Epub 2009 Dec 16.
AIM OF THE STUDY: To determine the pharmacokinetics of gimatecan, a camptothecin with a lipophilic substitution in position 7, given orally to patients participating in the phase I study.
3.DNA damage persistence as determinant of tumor sensitivity to the combination of Topo I inhibitors and telomere-targeting agents.
Biroccio A1, Porru M, Rizzo A, Salvati E, D'Angelo C, Orlandi A, Passeri D, Franceschin M, Stevens MF, Gilson E, Beretta G, Zupi G, Pisano C, Zunino F, Leonetti C. Clin Cancer Res. 2011 Apr 15;17(8):2227-36. doi: 10.1158/1078-0432.CCR-10-3033. Epub 2011 Feb 25.
PURPOSE: We previously reported that the G-quadruplex (G4) ligand RHPS4 potentiates the antitumor activity of camptothecins both in vitro and in tumor xenografts. The present study aims at investigating the mechanisms involved in this specific drug interaction.
4.A phase II trial of oral gimatecan for recurrent glioblastoma.
Hu J1, Wen PY, Abrey LE, Fadul CE, Drappatz J, Salem N, Supko JG, Hochberg F. J Neurooncol. 2013 Feb;111(3):347-53. doi: 10.1007/s11060-012-1023-0. Epub 2012 Dec 12.
Gimatecan is a lipophilic oral camptothecin analogue with preclinical activity in glioma models. We conducted a multicenter phase II trial to evaluate the efficacy of gimatecan in adults with recurrent glioblastoma. Eligibility criteria included ≤1 prior treatment for recurrent disease, age ≥18, Eastern Cooperative Oncology Group performance status 0-1, and normal organ function. Patients taking enzyme-inducing anti-seizure medications were excluded. Gimatecan 1.22 mg/m(2) was given orally once daily for 5 consecutive days during each 28-day cycle. The primary endpoint was progression-free survival at 6 months. A Simon 2-stage optimal design was used in which 19 patients were evaluated in the 1st stage, with an additional 36 patients accrued if >4 patients in stage 1 achieved PFS at 6 months. 29 patients were enrolled in the study, with median age of 58 years (range, 25-77 years); 58.6 % female. All patients received prior surgery, radiation therapy, and at least one chemotherapy regimen.
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CAS 292618-32-7 Gimatecan

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