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Titolo:
Antitumor efficacy, pharmacokinetics, and biodistribution of NX 211: A low-clearance liposomal formulation of lurtotecan
Autore:
Emerson, DL; Bendele, R; Brown, E; Chiang, SM; Desjardins, JP; Dihel, LC; Gill, SC; Hamilton, M; LeRay, JD; Moon-McDermott, L; Moynihan, K; Richardson, FC; Tomkinson, B; Luzzio, MJ; Baccanari, D;
Indirizzi:
Gilead Sci Inc, Boulder, CO 80301 USA Gilead Sci Inc Boulder CO USA 80301Gilead Sci Inc, Boulder, CO 80301 USA Glaxo Wellcome Inc, Res Inst, Res Triangle Pk, NC 27709 USA Glaxo WellcomeInc Res Triangle Pk NC USA 27709 Triangle Pk, NC 27709 USA
Titolo Testata:
CLINICAL CANCER RESEARCH
fascicolo: 7, volume: 6, anno: 2000,
pagine: 2903 - 2912
SICI:
1078-0432(200007)6:7<2903:AEPABO>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
TOPOISOMERASE-I INHIBITOR; SOLID TUMORS; PHASE-I; CAMPTOTHECIN ANALOGS; THERAPEUTIC ACTIVITY; STEALTH LIPOSOMES; DAUNORUBICIN; TOPOTECAN; GI147211; ENCAPSULATION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
41
Recensione:
Indirizzi per estratti:
Indirizzo: Emerson, DL Gilead Sci Inc, 2860 Wilderness Pl, Boulder, CO 80301 USA Gilead Sci Inc 2860 Wilderness Pl Boulder CO USA 80301 301 USA
Citazione:
D.L. Emerson et al., "Antitumor efficacy, pharmacokinetics, and biodistribution of NX 211: A low-clearance liposomal formulation of lurtotecan", CLIN CANC R, 6(7), 2000, pp. 2903-2912

Abstract

Lurtotecan is a clinically active water-soluble camptothecin analogue thathas been formulated into a low-clearance unilamellar liposome, NX 211, Comparative studies between free drug and NX 211 have been performed assessingpharmacokinetics in nude mice, tissue distribution in tumor-bearing mice, and antitumor efficacy in xenografts, Compared with lurtotecan, NX 211 demonstrated a significant increase in plasma residence time and a subsequent 1500-fold increase in the plasma area under the drug concentration curve. The volume of distribution was also greatly restricted, suggesting altered tissue distribution. Evaluation of tissues 24 h after administration of either [C-14]NX 211 Or [C-14]lurtotecan to ES-2 tumor-bearing mice demonstrated a 40-fold increase in radiolabeled compound in the tumors of NX 211-treatedmice compared with mice treated with lurtotecan, In single-dose efficacy studies, NX 211 produced a consistent 3-fold or greater increase in therapeutic index compared with lurtotecan in both the KB and ES-2 xenograft models. When compared at equitoxic levels in repeat-dose efficacy studies, NX 211generated durable cures lasting >60 days and a 28-fold increase in log,, cell kill, compared with lurtotecan and topotecan, respectively, Together, these data demonstrate that NX 211 has significant therapeutic advantage over Lurtotecan and that the improved antitumor activity is consistent with increased exposure and enhanced drug delivery to tumor sites.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/09/20 alle ore 15:49:13