Pharmacokinetics of recombinant human endostatin in rats

Yang, Xiao-Xia, Hu, Zen-Ping, Chan, Eli, Duan, Wei and Zhou, Shufeng 2006, Pharmacokinetics of recombinant human endostatin in rats, Current drug metabolism, vol. 7, no. 6, pp. 565-576.

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Title Pharmacokinetics of recombinant human endostatin in rats
Author(s) Yang, Xiao-Xia
Hu, Zen-Ping
Chan, Eli
Duan, WeiORCID iD for Duan, Wei
Zhou, Shufeng
Journal name Current drug metabolism
Volume number 7
Issue number 6
Start page 565
End page 576
Publisher Bentham Science Publishers Ltd
Place of publication Hilversum, The Netherlands
Publication date 2006-08
ISSN 1389-2002
Keyword(s) endostatin
allometric scaling
Summary The pharmacokinetics of recombinant human endostatin (rh-Endo) has not been established in the rat, although this species of animal is commonly used in the pharmacological studies of rh-Endo. This study aimed to investigate the pharmacokinetics, tissue distribution, and excretion of rh-Endo in rats. 125I-radiolabeled rh-Endo was administered to healthy rats by intravenous (i.v) bolus injection at 1.5, 4.5 and 13.5 mg/kg. The maximum plasma concentration (Cmax) and area under the plasma concentration versus time curve (AUC) of rh-Endo increased proportionally with the increase of the dosage. There were no significant differences in total body clearance (CL) and elimination half-life (t1/2beta) of rh-Endo among the three dosages used. A 93.5% and 2.2% of the radioactivity was recovered in the urine and feces, respectively, in bile-duct intact rats; whereas only 0.1% of the total radioactivity was excreted into the bile in bile-duct cannulated rats. rh-Endo was rapidly and widely distributed in the liver, kidneys, spleen and lungs. Furthermore, a significant allometric relationship between CL, but not volume of distribution (Vd) and t1/2beta of rh-Endo, and the body weight was observed across mouse, rat and monkey, with the predicted values in humans significantly lower than those observed in cancer patients. rh-Endo exhibited a linear pharmacokinetics in rats and it is mainly excreted through the urine.
Language eng
Field of Research 111599 Pharmacology and Pharmaceutical Sciences not elsewhere classified
HERDC Research category C1.1 Refereed article in a scholarly journal
Copyright notice ©2006, Bentham Science Publishers Ltd.
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Document type: Journal Article
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School of Medicine
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