地拉罗斯铁螯合物

Deferasirox Fe3+ chelate 是口服的铁螯合剂。

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Deferasirox是美国为此目的批准的第一种口服药物。地拉罗司的半衰期为8至16小时,每天一次给药。两个地拉索罗克分子能够结合1个铁原子,随后通过粪便排泄消除。其低分子量和高亲脂性允许药物口服,不像去铁胺,必须通过IV途径(静脉内输注)给药。与去铁酮一起,地拉罗司似乎能够从细胞(心肌细胞和肝细胞)中去除铁以及从血液中去除铁。

[1]. Yang LP, Keam SJ, Keating GM. Deferasirox : a review of its use in the management of transfusional chronic iron overload. Drugs. 2007;67(15):2211-30.

[2]. Kontoghiorghes GJ. Introduction of higher doses of deferasirox: better efficacy but not effective iron removal from the heart and increased risks of serious toxicities. Expert Opin Drug Saf. 2010 Jul;9(4):633-41.

[3]. Galanello R, Campus S, Origa R. Deferasirox: pharmacokinetics and clinical experience. Expert Opin Drug Metab Toxicol. 2012 Jan;8(1):123-34.

[4]. Donnelly JP, Lahav M. Deferasirox as adjunctive therapy for mucormycosis. J Antimicrob Chemother. 2012 Mar;67(3):519-20.

[5]. Lui GY, Obeidy P, Ford SJ et al. The Iron Chelator, Deferasirox, as a Novel Strategy for Cancer Treatment: Oral Activity Against Human Lung Tumor Xenografts and Molecular Mechanism of Action. Mol Pharmacol. 2012 Oct 16. [Epub ahead of print]

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