Chemistry and Pharmacokinetics of Gallium Maltolate, a Compound With High Oral Gallium Bioavailability

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Chemistry and Pharmacokinetics of Gallium Maltolate, a Compound With High Oral Gallium Bioavailability

Gallium maltolate, tris(3-hydroxy-2-methyl-4H-pyran-4-onato)gallium (GaM), is an orally active gallium compound for therapeutic use. It is moderately soluble in water (10.7 +/- 0.9 mg/mL at 25 composite functionC) with an octanol partition coefficient of 0.41+/-0.08. The molecule is electrically neutral in aqueous solution at neutral pH; a dilute aqueous solution (2.5 x10-(-5) M) showed little ...

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Pharmacokinetics of gallium maltolate after intragastric administration in neonatal foals.

OBJECTIVE To determine the pharmacokinetics of gallium maltolate (GaM) after intragastric administration in healthy foals. ANIMALS 6 healthy neonatal foals. PROCEDURES Each foal received GaM (20 mg/kg) by intragastric administration. Blood samples were obtained before (time 0) and at 0.25, 0.5, 1, 2, 4, 8, 12, 24, 36, and 48 hours after GaM administration for determination of serum gallium ...

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Development of gallium compounds for treatment of lymphoma: gallium maltolate, a novel hydroxypyrone gallium compound, induces apoptosis and circumvents lymphoma cell resistance to gallium nitrate.

Clinical studies have shown gallium nitrate to have significant antitumor activity against non-Hodgkin's lymphoma and bladder cancer, thus indicating that gallium-based drugs have potential for further development as antineoplastic agents. In this study, we compared the cytotoxicity of gallium maltolate, a novel gallium compound, with gallium nitrate in lymphoma cell lines, including p53 varian...

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Hepatocellular carcinoma detection by gallium scan and subsequent treatment by gallium maltolate: rationale and case study.

Gallium is antiproliferative to many types of cancer, due primarily to its ability to act as a non-functional mimic of ferric iron (Fe(3+)). Because Fe(3+) is needed for ribonucleotide reductase activity--and thus DNA synthesis--gallium can inhibit DNA production and cell division. Diagnostic gallium scans have shown that hepatocellular carcinoma (HCC) is commonly avid for gallium. Furthermore,...

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Pharmacokinetics of an orally administered methylcellulose formulation of gallium maltolate in neonatal foals.

Gallium is a trivalent semi-metal with anti-microbial effects because of its incorporation into crucial iron-dependent reproductive enzyme systems. Gallium maltolate (GaM) provides significant gallium bioavailability to people and mice following oral administration and to neonatal foals following intragastric administration. To study the prophylactic and therapeutic effects of GaM against Rhodo...

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ژورنال

عنوان ژورنال: Metal-Based Drugs

سال: 2000

ISSN: 0793-0291

DOI: 10.1155/mbd.2000.33