Journal ArticleDOI
A high-performance liquid chromatographic method for the measurement of the iron chelator 1,2-dimethyl-3-hydroxypyridin-4-one in human plasma.
TLDR
A rapid, accurate, and sensitive high-performance liquid chromatography method is described for measuring L1 in human plasma using a Hypercarb 7 microns column and monitoring the column eluent by ultraviolet absorption at 280 nm.Abstract:
1,2-Dimethyl-3-hydroxypyridin-4-one (CP020 or L1) is a novel oral iron chelator that has proved to be effective in animals and humans. A rapid, accurate, and sensitive high-performance liquid chromatography method is described for measuring L1 in human plasma using a Hypercarb 7 microns column and monitoring the column eluent by ultraviolet absorption at 280 nm. CP020 and the internal standard (CP094) were extracted into dichloromethane (2 x 5 ml) from plasma at neutral pH [0.25 ml of plasma + 0.75 ml of 60 mM 3-(N-morpholino)propanesulfonic acid buffer, pH 7.4]. The method proved to be linear (r2 = 0.998) in the clinical range of 0.5-50 micrograms/ml when 0.25 ml of plasma was used, with the coefficient of variation less than 10% even at the lower concentration range.read more
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Journal ArticleDOI
Critical comparison of novel and existing methods of compliance assessment during a clinical trial of an oral iron chelator.
Doreen Matsui,Christine Hermann,Julia Klein,Matitiahu Berkovitch,Nancy F. Olivieri,Gideon Koren +5 more
TL;DR: A combination of methods should be used in the evaluation of medication compliance during the investigation of a new drug, given the limitations of the available techniques for monitoring compliance.
Journal ArticleDOI
Assessment of the effect of the oral iron chelator deferiprone on asymptomatic Plasmodium falciparum parasitemia in humans.
Philip E. Thuma,Nancy F. Olivieri,George F. Mabeza,Godfrey Biemba,Dean Parry,Stenford Zulu,Frank F. Fassos,Robert A. McClelland,Gideon Koren,Gary M. Brittenham,Victor R. Gordeuk +10 more
TL;DR: Deferiprone was administered daily for three or four days in divided doses of 75 or 100 mg/kg of body weight, dosages that are effective for treating iron overload, and the mean peak plasma concentration achieved was within the range demonstrated to inhibit the growth of P. falciparum in vitro but the systemic exposure as determined by the 24-hr plasma concentration-time curve would not be predicted inhibit growth in vivo.
Journal ArticleDOI
The efficacy of oral deferiprone in acute iron poisoning
Matitiahu Berkovitch,Amir Livne,G Lushkov,Michael Segal,Clara Talmor,Yedidia Bentur,Julia Klein,Gideon Koren +7 more
TL;DR: Orally administered deferiprone can decrease morbidity and mortality caused by acute iron overdose in rats and holds promise in the treatment of iron poisoning in humans.
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An investigation into variability in the therapeutic response to deferiprone in patients with thalassemia major.
TL;DR: Regression analysis suggested that patients with initial hepatic iron concentration of less than or equal to 7.22 mg/g of dry weight liver tissue are unlikely to further decrease while taking deferiprone, and provided evidence that its effectiveness decreases in proportion to liver iron load.
Journal ArticleDOI
Iron chelating agents with clinical potential
TL;DR: Recently, selective iron chelators are finding an important role in the treatment of iron overload associated with many forms of thalassaemia as mentioned in this paper, and they appear to have potential in treating situations where a local increase in iron concentration causes an unfavourable pathology, for instance, in reperfused tissue (heart disease and stroke) and in Parkinsonian brain.