CGP 65015

CGP 65015 is an oral iron chelator, which can mobilize iron deposits.

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CGP 65015 is an oral iron chelator[1].

CGP65015 (150 μmol IBE/kg p.o. on d0) dramatically increases the urinary and faecal iron clearance, and still enhances iron elimination during the second post-treatment day in iron-overloaded marmosets[1].

Marmosets[1] To approximate the iron status of thalassaemic patients in the marmosets, the animals are iron-overloaded by three i.p. injections of iron (III) hydroxide polyisomaltose at 14-d intervals (200 mg/kg twice and 100 mg/kg at the third injection). Prior to the first exposure to an iron chelator (CGP 65015), the marmosets are rested for at least 8 weeks in order to allow definite distribution of the injected iron into all storage compartments. CGP 65015 is dispersed in 40% aqueous Cremophor RH 40 for oral administration of 150 μmol IBE/kg. All dosages are expressed in terms of 'iron binding equivalents' (IBE) which take into account the stoichiometry of the chelator in the iron complex, i.e. 150 μmol IBE correspond to 150, 300 and 450 μmol of a mono-, bi- and tridentate chelator respectively. The standard dose is 150 μmol iron binding equivalents (IBE) per kg body weight. The applied volume is 5 mL/kg body weight[1].

[1]. Sergejew T, et al. Chelator-induced iron excretion in iron-overloaded marmosets. Br J Haematol. 2000 Sep;110(4):985-92.

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