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Single oral dose cure of lethal P. yoelii with a new iron chelator in human clinical trials for iron overload
© Tripathi et al; licensee BioMed Central Ltd. 2010
- Published: 20 October 2010
- Iron Overload
- Iron Chelator
- Human Clinical Trial
Iron chelators for the treatment of malaria have proven therapeutic activity in vitro and in vivo in both humans and mice, but their clinical use has been limited by the unsuitable adsorption and pharmacokinetic properties of the few available chelators. FBS0701 is an oral iron chelator currently in Phase 2 human studies for the treatment of transfusional iron overload. The drug has very favorable absorption and PK properties allowing for once-daily use to deplete circulating free iron. Once-daily administration of FBS0701 in humans at well tolerated doses can achieve plasma concentrations in the high μM range.
P. falciparum drug inhibition was performed with Sybrgreen drug inhibition assays. Murine malaria was initiated by intraperitoneal inoculum of Balb/c mice followed for 30 days.
FBS0701 demonstrates a single oral dose cure of the lethal P. yoelii model. Significantly, this effect persists after the chelator has cleared from plasma. FBS0701 may find clinically utility as monotherapy, a malarial prophylactic or, more likely, in combination with other antimalarials.
This article is published under license to BioMed Central Ltd. This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.