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Bioanalysis of Deferitrin and Its Polyether Analog, a Novel, Orally Active Iron Chelator by Liquid Chromatography-Tandem Mass Spectrometry

机译:耐液相色谱 - 串联质谱法的耐热素及其聚醚模拟,一种新型,口服活性铁螯合剂的生物分析

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Deferitrin (GT56-252) is a novel, orally bio-available iron chelator that is being developed for treating patients with chronic iron overload to transfusional therapy, specifically in beta-thalassemia, sickle cell disease (SCD), and myelodysplasticc syndrome (MDS). Deferitrin is currently undergoing phase II clinical trial. The polyether analog of deferitrin was synthesized as a back-up which has shown better efficacy in the animal models. Since both compounds are metal chelating compounds, method development for bioanalysis was challenging. Here we presented a rugged liquid chromatography-tandem mass spectrometry (LC/MS/MS) bioanalysis method developed for quantifying deferitrin and its polyether analog in plasmas with the required sensitivity and a rapid analysis time.
机译:Deferitrin(GT56-252)是一种新型的口服生物可用的铁螯合剂,用于将慢性铁过载患者治疗到输血治疗,特别是在β-地中海贫血,镰状细胞疾病(SCD)和髓病变血糖综合征(MDS)中。 Deferitrin目前正在进行II期临床试验。延展素的聚醚类似物被合成为备份,在动物模型中显示出更好的功效。由于两种化合物都是金属螯合化合物,因此生物分析的方法开发是挑战性的。在这里,我们介绍了一种坚固的液相色谱 - 串联质谱(LC / MS / MS)生物分析方法,用于在等离子体中定量Deferitrin及其聚醚类似物,具有所需的灵敏度和快速分析时间。

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