In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib

@inproceedings{Rolf2015InVP,
  title={In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib},
  author={Michael G Rolf and Jon O. Curwen and Margaret Veldman-Jones and Cath A Eberlein and Jianyan Wang and Alex Harmer and Caroline J Hellawell and Martin Braddock},
  booktitle={Pharmacology research & perspectives},
  year={2015}
}
Off-target pharmacology may contribute to both adverse and beneficial effects of a new drug. In vitro pharmacological profiling is often applied early in drug discovery; there are fewer reports addressing the relevance of broad profiles to clinical adverse effects. Here, we have characterized the pharmacological profile of the active metabolite of fostamatinib, R406, linking an understanding of drug selectivity to the increase in blood pressure observed in clinical studies. R406 was profiled in… CONTINUE READING
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