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

@article{Rolf2015InVP,
  title={In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib},
  author={M. G. Rolf and J. Curwen and Margaret Veldman-Jones and C. Eberlein and Jianyan Wang and A. Harmer and Caroline J Hellawell and M. Braddock},
  journal={Pharmacology Research & Perspectives},
  year={2015},
  volume={3}
}
  • M. G. Rolf, J. Curwen, +5 authors M. Braddock
  • Published 2015
  • Medicine
  • Pharmacology Research & Perspectives
  • 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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