Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor.

@article{Basavapathruni2014NonclinicalPA,
  title={Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor.},
  author={Aravind Basavapathruni and Edward J. Olhava and Scott R. Daigle and Carly A Therkelsen and Lei Jin and P. Ann Boriack-Sjodin and Christina J. Allain and Christine R. Klaus and Alejandra Raimondi and Margaret Porter Scott and Angelos Dovletoglou and Victoria M. Richon and Roy M. Pollock and Robert A Copeland and Mikel P. Moyer and Richard Chesworth and Paul G. Pearson and Nigel J. Waters},
  journal={Biopharmaceutics & drug disposition},
  year={2014},
  volume={35 4},
  pages={237-52}
}
(2R,3R,4S,5R)-2-(6-Amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol (EPZ-5676) is a novel DOT1L histone methyltransferase inhibitor currently in clinical development for the treatment of MLL-rearranged leukemias. This report describes the preclinical pharmacokinetics and metabolism of EPZ-5676, an aminonucleoside analog with exquisite target potency and selectivity that has shown robust and durable… CONTINUE READING
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8972–8983

  • SongY.Amedicinal chemistry perspective for targeting histone H3 lys Anglin JL, 5622
  • Biopharm. Drug Dispos.
  • 2014
Highly Influential
10 Excerpts

reaching a consensus on values of human microsomal protein Biopharm

  • ZE Barter, MK Bayliss, PH Beaune, data et al. Scaling factors for the extrapolation of in vitro
  • Drug Dispos.
  • 2014

Amedicinal chemistry perspective for targeting histone H 3 lysine 79 methyltransferase DOT 1 L

  • JL Anglin, SongY
  • J Med Chem
  • 2013

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