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Physiologically Based Pharmacokinetic Modeling in Lead Optimization. 2. Rational Bioavailability Design by Global

Pankaj R Daga1, Michael B Bolger2, Ian S Haworth3

  • 1Novartis Institute of Biomedical Research , Emeryville , California 94608 , United States.

Molecular Pharmaceutics
|January 17, 2018
PubMed
Summary

Medicinal chemists can now efficiently optimize oral bioavailability (%F) by identifying key compound properties. This study uses physiologically based pharmacokinetic (PBPK) simulations and partial least squares regression (PLS) to map bioavailability landscapes.

Keywords:
PBPKPLSglobal sensitivity analysislead optimizationlead serieslocal modelmultiobjective optimization

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