Course Description

This course describes the estimation of in vivo drug distribution based on biomimetic properties. Volume of distribution, unbound volume of distribution, drug efficiency brain to plasma ratio.

Director, Honorary Professor at UCL School of Pharmacy

Klara Valko

Leaving GSK after 22 years of service, she is now founder director of Bio-Mimetic Chromatography Ltd providing data analysis, biomimetic HPLC method development and measurements, in vivo drug distribution modelling and various courses for pharmaceutical companies. She is an Honorary Professor to the UCL School of Pharmacy since 2004; leading the Physchem/ADME module for the Drug Discovery MSc course. She has developed biomimetic HPLC methods for high throughput measurements of serum albumin, glycoprotein and phospholipid binding. She invented the Chromatographic Hydrophobicity Index (CHI) for the fast determination of a compound’s lipophilicity using generic gradient reversed phase chromatography. She has built mathematical statistical models based on measured properties to predict human in vivo drug distribution, such as, volume of distribution, DRUGeff max and tissue/plasma partition. She has contributed to the Drug Efficiency Index (DEI) concept and dose estimation based on DEI. She has published over 100 papers that have achieved over 3000 citations. She has written a book on “Physicochemical and Biomimetic Properties in Drug Discovery; Chromatographic Techniques for lead optimization” published by Wiley in 2014. Currently, she is working on the second edition of the “Handbook of Analytical Separations” Volume 1 “Separation Methods in Drug Synthesis and Purification” published by Elsevier.  

Course curriculum

  • 1

    Modelling in vivo distribution of drugs

    • Background

  • 2

    Welcome to the course!

    • How to use this course

  • 3

    Models for volume of distribution

    • Handout for volume of distribution

    • Volume of distribution

    • Test your learning

  • 4

    Modelling unbound volume of distribution

    • Handout for unbound volume of distribution

    • Modelling unbound volume of distribution

    • Summary of volume of distribution and unbound volume of distribution

    • Test your learning

  • 5

    Drug efficiency concept

    • Handout for drug efficiency

    • Drug efficiency and drug efficiency index

    • Summary of drug efficiency

    • Summary of drug efficiency index

    • Test your learning

  • 6

    Plasma and tissue binding models

    • Plasma and tissue binding handout

    • Plasma and tissue binding models

    • Video 10.2 Plasma and tissue binding models

    • Test your learning

    • Here is the possibility to ask questions from the tutor