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Tissue Free Drug Concentrations

Wednesday April 25, 2018

8:30 am - 11:00 am Eastern Time (ET)

Room 15B


Chair :

Donglu Zhang

Julie Lade

Under thermodynamic conditions, the free drug concentration in tissues should equal to that in circulation. However, drug disposition factors such as antigen‐/drug transporters‐mediated uptake, and other common properties such as tissue accumulation and covalent binding kinetically alter drug forms and concentrations in tissues. In turn, the actual drug free concentrations in tissues instead of that in circulation determine efficacy and toxicity of a drug. This session will focus on examples to support the importance of tissue concentration of a drug or metabolites that is a critical parameter but often missing in drug discovery and development.


Donglu Zhang - Genentech

Exceptions to Free Drug Assumption

Jashvant Unadkat - University of Washington

Pursuing the Holy Grail of Predicting and Verifying Tissue Drug Concentrations: A Proteomics and PET-imaging Approach

Lijuan Jiang - Enanta Pharmaceuticals

Target Tissue Drug Concentrations are Critical for the Efficacy of Antibiotics and Anti-viral Drugs

Julie Lade - Amgen

Pharmacokinetics, Metabolism, and Biodistribution of a Liver-targeted siRNA Therapeutic

Sheerin Shahidi-Latham - Genentech

High-Resolution Imaging MALDI Mass Spectrometry to Assess Label-Free Drug Disposition in Tissues

Herana Seneviratne - Johns Hopkins University School of Medicine

MALDI Mass Spectrometry Imaging Reveals Heterogenous Distribution of Tenofovir and Tenofovir-Diphosphate in Human Colorectal Tissue

Gautham Gampa - University of Minnesota

Delivery of Active Drug Concentrations to Brain Tumor Targets