Prediction of Fraction Unbound in Microsomal and Hepatocyte Incubations: A Comparison of Methods across Industry Datasets-Reference-Cited by-同舟云学术

Prediction of Fraction Unbound in Microsomal and Hepatocyte Incubations: A Comparison of Methods across Industry Datasets

Published:2019-07-26 Issue:9 Volume:16 Page:4077-4085
ISSN:1543-8384
Container-title:Molecular Pharmaceutics
language:en
Short-container-title:Mol. Pharmaceutics

Author:

Winiwarter Susanne¹^ORCID,Chang George²,Desai Prashant³,Menzel Karsten⁴,Faller Bernard⁵,Arimoto Rieko⁶,Keefer Christopher²,Broccatell Fabio⁷

Affiliation:

1. DMPK, Research and Early Development, Cardiovascular, Renal and Metabolism (CVRM), BioPharmaceuticals R&D, AstraZeneca, Gothenburg SE-43183, Sweden

2. Pfizer Inc., Groton, Connecticut 06340, United States

3. Eli Lilly and Company, Indianapolis, Indiana 46285, United States

4. MSD, West Point, Pennsylvania 19486, United States

5. Novartis, CH-4056 Basel, Switzerland

6. Vertex Pharmaceuticals Inc., Boston, Massachusetts 02210, United States

7. Genentech Inc., South San Francisco, California 94080, United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Pharmaceutical Science,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.molpharmaceut.9b00525

Reference17 articles.

1. Microsome composition-based model as a mechanistic tool to predict nonspecific binding of drugs in liver microsomes

2. Evaluation of the human prediction of clearance from hepatocyte and microsome intrinsic clearance for 52 drug compounds

3. The Influence of Nonspecific Microsomal Binding on Apparent Intrinsic Clearance, and Its Prediction from Physicochemical Properties

4. Validation of Early Human Dose Prediction: A Key Metric for Compound Progression in Drug Discovery

5. Impact of Input Parameters on the Prediction of Hepatic Plasma Clearance Using the Well-Stirred Model

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