Whole blood or plasma: what is the ideal matrix for pharmacokinetic-driven drug candidate selection?

Author:

Dash Ranjeet P1ORCID,Veeravalli Vijayabhaskar2,Thomas Jennifer A1,Rosenfeld Clint3,Mehta Nirali4,Srinivas Nuggehally R5

Affiliation:

1. ADME-DMPK, Charles River Laboratories, Ashland, OH 44805, USA

2. Department of Neurology, Johns Hopkins University, Baltimore, MD 21205, USA

3. DMPK, Charles River Laboratories, Mattawan, MI 49071, USA

4. PHARMA-STATS, Ahmedabad, Gujarat 382210, India

5. Kenox Pharmaceuticals Inc., Monmouth Junction, NJ 08852, USA

Abstract

In the present era of drug development, quantification of drug concentrations following pharmacokinetic studies has preferentially been performed using plasma as a matrix rather than whole blood. However, it is critical to realize the difference between measuring drug concentrations in blood versus plasma and the consequences thereof. Pharmacokinetics using plasma data may be misleading if concentrations differ between plasma and red blood cells (RBCs) because of differential binding in blood. In this review, factors modulating the partitioning of drugs into RBCs are discussed and the importance of determining RBC uptake of drugs for drug candidate selection is explored. In summary, the choice of matrix (plasma vs whole blood) is an important consideration to be factored in during drug discovery.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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