Journal
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 123, Issue -, Pages 502-514Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejps.2018.08.008
Keywords
Protein binding; Albumin-facilitated uptake; In vitro-in vivo extrapolation
Categories
Funding
- National Science Foundation Graduate Research Fellowship Program [1144247]
- NIH [P30 DK026743]
- NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES [P30DK026743] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [T32GM007175] Funding Source: NIH RePORTER
Ask authors/readers for more resources
As explained by the free drug theory, the unbound fraction of drug has long been thought to drive the efficacy of a molecule. Thus, the fraction unbound term, or f(u), appears in equations for fundamental pharmacokinetic parameters such as clearance, and is used when attempting in vitro to in vivo extrapolation (IVIVE). In recent years though, it has been noted that IVIVE does not always yield accurate predictions, and that some highly protein bound ligands have more efficient uptake than can be explained by their unbound fractions. This review explores the evolution of f(u) terms included when implementing IVIVE, the concept of protein-facilitated uptake, and the mechanisms that have been proposed to account for facilitated uptake.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available