Design and measurement of drug tissue concentration asymmetry and tissue exposure-effect (Tissue PK-PD) evaluation
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R Zang, A Barth, H Wong, J Marik, J Shen…
Journal of Medicinal …, 2022
ACS Publications
The “free drug hypothesis” assumes that, in the absence of transporters, the steady state free plasma concentrations equal to that at the site of action that elicit pharmacologic effects. While it is important to utilize the free drug hypothesis, exceptions exist that the free plasma exposures, either at C max, C trough, and C average, or at other time points, cannot represent the corresponding free tissue concentrations. This “drug concentration asymmetry” in both total and free form can influence drug disposition and pharmacological effects. In this …
