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FIGURE 2-1 Roles of membrane transporters in pharmacokinetic pathways. Membrane transporters (T) play roles in pharmacokinetic pathways (drug absorption, distribution, metabolism, and excretion), thereby setting systemic drug levels. Drug levels often drive therapeutic and adverse drug effects.

(e.g., the thiazolidinedione troglitazone). Thus, uptake and efflux transporters determine the plasma and tissue concentrations of endogenous compounds and xenobiotics, thereby influencing either systemic or site-specific drug toxicity.

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