The impact of Organic Anion-Transporting Polypeptides (OATPs) on disposition and toxicity of antitumor drugs; insights from knockout and humanized mice

It is now widely accepted that organic anion-transporting polypeptides (OATPs), especially members of the OATP1A/1B family, can have a major impact on the disposition and elimination of a variety of endogenous molecules and drugs. Owing to their prominent expression in the sinusoidal plasma membrane of hepatocytes, OATP1B1 and OATP1B3 play key roles in the hepatic uptake and plasma clearance of a multitude of structurally diverse anti-cancer and other drugs. Here, we present a thorough assessment of the currently available OATP1A and OATP1B knockout and transgenic mouse models as key tools to study OATP functions in vivo.
Source: Drug Resistance Updates - Category: Drugs & Pharmacology Authors: Source Type: research