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Molecular structure and Tissue distribution
OATP2B1 (previously known as OATP-B) is expressed in various tissues, including the liver, intestine, placenta, heart and skin. The gene for OATP2B1 is located on chromosome 11q13. In the liver, OATP2B1 is expressed in the sinusoidal membrane of hepatocytes, indicating a possible role in the hepatic uptake of drugs from blood. In the intestine, OATP2B1 is expressed in the luminal membrane of small intestinal enterocytes, suggesting that it may participate in the active absorption of drugs. In the heart, OATP2B1 is expressed in the vascular endothelium and might thus mediate the uptake of its substrate drugs into the heart.

Interaction of OATP2B1 with endogenous compounds and drugs

Compared to other OATPs it has a narrow substrate specificity and transports only estrone-3-sulfate, BSP, and with very low affinity dehydroepiandrosterone-sulfate (DHEAS). For other compounds such as PGE2 and estradiol-17ß-glucuronide controversial results have been presented.
OATP2B1 substrates include the statins atorvastatin, fluvastatin, pravastatin and rosuvastatin and, for example, the antidiabetic drug glibenclamide. Similarly to OATP1B1 and OATP1B3, cyclosporine also inhibits OATP2B1, which may contribute to its interactions.Grapefruit juice and orange juice have been shown to inhibit OATP2B1 in vitro. Thus, it was hypothesized that they could reduce the absorption of OATP2B1 substrate drugs. However, grapefruit juice had no significant effect on the pharmacokinetics of oral glibenclamide in healthy subjects.

Figure 1 Concentration dependent uptake of estron-3-sulfate by OATP2B1 Figure 2 Inhibitory effect of various inhibitors (100 µM) on OATP2B1-mediated ES uptake



New validated products:

  • MRP2
  • roct1


2nd German Pharm-Tox Summit
Heidelberg, Germany
March 06-09, 2017

19th Barrier- and

Bad Herrenalb, Germany
May 15-17, 2017

14th European ISSX Meeting
Köln, Germany

June 26- 29, 2017

2nd Symposium on Transporters in Drug Discovery
London, UK
May 15-16, 2017

Münster Transporttage 2017
Münster, Germany
October 21 – 22, 2017


Guidance for Industry (FDA and EMA)