Drug Interactions Newsletter

Volume 1, Issue 34, 09/08/2009

Question

What medications commonly used in clinical practice rely upon the cell surface efflux transporter breast cancer resistance protein (BCRP) and are subject to drug interactions?

Answer

Periodically, the editorial board will release an issue that explains general principles or terms that all clinicians should be familiar with as they are frequently encountered in clinical practice.  They are also concepts built upon in many of the newsletters.  A thorough understanding of both the mechanism and the clinical application of a drug interaction provides the clinician with the greatest opportunity for identifying and determining the relevancy of a particular interaction.  While enzyme pathways are known to many clinicians as areas that cause drug interactions, influx and efflux transporters can also be major contributors. 

There are a number of cell surface efflux transporters that are designed to move certain types of medications out of the cell and most commonly include breast cancer resistant protein (BCRP), bile salt export pump (BSEP), multidrug resistance protein (MDR1; P-glycoprotein), MDR2, MDR3, multidrug resistance associated protein (MRP)-1, MRP2, MRP3, MRP4, MRP5, MRP6 and sodium/phosphate cotransporter (NPT1).(1)  These efflux transporters are located in....

The complete answer to this issue comes with a table that summarizes all of the medications known to be substrates, inhibitors and inducers of BCRP.

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