MRP Transporter Substrate Identification

Human MRP efflux transporter substrate identification is within our portfolio of in vitro drug transporter services. Cyprotex delivers consistent, high quality data in line with our published transporter strategy review,for either your early stage screening projects or your later stage regulatory studies.

Identifying potential substrates of the MRP efflux transporters in vitro:

• MRP2 (multidrug resistance associated protein 2; ABCC2), MRP3 (ABCC3) and MRP4 (ABCC4) are ATP binding cassette (ABC) efflux transporters which are located on the brush border membrane of enterocytes (MRP2), the canalicular membrane (MRP2) or sinusoidal membrane (MRP3, MRP4) of hepatocytes, the brush border membrane of renal proximal tubule epithelial cells (MRP2, MRP4) and at the blood-brain barrier (MRP4)¹.
• Consequently, these efflux transporters influence the absorption, distribution, metabolism and excretion of drugs/and or metabolites within the body.
• The International Transporter Consortium (ITC)¹ indicate that because MRP2, MRP3 and MRP4 are important determinants of hepatobiliary disposition of polar drug metabolites, for example glucuronide conjugates, then being a substrate of these transporters may contribute to the overall victim and perpetrator DDI potential of the parent drug.
• Cyprotex’s MRP efflux transporter substrate identification assay determines if your compound is a substrate of these key hepatobiliary transporters.

_{1) Zamek-Gliszczynski MJ et al., (2018) Transporters in Drug Development: 2018 ITC Recommendations for Transporters of Emerging Clinical Importance. Clin Pharmacol Ther 104(5): 890-899
2) FDA Guidance for Industry – In Vitro Drug Interaction Studies - Cytochrome P450 Enzyme- and Transporter-Mediated Drug Interactions (January 2020)}