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Transporters

Creative Animodel is an ideal provider of transporters assays to accelerate your drug discovery and development process. With experienced experts and state-of-the-art facilities, we can deliver high-quality and reliable data in a time-saving and cost-efficient manner.

What Are Transporters?

Transporter is a membrane protein serving the function of moving ions, small molecule or macromolecules. These transporters can be divided into efflux transporters belonging to the ATP-binding cassette (ABC) family and solute carrier (SLC) family members that mediate the influx or bidirectional movement of drugs across the cell membrane. It is recognized that drug transporters are important for absorption, distribution and excretion of many drugs. Polymorphisms or drug-drug interaction (DDI) can lead to loss of transports’ function, which can result in clinically significant changes in drug disposition, efficacy and toxicity. Many pharmaceutical companies and drug regulatory authorities have realized the requirement for transporters research in the early stage of drug development and for the prediction of transported-based drug interactions and genetic polymorphisms. Therefore, FDA and other regulatory agencies emphasize the importance of evaluating the potential of new drug candidates for transporter-mediated DDI with a determination of victim (substrate) and perpetrator (inhibition) potential.

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Figure 1. Expression of transporters with major roles in drug efficacy or toxicity in (a) human intestinal epithelia, (b) kidney proximal tubule epithelia, (c) hepatocytes, and (d) brain capillary endothelial cells (DeGorter M. K., 2012).

Transporters Assays at Creative Animodel

Based on transporters, Creative Animodel can perform tests for compound interactions and offer substrate assessment and inhibition services through diverse assay systems. As introduced before, drug transporters are divided into two classes, ABC and SLC family.

• ABC transporters.
Most ABC transporters of eukaryote are efflux pumps. They use ATP as an energy source to translocate their substrates across membranes. We can provide ABC transporters of pharmacological interest, including P-glycoprotein (P-gp), breast cancer resistance protein (BCRP, ABCG2) and bile salt export pump (BSEP).

• SLC transporters.
Most SLC transporters are secondary active transporters. They use the electrochemical potential stored in ion gradients. We can offer these SLC transporters of interest in drug R&D, including the organic anion transporting polypeptides (OATPs), organic anion transporters (OATs), organic cation transporters (OCTs), as well as multidrug and toxin extrusion transporters (MATEs).

Our Advantages
• Various in vitro transporter assay systems, including membrane vesicles, recombinant cell lines expressing uptake transporters, polarized cell monolayers, plated hepatocytes or hepatocytes in suspension, and sandwich-cultured hepatocytes
• Using probe substrates, inhibitors and parameters recommended by FDA, EMA and other regulatory agencies
• Rapid assessment of transporter using cutting-edge equipment
• Customized services based on specific requirements for content, cost, and time

Creative Animodel can provide satisfying transporters services. No matter what services you are looking for, we can offer comprehensive in vitro pharmacology services to you. We have a team of professional scientists with pharmaceutical knowledge to support you in all steps of drug discovery and development. If you have any questions or other specific needs, please feel free to contact us.

References
1. Brouwer K. L. R., et al.; In vitro methods to support transporter evaluation in drug discovery and development. Clinical Pharmacology & Therapeutics. 2013, 94(1): 95-112.
2. DeGorter M. K., et al.; Drug transporters in drug efficacy and toxicity. Annual review of pharmacology and toxicology. 2012, 52: 249-273.

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