Transporters have become increasingly important in drug development due to the major role they play in absorption, distribution and excretion of endogenous and exogenous compounds, as transporter-mediated drug-drug interactions (DDI) are associated with potential toxicological and pharmacological consequences. As shown in numerous publications, the effects of transporters on the pharmacokinetics of several drugs and associated DDI have been reported. Consequently, recent guidance documents released by the US FDA and European Medicines Agency (EMA) emphasize the importance of evaluating the potential of new drug candidates for transporter-mediated DDI.
Solute carrier (SLC) transporters are located in the small intestine, liver, kidney, blood-brain barrier, and so on. They play a role in the up-take of various drugs, as well as endogenous nutrients into cells and thus may influence the ADME properties of, or indeed adverse reactions to, a compound of interest. Thus, investigation of SLC transporters is expected to be helpful during drug development.
Ready-to-use cellular models for SLC assays
The European regulatory agency recommends the study of several transporters, including MDR1, OATP1B1, OATP1B3, OCT2, OAT1, OAT3, BCRP, OCT1, MATE1, MATE2 and BSEP in vitro. However, conditions for accessing commercially available tools for studying some of the recommended transporters, and namely SLC transporters, has up to now been a challenge for researchers.
Now, access to SLC research tools is largely facilitated through tebu-bio’s collaboration with GenoMembrane, to provide their TRANSiPORT brand of products.
What are their features?
- Cryopreserved format provides flexibility for experimental planning
- Cells are readily available
- Consistent with stable cell lines
- One vial contains 1 ×10E7 cells and supports one 24-well plate
- Cells are shipped with liquid nitrogen dry vapor shipper
- Cells can be thawed, plated and assayed in just two days
Which TRANSiPORT Cell Lines are currently available?
| Products | Cat. No |
| Human OATP1B1 | GM1002 |
| Human OATP1B3 | GM1006 |
| Human OAT1 | GM1003 |
| Human OAT3 | GM1004 |
| Human MATE1 | GM1014 |
| Human MATE2K | GM1015 |
| Human OCT1 | GM1008 |
| Human OCT2 | GM1005 |
| Human NTCP | GM1013 |
| Mock | GM1001 |
What is different with TRANSiPORT compared to existing patents?
The use of some transporters is restricted by patents. Bristol-Myers Squibb patented OATP1B1, Okayama University MATE1 & MATE2K.
One other company (Corning) also offers SLC transfected cells. However, their position regarding patents, albeit very clear, restricts use of their products in a way not always easy to apply for the user, by declining any responsibility regarding claims of the patents in question.
GenoMembrane & tebu-bio SLC Cells are licensed with the patent. This means that the researcher is covered for the use of these SLC cell lines, and can utilize the data for publication or dossier purposes.
In the coming weeks we will publish another post on this blog to illustrate cell culture and assay details. Please feel free to contact us or comment in the meantime!
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