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View some common Transporter study Q&A here.
View XenoTech's transporter assay decision tree here.
Drugs that are substrates or inhibitors of drug transporters have been implicated in drug-drug interactions. The 2012 FDA DDI draft guidance and the 2012 EMA guideline on investigation of drug interactions mention several specific transporters to investigate and assay conditions to follow. XenoTech’s experimental approach conforms to these scientific principles in evaluating test articles as Inhibitors and Substrates of Human P-gp, BCRP, OATP1B1, OATP1B3, OAT1, OAT3, OCT1 and OCT2 transporters.
All of XenoTech’s methods are state of the art and based on established scientific practices. For substrate studies, an LC/MS method will be developed for the analysis of each test article with a minimum of a single curve will be analyzed to establish dose response prior to the analysis of the study samples. XenoTech’s LC/MS (Analytical) group gives Transporter assays fast turnaround with same day assays.
XenoTech Transporter Services Benefits:
- In collaboration with Sekisui Medical, XenoTech is able to offer the widest selection of transporter assays on the market
- Assays available for all transporters mentioned in the FDA and EMA guidance documents
- Assays available for an extensive variety of non-FDA/EMA transporters, including exotic transporters expressed in oocytes
- In vivo studies available for a wide variety of transporters
- Studies are performed in a GLP-compliant facility and governed by XenoTech's in-house Quality Assurance Unit
- Ability to perform FDA/EMA submission studies with radiolabeled compounds or cold compounds due to XenoTech’s in-house Analytical Sciences group
- Ability to perform transporter substrate studies with complicated bioanalytics due to XenoTech’s in-house Analytical Sciences group
- Ability to deliver submission-ready reports due to XenoTech's in-house Knowledge Management group
- Ability to meet strict timelines, deliver industry-leading scientific quality and maintain unsurpassed levels of communication and trust
EMA / FDA Transporter Assays Available
XenoTech offers the full array of EMA/FDA recommended transporters.
In accordance with the 2012 EMA guidance, XenoTech evaluates intestinal permeability as outlined below.
|Caco-2||Intestinal Permeability Model - Substrate||Bidirectional permeability of TA across monolayer|
XenoTech offers the following Substrate transporter evaluation assays.
|MDCKII-MDR1||P-gp (MDR1)||Bidirectional permeability of TA across monolayer|
|MDCKII-BCRP||BCRP||Bidirectional permeability of TA across monolayer|
|HEK293||OATP1B1, OATP1B3, OCT1, OCT2||Accumulation of TA in transporter-expressing cells|
|S2||OAT1, OAT3||Accumulation of TA in transporter-expressing cells|
XenoTech offers the following Inhibitor transporter evaluation assays.
|Caco-2||P-gp||Bidirectional permeability of probe substrate in the presence of TA|
|MDCKII-MDR1||P-gp (MDR1)||Bidirectional permeability of probe substrate in the presence of TA|
|MDCKII-BCRP||BCRP||Bidirectional permeability of probe substrate in the presence of TA|
|HEK293||OATP1B1, OATP1B3, OCT1, OCT2||Accumulation of probe substrate in the presence of TA|
|S2||OAT1, OAT3||Accumulation of probe substrate in the presence of TA|
*Cell toxicity is assessed by measuring the lactate dehydrogenase (LDH) released from the cells, using unexposed media as a background control.