The Transporter Panel
Drug transporters play important roles in the absorption and tissue distribution of various compounds and their metabolites and thus can significantly affect their efficacy and safety. The impact of transporters on drug disposition and drug-drug interactions is an area of increasing concern to regulators, as highlighted by the recent White Paper in the International Transporter Consortium (see References).
Though various in vitro assays do allow the analysis of compound-transporter interactions, it remains difficult to estimate the in vivo consequences of such.
Different transporter knockout mice have proven to be valuable tools for studying the importance of a particular transporter for the disposition of a compound in vivo, and a wide range of transporter knockouts are now available. However, a remaining obstacle for the extrapolation of results obtained from animal studies to man is the potential difference in the interaction of a drug with transporters between species. Humanized transporter mouse models can help to overcome these limitations, and a number of these are available as part of the transADMET panel now, with further models in development.
Key utilities of these models include:
1. Tissue distribution. Investigation of transporter effects on distribution in vivo.
2. Transporter-mediated drug-drug interactions. Prediction of clinical impact of transporter induction or inhibition.
CXR and Taconic have partnered to make the transADMET Transporter models commercially available.
Contract services: CXR are co-exclusive suppliers of contract research services using transADMET mice. We also offer consultancy and advice to our customers. For more information on contract research services at CXR using the transADMET mice, contact us here or at info@cxrbiosciences.com.
Off the shelf mice: Mice may be purchased directly from Taconic by both academic and for-profit customers. To purchase transADMET mice, please visit the relevant model webpages:
In development:
Humanized BCRP Mouse
*These models are sold as Taconic Transgenie Models™.
Membrane transporters in drug development. The International Transporter Consortium. Nature Reviews Drug Discovery. Volume 9, March 2010, 215 – 236.
