1.THERE ARE A NUMBER OF ADDITIONAL TRANSPORTERS YOU SHOULD SERIOUSLY CONSIDER

TAKE HOME MESSAGES FROM THE ITC PAPERS: part 2

In 2010 the ITC presented 7 transporters it considered clinically relevant, now often referred to as the ’ITC-7’: OAT1, OAT3, OCT2, OATP1B1, OATP1B3, P-gp and BCRP. Hillgren et al. summarize a number of transporters of emerging importance:

MATEs: MATEs are expressed in the liver (MATE1) and kidney (MATE1, MATE2-K) and are involved in the transport of cationic and zwitterionic molecules like Metformin and Cimetidine. Due to their important role in renal excretion of drugs the ITC suggests adding MATEs to the OAT1/3 and OCT2 decision trees, i.e. inhibition of MATEs should be studied for each new molecular entity (NME), whereas substrate studies should be performed for compounds showing more than 25% renal, active secretion.

Read more →