DDI Marker Studies Knowledgebase – quarterly update

The DDI Marker Studies Knowledgebase has been updated in July 2024 and is available in the DIDB Resource Center.

Our Editorial Team has dedicated effort on identifying substrates and inhibitors for OAT1, OAT3, OCT2, MATE1, and MATE2-K transporters. In this update, we have added 29 substrates and inhibitors of these transporters. Overall, 60 compounds have been identified as substates, inhibitors, and inducers of CYP enzymes and various transporters, including P-gp, BCRP, OATP1B1, OATP1B3, OAT1, OAT3, OCT2, MATE1, and MATE2-K. Notably, two compounds are classified as sensitive substrates of CYP3A, and a compound previously considered a moderate CYP2D6 inhibitor is now recognized as a strong inhibitor based on recent DDI data. These compounds could potentially lead to significant drug interactions mediated by these CYPs.

To view a comprehensive list of additions and modifications, including new compounds and updates to existing entries, you may use the “Recent Update” column (Column AE) on the spreadsheet and select “yes.”

In addition to substrates, inhibitors and inducers of CYPs and transporters, the Knowledgebase provides useful information on the compounds therapeutic class, clinical recommended dosage, pharmacokinetics (e.g., dose proportionality accumulation ratio, time to steady-state), QT prolongation, and NTI characteristics.

As always, feel free to contact us if you have any questions or comments.