DDI Marker Studies Knowledgebase – quarterly update

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

Our Editorial Team has dedicated effort on identifying substrates and perpetrators of UGT enzymes. More than 30 UGT substrates, inhibitors, and inducers recommended by the ICH M12 DDI guideline have been added to the knowledgebase with supporting DDI and/or PGx evidence. In addition, we have continued to identify substrates and inhibitors for renal transporters by reviewing all the existing data. Overall, 65 compounds have been identified as substates, inhibitors, and inducers of CYPs, UGTs, and various transporters, including P-gp, BCRP, OATP1B1, OATP1B3, OAT1, OAT3, OCT2, MATE1, and MATE2-K. Notably, one compound was classified as a sensitive substrate of CYP1A2 and one as a strong inhibitor of CYP3A based on PBPK data (AUCR > 10), which 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.