TABLE 5

Summary of the tissue- and isoform-specific UGTs responsible for cabotegravir, dolutegravir, and raltegravir metabolism based on relations of Km values derived from expression systems

HLMsHIMsHKMs
CabotegravirUGT1A1aNDND
DolutegravirUGT1A9 > UGT1A1aUGT1A3 > UGT1A8 > UGT1A1aUGT1A9
RaltegravirUGT1A9 > UGT1A1UGT1A8 > UGT1A1UGT1A9

  • ND, not determined.

  • ↵a Greater than 2-fold difference in isoform UGT Km value from that observed for the tissue Km value.