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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
| HLMs | HIMs | HKMs | |
|---|---|---|---|
| Cabotegravir | UGT1A1a | ND | ND |
| Dolutegravir | UGT1A9 > UGT1A1a | UGT1A3 > UGT1A8 > UGT1A1a | UGT1A9 |
| Raltegravir | UGT1A9 > UGT1A1 | UGT1A8 > UGT1A1 | UGT1A9 |
ND, not determined.
Greater than 2-fold difference in isoform UGT Km value from that observed for the tissue Km value.
