Table 4.
Examples for phase 2 DME, phenotypes, substrates and inhibitors/inducers. N.a. = not applicable; NM = normal metabolizers; IM = intermediate metabolizers; PM = poor metabolizers; RM = rapid metabolizers; UM = ultra-rapid metabolizers. Examples are from the pharmgkb database: www.pharmgkb.org, accessed on 29 March 2021.
| Enzyme | Known Phenotypes | Substrates | Phenoconversion |
|---|---|---|---|
| UGT1A1 | NM, IM, PM | bilirubin, irinotecan, estradiol | Atazanavir, carbamazepine, phenytoin, phenobarbital, rifampicin, ritonavir, lamotrigin, efavirenz, tyrosine-kinase inhibitors |
| UGT1A4 | Normal function, increased function, decreased function | valproic acid, lamotrigine, allopurinol, febuxostat, tamoxifen, clozapine, anastrozole | methylene blue, ertugliflozin, carbamazepine, phenytoin |
| UGT1A6 | n.a. | allopurinol, febuxostat, methothrexat, valproic acid | troglitazone, fosphenytoin, phenytoin, carbamazepine |
| UGT1A9 | n.a. | allopurinol, febuxostat, methothrexat, valproic acid | vandetanib |
| UGT2B7 | n.a. | zodovudine, oxycodone, efavirenz, methadone, lamotrigine, morphine, codeine, fentanyl. | flunitrazepam, ketoconazole, umifenovir, phenobarbital, mefenamic acid |
| UGT2B15 | normal function decreased funtion |
oxazepam, lorazepam | |
| N-acetyltransferase (NAT2) | fast slow |
isoniazid, hydralazine, dapsone, caffein, procainamide | |
| Thiopurine Methyl Transferase (TPMT) | NM, IM, possibly intermediate, PM | thiopurines | allopurinol |
| Nudix hydrolase 15 (NUDT 15) | NM, IM, possibly intermediate, PM | thiopurines |