Pub. Date : 2014 Jul
PMID : 24820076
3 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Isoniazid mediates the CYP2B6*6 genotype-dependent interaction between efavirenz and antituberculosis drug therapy through mechanism-based inactivation of CYP2A6. | Isoniazid | cytochrome P450 family 2 subfamily A member 6 | Homo sapiens |
| 2 | Importantly, isoniazid demonstrated potent time-dependent inhibition of efavirenz 7-hydroxylation in both HLMs (inhibitor concentration required for half-maximal inactivation [KI] = 30 muM; maximal rate constant of inactivation [kinact] = 0.023 min(-1)) and recombinant CYP2A6 (KI = 15 muM; kinact = 0.024 min(-1)) and also formed a metabolite intermediate complex consistent with mechanism-based inhibition. | Isoniazid | cytochrome P450 family 2 subfamily A member 6 | Homo sapiens |
| 3 | In conclusion, the results of this study identify isoniazid as the most likely perpetrator of this clinically important drug-drug interaction through mechanism-based inactivation of CYP2A6. | Isoniazid | cytochrome P450 family 2 subfamily A member 6 | Homo sapiens |