Pub. Date : 2002 Jan
PMID : 11868802
3 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | After a 15-min preincubation with NADPH, isoniazid showed an increased inhibitory potency toward CYP1A2, CYP2A6, CYP2C19 and CYP3A4 activities (Ki = 56, 60, 10 and 36 microM, respectively). | Isoniazid | cytochrome P450 family 2 subfamily A member 6 | Homo sapiens |
| 2 | In addition, the inactivation of CYP1A2, CYP2A6, CYP2C19 and CYP3A4 by isoniazid was NADPH-, time- and concentration dependent, and was characterised by Kinact values of 0.11, 0.13, 0.09 and 0.08 min(-1), and K1 values of 285, 173, 112 and 228 microM, respectively. | Isoniazid | cytochrome P450 family 2 subfamily A member 6 | Homo sapiens |
| 3 | CONCLUSIONS: As the peak plasma concentrations of isoniazid are around 30-50 microM, isoniazid at clinically relevant concentrations reversibly inhibits CYP2C19 and CYP3A4 activities, and mechanistically inactivates CYP1A2, CYP2A6, CYP2C19 and CYP3A4 in human liver microsomes. | Isoniazid | cytochrome P450 family 2 subfamily A member 6 | Homo sapiens |