Pub. Date : 2010 Nov
PMID : 20959500
6 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Induction of CYP3A4 by vinblastine: Role of the nuclear receptor NR1I2. | Vinblastine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 2 | OBJECTIVE: To evaluate the CYP3A4 induction potential of vinblastine both clinically and in vitro and determine the involvement of the nuclear receptors NR1I2 and the constitutive androstane receptor (NR1I3). | Vinblastine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 3 | RESULTS: In 6 patients with cancer, vinblastine increased the median (95% CI) clearance of the CYP3A4 phenotyping probe midazolam from 21.7 L/h (12.6 to 28.1) to 32.3 L/h (17.3 to 53.9) (p = 0.0156, Wilcoxon signed-rank test). | Vinblastine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 4 | In vitro, vinblastine induced CYP3A4 protein. | Vinblastine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 5 | CONCLUSIONS: Collectively, these findings suggest that vinblastine is able to induce CYP3A4, at least in part, via an NR1I2-dependent mechanism, and thus has the potential to facilitate its own elimination and cause interactions with other CYP3A4 substrates. | Vinblastine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 6 | CONCLUSIONS: Collectively, these findings suggest that vinblastine is able to induce CYP3A4, at least in part, via an NR1I2-dependent mechanism, and thus has the potential to facilitate its own elimination and cause interactions with other CYP3A4 substrates. | Vinblastine | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |