Pub. Date : 2018 Apr
PMID : 29273968
12 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | SimCYP, a physiologically based PK model, was developed and used to predict the effects of fluconazole and CYP2C9 genetic polymorphism on siponimod metabolism. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 2 | RESULTS: Correlation analysis suggested that CYP2C9 is the main enzyme responsible for siponimod metabolism in humans. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 3 | Compared with the CYP2C9*1/*1 genotype, HLM incubations from CYP2C9*3/*3 and CYP2C9*2/*2 donors showed ~ 10- and 3-fold decrease in siponimod metabolism, respectively. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 4 | Compared with the CYP2C9*1/*1 genotype, HLM incubations from CYP2C9*3/*3 and CYP2C9*2/*2 donors showed ~ 10- and 3-fold decrease in siponimod metabolism, respectively. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 5 | Simulations of enzyme contribution predicted that in the CYP2C9*1/*1 genotype, CYP2C9 is predominantly responsible for siponimod metabolism (~ 81%), whereas in the CYP2C9*3/*3 genotype, its contribution is reduced to 11%. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 6 | Simulations of enzyme contribution predicted that in the CYP2C9*1/*1 genotype, CYP2C9 is predominantly responsible for siponimod metabolism (~ 81%), whereas in the CYP2C9*3/*3 genotype, its contribution is reduced to 11%. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 7 | Simulations of enzyme contribution predicted that in the CYP2C9*1/*1 genotype, CYP2C9 is predominantly responsible for siponimod metabolism (~ 81%), whereas in the CYP2C9*3/*3 genotype, its contribution is reduced to 11%. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 8 | The predicted exposure increase of siponimod with fluconazole 200 mg was 2.0-2.4-fold for CYP2C9*1/*1 genotype. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 9 | In silico simulation predicted a significant reduction in siponimod clearance in the CYP2C9*2/*2 and CYP2C9*3/*3 genotypes based on the in vitro metabolism data; the predicted exposure was close (within 30%) to the observed results for the CYP2C9*2/*3 and CYP2C9*3/*3 genotypes. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 10 | In silico simulation predicted a significant reduction in siponimod clearance in the CYP2C9*2/*2 and CYP2C9*3/*3 genotypes based on the in vitro metabolism data; the predicted exposure was close (within 30%) to the observed results for the CYP2C9*2/*3 and CYP2C9*3/*3 genotypes. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 11 | In silico simulation predicted a significant reduction in siponimod clearance in the CYP2C9*2/*2 and CYP2C9*3/*3 genotypes based on the in vitro metabolism data; the predicted exposure was close (within 30%) to the observed results for the CYP2C9*2/*3 and CYP2C9*3/*3 genotypes. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |
| 12 | In silico simulation predicted a significant reduction in siponimod clearance in the CYP2C9*2/*2 and CYP2C9*3/*3 genotypes based on the in vitro metabolism data; the predicted exposure was close (within 30%) to the observed results for the CYP2C9*2/*3 and CYP2C9*3/*3 genotypes. | siponimod | cytochrome P450 family 2 subfamily C member 9 | Homo sapiens |