Perpetrator | In Vitro Substrate | IC_{50} | [I]_{1}/IC_{50} | [I]_{2}/IC_{50} | AUC Ratio | C_{max} Ratio | In Vivo Victim | Reference |
---|---|---|---|---|---|---|---|---|

µM | ||||||||

Alectinib | N/P | 0.1 | 13^{a}^{,}^{b} | 49729^{a}^{,}^{b} | N/T^{c} | FDA (2015b) | ||

Alectinib metabolite M4 | N/P | 2.6 | 0.2 | N/A | ||||

Brexpiprazole | Prazosin | 1.16 | 0.40^{a}^{,}^{b} | 32^{a}^{,}^{b} | 1.12 | Rosuvastatin | FDA (2015v) | |

Brexpiprazole metabolite DM-3411 | Prazosin | 3.04 | 0.047 | N/A | ||||

Cariprazine | N/P | Weak (value N/P) | N/T | FDA (2015zd) | ||||

Cobimetinib | Estrone-3-sulfate | 3.3 | 0.16^{a} | 137^{a}^{,}^{b} | N/T | FDA (2015h) | ||

Daclatasvir | Genistein | 10.9 | 0.21^{a}^{,}^{b} | 30^{a}^{,}^{b} | 1.47 | 1.84 | Rosuvastatin | FDA (2015j) |

Isavuconazonium sulfate | N/P | 92 | 0.19^{a}^{,}^{b} | 20^{a}^{,}^{b} | No effect (value N/P) | Methotrexate | FDA (2015i) | |

Lesinurad | Methotrexate | 62.7% at 100 µM | <0.01 | N/T | FDA (2015zg) | |||

Osimertinib | N/P | 2 | 0.063^{a} | 320^{b} | N/T, PMR | FDA (2015x) | ||

Rolapitant | Cladribine | 0.172 | 10^{b} | 8364^{a}^{,}^{b} | 2.18 | 2.38 | Sulfasalazine | FDA (2015za) |

Selexipag | Methotrexate | 1.9 | 0.017^{a} | 0.42^{a} | N/T | FDA (2015z) | ||

Selexipag metabolite ACT-333679 | Methotrexate | 5.6 | N/A | N/A | ||||

Sonidegib | N/P | 1.5 | 0.98^{a}^{,}^{b} | 783^{a}^{,}^{b} | N/T | FDA (2015t) |

N/P, not provided; N/T, not tested.

↵

^{a}The ratio was calculated by the University of Washington Drug Interaction Database editorial team.↵

^{b}Values exceed the FDA cut-off value of 0.1 ([*I*]_{1}/ IC_{50}) or 10 ([*I*]_{2}/IC_{50}).↵

^{c}A clinical study was recommended in the comments by the FDA reviewers.