ib and imatinib are both moderate inhibitors and substrates of CYP3A4.
Imipramine: (Major) Avoid coadministration of ribociclib with imipramine due to an increased risk for QT prolongation. Systemic exposure of imipramine may also be increased resulting in increase in treatment-related adverse reactions. Ribociclib has been shown to prolong the QT interval in a concentration-dependent manner. Tricyclic antidepressants (TCAs) share pharmacologic properties similar to the Class IA antiarrhythmic agents and may prolong the QT interval, particularly in overdose or with higher-dose prescription therapy (elevated serum concentrations). Concomitant use may increase the risk for QT prolongation. Ribociclib is also a moderate CYP3A4 inhibitor and imipramine is a CYP3A4 substrate.
Indacaterol: (Moderate) Due to a possible risk for QT prolongation, ribociclib and long-acting beta-agonists should be used together cautiously. Beta-agonists may be associated with adverse cardiovascular effects including QT interval prolongation, usually at higher doses, when associated with hypokalemia, or when used with other drugs known to prolong the QT interval like ribociclib. This risk may be more clinically significant with long-acting beta-agonists such as indacaterol as compared to short-acting beta-agonists. Ribociclib is also a moderate CYP3A4 inhibitor and indacaterol is a CYP3A4 substrate.
Indacaterol; Glycopyrrolate: (Moderate) Due to a possible risk for QT prolongation, ribociclib and long-acting beta-agonists should be used together cautiously. Beta-agonists may be associated with adverse cardiovascular effects including QT interval prolongation, usually at higher doses, when associated with hypokalemia, or when used with other drugs known to prolong the QT interval like ribociclib. This risk may be more clinically significant with long-acting beta-agonists such as indacaterol as compared to short-acting beta-agonists. Ribociclib is also a moderate CYP3A4 inhibitor and indacaterol is a CYP3A4 substrate.
Indinavir: (Major) Avoid coadministration of ribociclib with indinavir, as the systemic exposure of both drugs may be increased resulting in an increase in treatment-related adverse reactions (e.g., neutropenia, QT prolongation); consider alternative treatment with less potential for CYP3A inhibition. If concomitant use is unavoidable, reduce the dose of ribociclib to 400 mg once daily; if indinavir is discontinued, the original dose of ribociclib may be resumed after at least 5 half-lives of indinavir. Ribociclib is extensively metabolized by CYP3A4 and indinavir is a strong CYP3A4 inhibitor. Ribociclib is also a moderate CYP3A4 inhibitor and indinavir is a sensitive CYP3A4 substrate.
Irinotecan: (Moderate) Use caution if coadministration of ribociclib with irinotecan is necessary, as the systemic exposure of irinotecan may be increased resulting in an increase in treatment-related adverse reactions including diarrhea, nausea, vomiting, and myelosuppression. Ribociclib is a moderate CYP3A4 inhibitor and irinotecan is a CYP3A4 substrate.
Isavuconazonium: (Moderate) Use caution if coadministration of ribociclib with isavuconazonium is necessary, as the systemic exposure of isavuconazole, the active component, may be increased resulting in increase in treatment-related adverse reactions. Exposure to ribociclib may also increase, increasing in ribociclib-related adverse reactions (e.g., neutropenia, QT prolongat |
