sulting in increase in treatment-related adverse reactions. Ribociclib is a moderate CYP3A4 inhibitor and ethosuximide is a CYP3A4 substrate.
Etonogestrel: (Minor) Coadministration of etonogestrel and moderate CYP3A4 inhibitors such as ribociclib may increase the serum concentration of etonogestrel.
Etoposide, VP-16: (Moderate) Use caution if coadministration of ribociclib with etoposide is necessary, as the systemic exposure of etoposide may be increased resulting in increase in treatment-related adverse reactions. Ribociclib is a moderate CYP3A4 inhibitor and etoposide is a CYP3A4 substrate.
Etravirine: (Moderate) Use caution if coadministration of ribociclib with etravirine is necessary, as the systemic exposure to ribociclib may decrease, resulting in decreased efficacy; exposure to etravirine may also increase, resulting in an increase of treatment-related adverse reactions. Ribociclib is extensively metabolized by CYP3A4 and etravirine is a CYP3A4 inducer. Ribociclib is also a moderate CYP3A4 inhibitor and etravirine is a CYP3A4 substrate.
Everolimus: (Major) Use caution if coadministration of ribociclib, a moderate CYP3A4 inhibitor, with everolimus, a sensitive CYP3A4 substrate, is necessary, as the systemic exposure of everolimus may be increased resulting in an increase in everolimus-related adverse reactions. Everolimus (Afinitor) dose adjustments are recommended for dual moderate CYP3A4 and P-glycoprotein (P-gp) inhibitors, but recommendations are not available for agents that only inhibit CYP3A4. Everolimus (Zortress) doses should be adjusted as necessary to maintain whole blood trough concentrations between 3 and 8 ng/mL.
Ezetimibe; Simvastatin: (Moderate) Use caution if ribociclib is coadministered with simvastatin, as the systemic exposure of simvastatin may increase resulting in simvastatin-related adverse reactions. Ribociclib is a moderate CYP3A4 inhibitor and simvastatin is a CYP3A4 substrate.
Ezogabine: (Major) Avoid coadministration of ribociclib with ezogabine due to an increased risk for QT prolongation. Ribociclib has been shown to prolong the QT interval in a concentration-dependent manner. Ezogabine has been associated with QT prolongation. Concomitant use may increase the risk for QT prolongation.
Felbamate: (Moderate) Use caution if ribociclib is coadministered with felbamate, as exposure to ribociclib may decrease, resulting in reduced efficacy. Ribociclib is extensively metabolized by CYP3A4 and felbamate is a CYP3A4 inducer.
Felodipine: (Moderate) Use caution if coadministration of ribociclib with felodipine is necessary, as the systemic exposure of felodipine may be increased resulting in an increase in treatment-related adverse reactions (e.g., hypotension). Ribociclib is a moderate CYP3A4 inhibitor and felodipine is a CYP3A4 substrate.
Fentanyl: (Moderate) Use caution if coadministration of ribociclib, a moderate CYP3A4 inhibitor, with fentanyl, a CYP3A4 substrate, is necessary, as the systemic exposure of fentanyl may be increased resulting in an increase in fentanyl-related adverse reactions. Monitor patients for respiratory depression and sedation at frequent intervals and adjust the dose of fentanyl if necessary.
Fingolimod: (Major) Avoid coadministration of ribociclib with fingolimod due to an increased risk for QT prolongation and torsade de pointes (TdP). Ribociclib has been shown to prolong the QT interval in a concentration-dependent manner. |
