ibitor treatment, due to opposing pharmacologic actions. Aromatase inhibitors (e.g., aminoglutethimide, anastrozole, exemestane, letrozole, testolactone, vorozole) exhibit their antiestrogenic effects by reducing the peripheral conversion of adrenally synthesized androgens (e.g., androstenedione) to estrogens through inhibition of the aromatase enzyme.
Eszopiclone: (Minor) Use caution if ribociclib is coadministered with eszopiclone, as the systemic exposure of eszopiclone may increase, resulting in adverse reactions such as prolonged sedative effects. Ribociclib is a moderate CYP3A4 inhibitor, and eszopiclone is primarily a CYP3A4 substrate. Coadministration with a potent CYP3A4 inhibitor resulted in a 2.2-fold increase in eszopiclone exposure; the effects of coadministration with a moderate CYP3A4 inhibitor have not been clearly defined.
Ethanol: (Moderate) Use caution if coadministration of ribociclib with alcohol is necessary, as the systemic exposure of ribociclib may be decreased resulting in decreased efficacy. Ribociclib is extensively metabolized by CYP3A4 and alcohol is a moderate CYP3A4 inducer. (Moderate) Use caution if coadministration of ribociclib with alcohol is necessary, as the systemic exposure of ribociclib may be decreased resulting in decreased efficacy. Ribociclib is extensively metabolized by CYP3A4 and alcohol is a moderate CYP3A4 inducer. Coadministration with a strong CYP3A4 inducer decreased the ribociclib AUC and Cmax by 89% and 81%, respectively, in healthy volunteers; moderate CYP3A4 inducers may also decrease ribociclib exposure.
Ethinyl Estradiol: (Moderate) Use caution if coadministration of ribociclib with ethinyl estradiol is necessary, as the systemic exposure of ethinyl estradiol may be increased resulting in an increase in estrogenic-related adverse reactions (e.g., nausea, breast tenderness). Ribociclib is a moderate CYP3A4 inhibitor and ethinyl estradiol is a CYP3A4 substrate.
Ethinyl Estradiol; Desogestrel: (Moderate) Use caution if coadministration of ribociclib with ethinyl estradiol is necessary, as the systemic exposure of ethinyl estradiol may be increased resulting in an increase in estrogenic-related adverse reactions (e.g., nausea, breast tenderness). Ribociclib is a moderate CYP3A4 inhibitor and ethinyl estradiol is a CYP3A4 substrate.
Ethinyl Estradiol; Ethynodiol Diacetate: (Moderate) Use caution if coadministration of ribociclib with ethinyl estradiol is necessary, as the systemic exposure of ethinyl estradiol may be increased resulting in an increase in estrogenic-related adverse reactions (e.g., nausea, breast tenderness). Ribociclib is a moderate CYP3A4 inhibitor and ethinyl estradiol is a CYP3A4 substrate.
Ethinyl Estradiol; Etonogestrel: (Moderate) Use caution if coadministration of ribociclib with ethinyl estradiol is necessary, as the systemic exposure of ethinyl estradiol may be increased resulting in an increase in estrogenic-related adverse reactions (e.g., nausea, breast tenderness). Ribociclib is a moderate CYP3A4 inhibitor and ethinyl estradiol is a CYP3A4 substrate. (Minor) Coadministration of etonogestrel and moderate CYP3A4 inhibitors such as ribociclib may increase the serum concentration of etonogestrel.
Ethinyl Estradiol; Levonorgestrel: (Moderate) Use caution if coadministration of ribociclib with ethinyl estradiol is necessary, as the systemic exposure of ethinyl estradiol may be increased resulting in an |
