Drug Interactions between elagolix / estradiol / norethindrone and sebetralstat

Consumer information for this interaction is not currently available.

GENERALLY AVOID: Coadministration with grapefruit juice may increase the plasma concentrations of sebetralstat. The mechanism is decreased clearance of sebetralstat due to inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits. The interaction has not been studied with grapefruit juice but has been reported for the potent CYP450 3A4 inhibitor, itraconazole. In a clinical study, sebetralstat peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 2.4-fold and 5.2-fold, respectively, following concomitant administration of the potent CYP450 3A4 inhibitor, itraconazole (200 mg once daily for 6 days). In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands. Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition. Increased exposure to sebetralstat may increase the risk and/or severity of adverse effects such as headache and QT prolongation. The use of sebetralstat alone at doses 2.5 times the maximum recommended dose has been associated with a mean increase in corrected QT (QTc) interval of 10.4 msec. Although clinical data are lacking for sebetralstat, in general, prolongation of the QT interval may increase the risk of ventricular arrhythmias such as ventricular tachycardia and torsade de pointes.

MANAGEMENT: Consumption of food or drinks containing grapefruit should generally be avoided during treatment with sebetralstat.

Grapefruit juice may increase the blood levels of certain medications such as norethindrone. You may want to limit your consumption of grapefruit and grapefruit juice during treatment with norethindrone. However, if you have been regularly consuming grapefruit or grapefruit juice with the medication, then it is advisable for you to talk with your doctor before changing the amounts of these products in your diet, as this may alter the effects of your medication. Contact your doctor if your condition changes or you experience increased side effects. Orange juice is not expected to interact.

Information for this minor interaction is available on the professional version.

Information for this minor interaction is available on the professional version.