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Drug Interactions between betrixaban and selpercatinib

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Moderate

betrixaban selpercatinib

Applies to: betrixaban and selpercatinib

MONITOR: Coadministration with inhibitors of P-glycoprotein (P-gp) may increase the plasma concentrations of betrixaban, which is a substrate of the efflux transporter. When administered with the potent P-gp inhibitor verapamil, betrixaban peak plasma concentration (Cmax) increased by nearly 5-fold and systemic exposure (AUC) increased by approximately 3-fold compared to betrixaban administered alone. When given with ketoconazole, another P-gp inhibitor, betrixaban Cmax and AUC increased by a little more than 2-fold each. In the Acute Medically Ill Prevention with Extended Duration Betrixaban (APEX) Study, use of betrixaban at a 50% dosage reduction in combination with P-gp inhibitors or in the presence of severe renal impairment was associated with increased relative risks of bleeding, including major bleeding, compared to treatment with enoxaparin.

MANAGEMENT: Caution is advised when betrixaban is used with P-gp inhibitors. Closer monitoring of the pharmacologic effects of betrixaban may be appropriate whenever a P-gp inhibitor is added to or withdrawn from therapy. Patients should be routinely evaluated for signs and symptoms suggesting blood loss such as a drop in hemoglobin and/or hematocrit, hypotension, or fetal distress (in pregnant women). Concomitant use of betrixaban with P-gp inhibitors should be avoided in patients with severe renal impairment (CrCl<30 mL/min).

References (1)
  1. (2017) "Product Information. Bevyxxa (betrixaban)." Portola Pharmaceuticals

Drug and food interactions

Major

selpercatinib food

Applies to: selpercatinib

GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of selpercatinib. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. Inhibition of hepatic CYP450 3A4 may also contribute. The interaction has not been studied with grapefruit juice, but has been reported for other CYP450 3A4 inhibitors. When a single dose of selpercatinib (160 mg) was coadministered with multiple doses of itraconazole (200 mg once daily), a potent CYP450 3A4 inhibitor, selpercatinib peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 30% and 133%, respectively. Based on pharmacokinetic modeling, administration of multiple doses of selpercatinib (160 mg twice daily) with multiple doses of the moderate CYP450 3A4 inhibitors diltiazem (60 mg three times daily), fluconazole (200 mg once daily), or verapamil (80 mg three times daily) is predicted to increase selpercatinib Cmax by 46% to 76% and AUC by 60% to 99%. 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 selpercatinib may increase the risk of serious adverse effects such as QT interval prolongation, liver transaminase and bilirubin elevations, hypertension, hemorrhage, edema, and hypersensitivity reactions (e.g., fever, rash, arthralgias/myalgias with concurrent decreased platelets or transaminitis).

MANAGEMENT: Until further information is available, it may be advisable for patients to limit or avoid consumption of grapefruit and grapefruit juice during treatment with selpercatinib.

References (4)
  1. (2024) "Product Information. Retevmo (selpercatinib)." Lilly, Eli and Company
  2. (2023) "Product Information. Retevmo (selpercatinib)." Eli Lilly Australia Pty Ltd, vA1.0
  3. (2024) "Product Information. Retsevmo (selpercatinib)." Eli Lilly and Company Ltd
  4. (2024) "Product Information. Retevmo (selpercatinib)." Loxo Oncology Inc
Moderate

betrixaban food

Applies to: betrixaban

ADJUST DOSING INTERVAL: Food reduces the oral bioavailability of betrixaban. When administered with a low-fat (900 calories; 20% fat) or high-fat (900 calories; 60% fat) meal, betrixaban peak plasma concentration (Cmax) and systemic exposure (AUC) decreased relative to administration in the fasting state by an average of 70% and 61%, respectively, with the low-fat meal and 50% and 48%, respectively, with the high-fat meal. The effect of food on betrixaban pharmacokinetics could be observed for up to 6 hours after meal intake.

MANAGEMENT: The manufacturer recommends taking betrixaban at the same time each day with food.

References (1)
  1. (2017) "Product Information. Bevyxxa (betrixaban)." Portola Pharmaceuticals

Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

Further information

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