Drug Interactions between betrixaban and ivacaftor / lumacaftor
This report displays the potential drug interactions for the following 2 drugs:
- betrixaban
- ivacaftor/lumacaftor
Interactions between your drugs
ivacaftor betrixaban
Applies to: ivacaftor / lumacaftor and betrixaban
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monitoring of the pharmacologic effects of betrixaban may be appropriate whenever a P-gp inhibitor is added to or withdrawn from therapy.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
- (2017) "Product Information. Bevyxxa (betrixaban)." Portola Pharmaceuticals
lumacaftor betrixaban
Applies to: ivacaftor / lumacaftor and betrixaban
GENERALLY AVOID: Coadministration with inducers of P-glycoprotein (P-gp) may reduce the systemic exposure and pharmacodynamic effects of betrixaban, which is a substrate of the efflux transporter. Data evaluating this interaction are not available.
MANAGEMENT: The use of betrixaban with P-gp inducers should generally be avoided. If use is unavoidable, pharmacologic response to betrixaban should be monitored closely.
References
- (2017) "Product Information. Bevyxxa (betrixaban)." Portola Pharmaceuticals
- Gelosa P, Castiglioni L, Tenconi M, et al. (2018) "Pharmacokinetic drug interactions of the non-vitamin K antagonist oral anticoagulants (NOACs)" Pharmacol Res, 135, p. 60-79
Drug and food interactions
ivacaftor food
Applies to: ivacaftor / lumacaftor
GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of ivacaftor. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. Elexacaftor and tezacaftor are also CYP450 3A4 substrates in vitro and may interact similarly with grapefruit juice, whereas lumacaftor is not expected to interact.
ADJUST DOSING INTERVAL: According to prescribing information, systemic exposure to ivacaftor increased approximately 2.5- to 4-fold, systemic exposure to elexacaftor increased approximately 1.9- to 2.5-fold, and systemic exposure to lumacaftor increased approximately 2-fold following administration with fat-containing foods relative to administration in a fasting state. Tezacaftor exposure is not significantly affected by administration of fat-containing foods.
MANAGEMENT: Patients treated with ivacaftor-containing medications should avoid consumption of grapefruit juice and any food that contains grapefruit or Seville oranges. All ivacaftor-containing medications should be administered with fat-containing foods such as eggs, avocados, nuts, meat, butter, peanut butter, cheese pizza, and whole-milk dairy products. A typical cystic fibrosis diet will satisfy this requirement.
References
- (2012) "Product Information. Kalydeco (ivacaftor)." Vertex Pharmaceuticals
- (2015) "Product Information. Orkambi (ivacaftor-lumacaftor)." Vertex Pharmaceuticals
- (2022) "Product Information. Symdeko (ivacaftor-tezacaftor)." Vertex Pharmaceuticals
- (2019) "Product Information. Trikafta (elexacaftor/ivacaftor/tezacaftor)." Vertex Pharmaceuticals
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
- (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.
See also
Report options
Drug Interaction Classification
| Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit. | |
| Moderately clinically significant. Usually avoid combinations; use it only under special circumstances. | |
| 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. | |
| No interaction information available. |
Further information
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