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Drug Interactions between eltrombopag and lusutrombopag

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

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Interactions between your drugs

Moderate

eltrombopag lusutrombopag

Applies to: eltrombopag and lusutrombopag

MONITOR: Coadministration with eltrombopag may increase the plasma concentrations of drugs that are substrates of the organic anion transporting polypeptide (OATP) 1B1 and/or breast cancer resistance protein (BCRP) transporters. The mechanism is decreased clearance due to inhibition of OATP1B1-mediated hepatic uptake and BCRP-mediated intestinal and hepatobiliary efflux by eltrombopag. The interaction has been demonstrated for rosuvastatin, a known substrate of both OATP 1B1 and BCRP. In 39 healthy adult subjects given eltrombopag 75 mg once daily for 4 days prior to coadministration with a single 10 mg dose of rosuvastatin on day 5, mean rosuvastatin peak plasma concentration (Cmax) increased by 103% and systemic exposure (AUC) by 55%.

MANAGEMENT: Caution is advised during concomitant use of eltrombopag with drugs that are substrates of the OATP1B1 and/or BCRP transporters, particularly those with a narrow therapeutic range. Dosage adjustments as well as clinical and laboratory monitoring may be appropriate for some drugs whenever eltrombopag is added to or withdrawn from therapy.

References (5)
  1. Canadian Pharmacists Association (2006) e-CPS. http://www.pharmacists.ca/function/Subscriptions/ecps.cfm?link=eCPS_quikLink
  2. Cerner Multum, Inc. "Australian Product Information."
  3. (2008) "Product Information. Promacta (eltrombopag)." GlaxoSmithKline
  4. Kalliokoski A, Niemi M (2009) "Impact of OATP transporters on pharmacokinetics." Br J Pharmacol, 158, p. 693-705
  5. Allred AJ, Bowen CJ, Park JW, et al. (2011) "Eltrombopag increases plasma rosuvastatin exposure in healthy volunteers." Br J Clin Pharmacol, 72, p. 321-9

Drug and food interactions

Moderate

eltrombopag food

Applies to: eltrombopag

ADJUST DOSING INTERVAL: Food may reduce the oral bioavailability of eltrombopag. In healthy volunteers, a standard high-fat breakfast significantly decreased plasma eltrombopag peak plasma concentration (Cmax) by 65% and systemic exposure (AUC) by 59% and delayed Tmax by one hour. The calcium content of this meal may have also contributed to this decrease in exposure. In another study, adult subjects administered a single 25 mg dose of eltrombopag for oral suspension with a high-calcium, moderate-fat, moderate-calorie meal exhibited a 79% decrease in Cmax and 75% decrease in AUC of eltrombopag. Administration of eltrombopag 2 hours after the high-calcium meal decreased eltrombopag Cmax by 48% and AUC by 47%, while administration 2 hours before the high-calcium meal decreased eltrombopag Cmax by 14% and AUC by 20%.

ADJUST DOSING INTERVAL: Polyvalent cations such as aluminum, calcium, iron, magnesium, and zinc can significantly reduce the gastrointestinal absorption of eltrombopag due to chelation. In one clinical trial, administration of a single 75 mg dose of eltrombopag with an antacid containing 1524 mg aluminum hydroxide and 1425 mg magnesium carbonate resulted in an approximately 70% decrease in eltrombopag Cmax and AUC.

MANAGEMENT: Eltrombopag should be taken on an empty stomach one hour before or two hours after a meal. Additionally, eltrombopag should be taken at least 2 hours before or 4 hours after any products that contain polyvalent cations such as antacids, mineral supplements, dairy products, and fortified juices.

References (2)
  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. (2008) "Product Information. Promacta (eltrombopag)." GlaxoSmithKline

Therapeutic duplication warnings

Therapeutic duplication is the use of more than one medicine from the same drug category or therapeutic class to treat the same condition. This can be intentional in cases where drugs with similar actions are used together for demonstrated therapeutic benefit. It can also be unintentional in cases where a patient has been treated by more than one doctor, or had prescriptions filled at more than one pharmacy, and can have potentially adverse consequences.

Duplication

Platelet-stimulating agents

Therapeutic duplication

The recommended maximum number of medicines in the 'platelet-stimulating agents' category to be taken concurrently is usually one. Your list includes two medicines belonging to the 'platelet-stimulating agents' category:

  • eltrombopag
  • lusutrombopag

Note: In certain circumstances, the benefits of taking this combination of drugs may outweigh any risks. Always consult your healthcare provider before making changes to your medications or dosage.

See also

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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

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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