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Drug Interactions between halofantrine and Lazcluze

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

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Interactions between your drugs

Moderate

halofantrine lazertinib

Applies to: halofantrine and Lazcluze (lazertinib)

MONITOR: Lazertinib may increase the concentration and adverse effects of drugs which rely on CYP450 3A4 and/or breast cancer resistance protein (BCRP) for clearance via inhibition of the isoenzyme and/or the efflux transporter. However, for drugs whose therapeutic effects are dependent on the formation of active metabolites via CYP450 3A4 (e.g., amiodarone, cyclophosphamide, ifosfamide), inhibition of this isoenzyme may result in a reduction in efficacy. In one pharmacokinetic study, healthy participants (n=20) received the sensitive CYP450 3A4 substrate midazolam and BCRP substrate rosuvastatin at baseline and again with steady-state lazertinib. Coadministration increased midazolam's peak plasma concentration (Cmax) and systemic exposure (AUC) by 1.4- and 1.5-fold, respectively. Likewise, rosuvastatin's Cmax and AUC increased by 2.2- and 2-fold, respectively. Data for less sensitive substrates or drugs metabolized and/or transported by multiple routes are unavailable.

MANAGEMENT: Caution is advised if lazertinib is used concurrently with agents that are substrates of CYP450 3A4 and/or the efflux transporter BCRP. This may be particularly important in cases where minimal changes in the substrate's concentration could result in serious adverse reactions (if the agent is cleared via CYP450 3A4 and/or BCRP) or a significant reduction in efficacy (if the medication has active metabolites formed via CYP450 3A4). Dose adjustments and/or increased monitoring may be required. Consultation with the labeling of the substrate in question is advised.

References (2)
  1. (2024) "Product Information. Lazcluze (lazertinib)." Janssen Biotech, Inc.
  2. Mehta J, Sanga M, Haddish-Berhane N, et al. (2024) PII-110-drug-drug interaction effect of steady state lazertinib exposure on the single-dose pharmacokinetics of midazolam, rosuvastatin and metformin. https://ascpt2024.eventscribe.net/fsPopup.asp?PosterID=656218&mode=posterInfo

Drug and food interactions

Major

halofantrine food

Applies to: halofantrine

GENERALLY AVOID: Grapefruit juice may increase the plasma concentration of halofantrine. The mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits. After administration of 500 mg with 250 mL regular-strength grapefruit juice daily for 3 days, average halofantrine AUC increased 2.8-fold and peak plasma concentrations increased 3.2-fold, compared to water, in healthy subjects (n=12). QT interval prolongation increased from an average of 17 ms with water to 31 ms with grapefruit juice. Halofantrine, even at recommended doses, can cause dose-related prolongation of the QT interval, resulting in an elevated risk of potentially fatal ventricular arrhythmias including ventricular tachycardia and torsade de pointes.

ADJUST DOSING INTERVAL: The presence of food may increase the absorption and toxicity of halofantrine. Peak plasma concentrations increased seven-fold and AUC increased three-fold in healthy subjects when halofantrine was administered with high-fat food.

MANAGEMENT: The authors of the study recommend that grapefruit juice be avoided during halofantrine therapy. The manufacturer recommends performing an ECG before initiating halofantrine therapy and cardiac monitoring during and for 8 to 12 hours after completion of therapy. Halofantrine should be taken on an empty stomach at least 1 hour before or 2 hours after food.

References (4)
  1. Giao PT, de Vries PJ (2001) "Pharmacokinetic interactions of antimalarial agents." Clin Pharmacokinet, 40, p. 343-73
  2. (2003) "Product Information. Halfan (halofantrine)." GlaxoSmithKline
  3. Charbit B, Becquemont L, Lepere B, Peytavin G, Funck-Bretano C (2002) "Pharmacokinetic and pharmacodynamic interaction between grapefruit juice and halofantrine." Clin Pharmacol Ther, 72, p. 514-23
  4. Abernethy DR, Wesche DL, Barbey JT, et al. (2001) "Stereoselective halofantrine disposition and effect: concentration-related QTc prolongation." Br J Clin Pharmacol, 51, p. 231-7

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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