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Drug interactions

Lorlatinib + Rifampin

Severity: Contraindicated

Lorlatinib and Rifampin: contraindicated interaction.

Last updated Sources: US FDA label

For healthcare professionals — reference only. This page is a brief summary, not medical advice and not a substitute for official labeling or clinical judgement. Always verify before prescribing or dispensing.

Summary

Rifampin markedly reduces lorlatinib exposure and in healthy volunteers caused serious liver enzyme elevations when combined with lorlatinib. Efficacy may be lost, and hepatotoxicity is a safety concern, so labeling contraindicates the combination.

What this interaction means in plain words

Lorlatinib and Rifampin are not normally used together. Taking them at the same time is expected to cause harm or make one of them unsafe, so a different medicine is usually chosen for one of the two.

Evidence level: High

Why it happens

Potent induction of CYP3A4 (and other pathways) increases lorlatinib clearance.

What to do

Do not combine; use an alternative antimycobacterial regimen where possible. Stop rifampin for about 3 half-lives before starting lorlatinib.

What to ask your pharmacist

  • Is there an alternative to one of these two medicines for me?
  • If both are essential, who is monitoring me and how often?
  • Which symptoms mean I should stop and seek help straight away?

Bring a full list of your medicines, including over-the-counter products, supplements and herbal remedies, to every pharmacy visit.

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References

Frequently asked questions

Can I take Lorlatinib with Rifampin?

MediHelp rates the interaction as contraindicated. Lorlatinib and Rifampin are not normally used together. Taking them at the same time is expected to cause harm or make one of them unsafe, so a different medicine is usually chosen for one of the two. Rifampin markedly reduces lorlatinib exposure and in healthy volunteers caused serious liver enzyme elevations when combined with lorlatinib. Efficacy may be lost, and hepatotoxicity is a safety concern, so labeling contraindicates the combination.

How serious is the interaction between Lorlatinib and Rifampin?

MediHelp rates it contraindicated, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Do not combine; use an alternative antimycobacterial regimen where possible. Stop rifampin for about 3 half-lives before starting lorlatinib.

What other medicines interact with Lorlatinib?

MediHelp also lists interactions of Lorlatinib with, for example, Amobarbital, Apalutamide, Butabarbital. The full list is on the Lorlatinib page.

Full monographs, dosing and an interaction checker in the MediHelp app

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