Drug interactions
Ketoconazole + Pexidartinib
Severity: Major
Ketoconazole and Pexidartinib: major interaction.
Last updated
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
Ketoconazole increases pexidartinib exposure, which may worsen hepatotoxicity, a serious risk of this drug. Pexidartinib is also cleared partly by glucuronidation, adding to the exposure increase.
What this interaction means in plain words
Ketoconazole and Pexidartinib can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for.
Ketoconazole belongs to Anti Fungals; Pexidartinib belongs to Oncology.
Why it happens
Inhibition of CYP3A4 metabolism and possibly UGT1A4 glucuronidation of pexidartinib.
What to do
Avoid the combination if possible; if required, reduce the pexidartinib dose per labeling and monitor liver tests closely.
What to ask your pharmacist
- Does the benefit of taking both outweigh the risk in my case?
- Do I need any blood test, ECG or other check while on both?
- What early warning signs should I watch for, and what should I do if they appear?
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Other interactions of Ketoconazole
- Alfuzosin + Ketoconazole Contraindicated
- Alprazolam + Ketoconazole Contraindicated
- Avanafil + Ketoconazole Contraindicated
- Conivaptan + Ketoconazole Contraindicated
- Dihydroergotamine intranasal + Ketoconazole Contraindicated
- Dihydroergotamine + Ketoconazole Contraindicated
Other interactions of Pexidartinib
Frequently asked questions
Can I take Ketoconazole with Pexidartinib?
MediHelp rates the interaction as major. Ketoconazole and Pexidartinib can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for. Ketoconazole increases pexidartinib exposure, which may worsen hepatotoxicity, a serious risk of this drug. Pexidartinib is also cleared partly by glucuronidation, adding to the exposure increase.
How serious is the interaction between Ketoconazole and Pexidartinib?
MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Avoid the combination if possible; if required, reduce the pexidartinib dose per labeling and monitor liver tests closely.
What other medicines interact with Ketoconazole?
MediHelp also lists interactions of Ketoconazole with, for example, Alfuzosin, Alprazolam, Avanafil. The full list is on the Ketoconazole page.
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