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Does Ketoconazole Interact with Irinotecan Hydrochloride?

Ketoconazole and Irinotecan Hydrochloride have a contraindicated drug interaction according to U.S. FDA drug labeling data. CYP3A4 and UGT1A1 inhibitor increases exposure to irinotecan and active metabolite SN-38. Do not administer unless no therapeutic alternatives. The mechanism involves cyp3a4 and ugt1a1 inhibition. Patients taking both medications should consult their healthcare provider before starting, stopping, or changing the dosage of either drug. This information is based on official FDA drug labeling sourced from OpenFDA and the NIH National Library of Medicine.

Severity
Contraindicated
Ketoconazole Class
Azole Antifungal
Management
Do not take together
Data Source
U.S. FDA via OpenFDA

How This Interaction Works

The interaction between Ketoconazole and Irinotecan Hydrochloride occurs because cyp3a4 and ugt1a1 inhibition. Clinically, this means cyp3a4 and ugt1a1 inhibitor increases exposure to irinotecan and active metabolite sn-38. do not administer unless no therapeutic alternatives. Because of the severity of this interaction, these medications are contraindicated — meaning they should not be taken together under any circumstances. If you are currently taking both, contact your healthcare provider immediately to discuss alternatives.

What To Tell Your Doctor or Pharmacist

If you are taking Ketoconazole and your doctor is considering prescribing Irinotecan Hydrochloride (or vice versa), make sure to:

  • Inform your doctor and pharmacist of all current medications, including over-the-counter drugs and supplements
  • Ask whether the benefits of combining these medications outweigh the risks for your specific situation
  • Ask what symptoms to watch for that would indicate the interaction is causing problems
  • Ask about alternative medications that do not interact with your current regimen
  • Ask how frequently you should be monitored while these are co-prescribed
  • Never stop or change either medication without first consulting your healthcare provider
💊 Ketoconazole(T8 Keto Flush)+💊 Irinotecan Hydrochloride(Camptosar)

Severity & Interaction Details

⛔
contraindicated
Avoid this combination
FDA labeling lists this pair as contraindicated. The risk outweighs the benefit in nearly all cases.
Severity scale
MinorContra
On record
Yes
Drug A class
Azole Antifungal
Drug B class
—
Source
NLP:irinotecan hydrochloride

What this means in plain English

CYP3A4 and UGT1A1 inhibitor increases exposure to irinotecan and active metabolite SN-38. Do not administer unless no therapeutic alternatives.

About Ketoconazole and Irinotecan Hydrochloride

Ketoconazole is an Azole Antifungal. You may recognize them by the brand names Ketodan and Camptosar. Ketoconazole is taken by mouth, whereas Irinotecan Hydrochloride is given by intravenous (IV) infusion. Both Ketoconazole and Irinotecan Hydrochloride carry an FDA boxed warning — the agency's most serious safety designation.

What the FDA label says

"CYP3A4 and UGT1A1 inhibition"

📖 Source: NLP:irinotecan hydrochloride

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Data integrity: Every interaction shown is extracted directly from official U.S. FDA drug labeling via openFDA and the U.S. National Library of Medicine (NIH) — no interactions are invented, inferred, or manually edited. Maintained by CheckDrugInteractions.com. See our methodology or report a correction at support@checkdruginteractions.com.

Data sourced from U.S. FDA drug labeling via openFDA and the NIH National Library of Medicine, supplemented with a small number of well-established interactions from curated clinical references. For informational purposes only. Always consult your pharmacist or physician.