Itraconazole is an antifungal medication that has been studied as a medication for prostate cancer and lung cancer in a small number of patients.
Safety and precautions
Itraconazole inhibits the enzyme P450 CYP3A4, which helps the body to process and get rid of medications. This means that if someone is taking itraconazole, other medications may stay in their bodies longer, and at a higher dose, than intended. Your physician may need to adjust the doses of other medications if you are taking itraconazole.
Itraconazole can cause serious imbalances including low potassium, edema (swelling), and high blood pressure. Other side effects include fatigue, nausea, anorexia, and rash.
Side effects or adverse events
Among people with prostate cancer taking itraconazole in clinical trials, the most common side effects are a combination of low potassium (hypokalemia), edema, and high blood pressure, which increase with the dose and suggest that itraconazole may cause mineralocorticoid imbalances (imbalances in the hormones that regulate salt and water in the blood).1Antonarakis ES, Heath EI et al. Repurposing itraconazole as a treatment for advanced prostate cancer: a noncomparative randomized phase II trial in men with metastatic castration-resistant prostate cancer. Oncologist. 2013;18(2):163-73 People with prostate cancer also experienced fatigue, nausea, low appetite, and rashes.2Antonarakis ES, Heath EI et al. Repurposing itraconazole as a treatment for advanced prostate cancer: a noncomparative randomized phase II trial in men with metastatic castration-resistant prostate cancer. Oncologist. 2013;18(2):163-73; Lee M, Hong H et al. Itraconazole as a noncastrating treatment for biochemically recurrent prostate cancer: a phase 2 study. Clinical Genitourinary Cancer. 2019 Feb;17(1):e92-e96.
In rare cases, itraconazole can cause heart failure, liver failure, and possibly birth defects when taken during pregnancy.3Kurn H, Wadhwa R. Itraconazole. In: StatPearls [Internet]. 17 Apr 2023.
Interactions with other therapies
Because itraconazole changes the way your body processes medications, it can interact with a wide range of other medications, from dexamethasone to hormone treatments for prostate cancer.4Varis T, Kivistö KT et al. The cytochrome P450 3A4 inhibitor itraconazole markedly increases the plasma concentrations of dexamethasone and enhances its adrenal-suppressant effect. Clinical Pharmacology and Therapeutics. 2000 Nov;68(5):487-94; Gibbons JA, de Vries M et al. Pharmacokinetic drug interaction studies with enzalutamide. Clinical Pharmacokinetics. 2015 Oct;54(10):1057-69. If you are taking itraconazole, your physician may need to adjust the dose of any other medications you take.
Do not use (contraindications)
Contraindications for itraconazole are heart failure and liver failure, since in rare cases, itraconazole can cause heart or liver damage (toxicity).5Kurn H, Wadhwa R. Itraconazole. In: StatPearls [Internet]. 17 Apr 2023. There is mixed data on whether itraconazole may cause birth defects, so it is only prescribed to pregnant people when the benefits outweigh the risks.6Bar-Oz B, Moretti ME et al. Pregnancy outcome after in utero exposure to itraconazole: a prospective cohort study. Am J Obstetrics and Gynecology. 2000 Sep;183(3):617-20.; Kurn H, Wadhwa R. Itraconazole. In: StatPearls [Internet]. 17 Apr 2023.
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References