Published research on Itraconazole

5 peer-reviewed publications on Itraconazole in oncology research, clinical work first, then laboratory studies. Each entry reports what the authors stated; follow the link for the full paper.

1. Clinical trial

   Open-label, exploratory phase II trial of oral itraconazole for the treatment of basal cell carcinoma

   Kim DJ et al., Journal of Clinical Oncology, 2014

   In 19 treated patients with basal cell carcinoma, itraconazole reduced tumor cell proliferation by 45%, Hedgehog pathway activity by 65% and tumor area by 24%, with two adverse events reported (grade 2 fatigue and grade 4 congestive heart failure).

2. Clinical trial

   Phase 2 study of pemetrexed and itraconazole as second-line therapy for metastatic nonsquamous non-small-cell lung cancer

   Rudin CM et al., Journal of Thoracic Oncology, 2013

   In a randomized phase 2 study of 23 patients stopped early, adding itraconazole to pemetrexed was associated with a non-significant difference in progression-free survival (5.5 vs 2.8 months, p = 0.089) and longer overall survival (median 32 vs 8 months, p = 0.012), with no evident difference in toxicity.

3. Clinical trial

   Repurposing itraconazole as a treatment for advanced prostate cancer: a noncomparative randomized phase II trial in men with metastatic castration-resistant prostate cancer

   Antonarakis ES et al., The Oncologist, 2013

   In 46 men with chemotherapy-naive metastatic castration-resistant prostate cancer, the high-dose arm met its prespecified 24-week PSA progression-free survival endpoint (48.0%) while the low-dose arm closed early for futility (11.8%), and the authors concluded that high-dose itraconazole had modest antitumor activity not mediated by testosterone suppression.

4. In vivo

   Itraconazole inhibits angiogenesis and tumor growth in non-small cell lung cancer

   Aftab BT et al., Cancer Research, 2011

   Itraconazole inhibited endothelial cell proliferation, migration and tube formation in vitro and, in primary xenograft models of human non-small cell lung cancer, showed single-agent growth-inhibitory activity with reduced tumor vascularity and enhanced the antitumor efficacy of cisplatin.

5. In vivo

   Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growth

   Kim J et al., Cancer Cell, 2010

   In a screen of drugs previously tested in humans, itraconazole was identified as a Hedgehog pathway antagonist acting on Smoothened, and systemic administration suppressed Hedgehog pathway activity and medulloblastoma growth in a mouse allograft model at serum levels comparable to those seen in antifungal therapy.

Itraconazole in the catalog (specifications, pack sizes, Certificate of Analysis)