Itraconazole is a common antifungal developed in the 1980s. It has now been re-purposed for cancer. It is used to prevent or treat chronic fungal infections. It has been clinically used for 30 years with an established safety record.

Retrospective studies of patients with ovarian cancer and recurrent triple negative breast cancer taking itraconazole revealed significant increases in overall survival and is thought to be due to its antiangiogenic effect. Recent studies have shown it to be useful in regulating other pathways.

In 2017 itraconazole was reviewed as an anticancer agent in Oncology Letters. It was found that the anticancer activities included activation of AMP kinase and inhibition of mTOR which inhibits cancer growth. It has also been shown to reverse chemo resistance mediated by P glycoprotein and other cancer pathways.

Another study of cervical cancer cells in vitro in Anticancer Research 2017 showed that itraconazole modulates several different cancer pathways inhibiting cancer cell growth.

In 2019 a phase two clinical trials for recurrent prostate cancer was done. In the study, 19 men were given itraconazole 300 mg orally twice a day for 12 weeks. Of the 19, one had a greater than 50% reduction in the PSA and nine others had a 25% reduction in PSA after 12 weeks of itraconazole.

Itraconazole is also a potent inhibitor of inflammation and the 5 LOX pathways which can inhibit cancer growth.

In 2017 the anticancer effect of oral administration was investigated on gastric cancer cell lines using in vitro and in vivo animal models. They found the remarkable inhibition of gastric cancer cell proliferation. There was down regulation of cancer signals.

In 2017 in Cancer Letters, it was found that itraconazole has an antiproliferative effect of breast cancer cell lines and induced cancer cell death. Also, in 2017 itraconazole was found to inhibit endometrial cancer cell lines.

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