Anti-fungal Drug Itraconazole Found to Inhibit Angiogenesis

Researchers have found that the anti-fungal drug itraconazole inhibits the formation of new blood vessels (angiogenesis) that is characteristic of diseases such as cancer, diabetic retinopathy, and rheumatoid arthritis.

Itraconazole was one of more than 2400 drugs that were screened by investigators at Johns Hopkins University (Baltimore, MD, USA) for indications of activity as angiogenesis inhibitors. Since it is already approved for human use by the [U.S.] Food and Drugs Administration (FDA), discovery of a possible role for itraconazole as an anti-angiogenesis drug was especially exciting.

Results published in the April 13, 2007, online edition of the journal ACS Chemical Biology revealed that in mice induced to have excess blood vessel growth, treatment with itraconazole reduced blood vessel growth by 67% compared to a placebo. Itraconazole appeared to work by inhibiting the enzyme lanosterol 14-alpha-demethylase (14DM), which is essential for endothelial cell proliferation.

"We were surprised, to say the least, that itraconazole popped up as a potential blocker of angiogenesis,” said senior author Dr. Jun O. Liu, professor of pharmacology at Johns Hopkins University. "We could not have predicted that an anti-fungal drug would have such a role. Itraconazole can be taken orally for fungal infection, and therefore oral delivery may work for angiogenesis as well.”


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