Ciclopirox (HOE296b) exerts its action by binding to and chelating trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential co-factors for enzymes. Ciclopirox is a synthetic, broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities. This may lead to a loss of activity of enzymes that are essential for cellular metabolism, the organization of cell wall structure and other crucial cell functions. In addition, ciclopirox exerts its anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX).

Ciclopirox induces the activity of HIF-1-mediated reporter genes and the expression of endogenous HIF-1 target genes, including increased levels of mRNA expression, transcription, and vascular endothelial growth factor protein. It exerts a dose-dependent inhibitory effect on the growth of Candida albicans yeast and filamentous cells. Ciclopirox prevents mitochondrial damage induced by H2O2 by maintaining mitochondrial transmembrane potential. In adenocarcinoma SK-HEP-1 cells, Ciclopirox decreases MTT reduction (a marker of mitochondrial function) and completely blocks the release of lactate dehydrogenase (a marker of cell death) stimulated by hydrogen peroxide. In astrocytes treated with SIN-1 under glucose deprivation, Ciclopirox increases and maintains high levels of MTP, also preventing the depletion of adenosine triphosphate. Furthermore, Ciclopirox effectively inhibits the opening of mitochondrial permeability transition pores induced by hydrogen peroxide and protects astrocytes from peroxynitrite toxicity by mitigating mitochondrial dysfunction caused by nitrite.