Ciclopirox ethanolamine is a synthetic broad-spectrum antifungal agent belonging to the hydroxypyridone derivative class, exhibiting antifungal, antibacterial, and anti-inflammatory activities. Ciclopirox ethanolamine functions as an iron chelator that chelates polyvalent cations, inhibits metal-dependent enzymes, interferes with mitochondrial transport processes, and affects cell membrane permeability. Ciclopirox ethanolamine shows potential application value in research areas including antitumor therapy, stem cell and developmental biology, neurodegenerative diseases, and autoimmune diseases[1-4].
In vitro, treatment with 0.064-40μM Ciclopirox ethanolamine for 48 hours reduced cell viability, induced apoptosis, and decreased mitochondrial membrane potential in K562, HL-60, Jurkat, RS4-11, OCI-M2, and OCI-AML2 cells[5]. Pretreatment with 0.2-2μM Ciclopirox ethanolamine for 2 hours followed by 8-hour oxygen-glucose deprivation and 24-hour reoxygenation increased cell viability, reduced apoptotic cell proportion, and attenuated cell shrinkage in 661W photoreceptor cells[6]. Treatment with 0-20μM Ciclopirox ethanolamine for 24 hours decreased p-S6K1 and p-4E-BP1 levels and reduced cell numbers in Rh30, RD, MDA-MB-231, MDA-MB-435, PC-3, PCI-13, and SRB1-M7 cells[7].
In vivo, intraperitoneal injection of 10mg/kg Ciclopirox ethanolamine once daily for 27 consecutive days reduced kidney-to-body weight ratio, kidney size, cystic index, blood urea nitrogen levels, Ki67-positive cell proportion in renal tissue, fibrosis degree, and ferritin (FTH1/FTL) protein levels, while increasing LC3B-II and NCOA4 protein levels in renal tissue of Pkd1RC/RC Pkd2+/- polycystic kidney disease (PKD) mice[8]. A single intraperitoneal injection of 10-20mg/kg Ciclopirox ethanolamine improved survival rate, reduced serum ALT and AST levels, ameliorated liver pathological injury, decreased serum and liver IL-1β levels, and attenuated caspase-1 cleavage and IL-1β maturation in liver tissue of LPS-induced septic C57BL/6 mice[9]. Topical application of 1-3μg/eye/drop Ciclopirox ethanolamine three times daily for 5 days reduced corneal epithelial viral shedding, alleviated blepharitis scores, and decreased latent HSV-1 genome copy numbers in trigeminal ganglia of BALB/c mice with corneal scratch infection of HSV-1 KOS[10].
References:
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[2] Starova A, Aly R. The safety and efficacy of ciclopirox olamine for the treatment of seborrheic dermatitis. Expert Opin Drug Saf. 2005 Mar;4(2):235-9.
[3] Sato E, Kohno M, Nakashima T, Niwano Y. Ciclopirox olamine directly scavenges hydroxyl radical. Int J Dermatol. 2008 Jan;47(1):15-8.
[4] Foti C, Diaferio A, Bonamonte D. Allergic contact dermatitis from ciclopirox olamine. Australas J Dermatol. 2001 May;42(2):145.
[5] Zhou H, Chen H, Luo K, et al. Inhibition of autophagy enhances the sensitivity of ciclopirox olamine in human chronic myelogenous leukemia K562 cells. Int J Med Sci. 2025;22(15):4013-4025.
[6] Du E, Jia X, Li X, et al. Neuroprotective effect of ciclopirox olamine in retinal ischemia/reperfusion injury. BMC Mol Cell Biol. 2024 Oct 9;25:22.
[7] Zhou H, Shang C, Wang M, et al. Ciclopirox Olamine inhibits mTORC1 signaling by activation of AMPK. Biochem Pharmacol. 2016 Sep 15;116:39-50.
[8] Radadiya PS, Thornton MM, Puri RV, et al. Ciclopirox olamine induces ferritinophagy and reduces cyst burden in polycystic kidney disease. JCI Insight. 2021 Mar 30;6(9):e141299.
[9] Xia X, You H, Zhang K, et al. Ciclopirox Olamine Inhibits the NLRP3 Inflammasome to Alleviate Inflammatory Diseases. Adv Sci (Weinh). 2026;13:e75704.
[10] Bernier M, Morrison LA, et al. Topical ciclopirox olamine reduces HSV-1 replication and disease in a mouse corneal infection model. Antiviral Res. 2020 Jan;173:104642.