Alexidine 2HCl (dihydrochloride) is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis. Alexidine 2HCl (AXD) as a drug with the highest antifungal and antibiofilm activity against a diverse range of fungal pathogens. AXD significantly potentiated the efficacy of fluconazole against biofilms, displayed low mammalian cell toxicity, and eradicated biofilms growing in mouse central venous catheters in vivo, highlighting its potential as a pan-antifungal drug. AXD has pronounced antifungal activity, including against preformed biofilms, at concentrations lower than mammalian cell toxicity. AXD potentiated the activity of fluconazole and amphotericin B against Candida biofilms in vitro and prevented biofilm growth in vivo[1]. Alexidine was effective in killing the trophozoites at a concentration of 10 mg/mL. However, a higher concentration of Alexidine (100 mg/mL) is required to kill Acanthamoeba cysts and the cytotoxic activities of Alexidine are comparable with chlorhexidine. both Alexidine and chlorhexidine at 100 mg/mL induced significant cytopathic effect on the corneal epithelial cells in vitro[2]. lexidine dihydrochloride (AD) is a bisbiguanide compound commonly used as an oral disinfectant and in contact lens solutions. It possesses antimicrobial, anti-inflammatory and anticancer properties. AD inhibits OC formation and bone resorption in vitro and exert prophylatic protection against LPS-induced osteolysis in vivo[3]. Alexidine dihydrochloride did not interfere with the activities of cisplatin, 5-fluorouracil, or radiation, and interacted in a less-than-additive manner. FaDu ((human hypopharyngeal squamous cancer)) cell clonogenic survival was reduced to < 5% with 1 mM alexidine dihydrochloride, and, correspondingly, this compound decreased the in vivo tumor-forming potential of FaDu cells[4].
Alexidine 2HCl/阿来西定二盐酸盐 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HepG2 cells
3.3 μM
ameliorate oleic acid-induced lipid accumulation
Nat Commun. 2017 Dec 22;8(1):2270
HeLa cells
3.3 μM
4 h
promote autophagic flux and TFEB nuclear translocation
Nat Commun. 2017 Dec 22;8(1):2270
Enterococcus faecalis
1%
5 and 10 min
To compare the antimicrobial activity of 1% Alexidine with that of 2% chlorhexidine against Enterococcus faecalis. Results showed that both 1% Alexidine and 2% chlorhexidine significantly reduced bacterial counts after 5 and 10 minutes of soaking, with no significant difference between the two agents.
Int J Oral Sci. 2013 Mar;5(1):26-31
Enterococcus faecalis D1
2%–0.0078%
1 and 5 min
To evaluate the efficacy of Alexidine alone and combined with N-acetylcysteine against biofilms of a clinical isolate Enterococcus faecalis D1. Results showed that after 1 min exposure, Alexidine eradicated biofilms at all concentrations except the two lowest; after 5 min, all concentrations achieved complete eradication. Combination with NAC showed similar results.
Int J Oral Sci. 2013 Sep;5(3):146-9
Enterococcus faecalis ATCC 29212
2%–0.0078%
1 and 5 min
To evaluate the efficacy of Alexidine alone and combined with N-acetylcysteine against biofilms of two Enterococcus faecalis strains. Results showed that after 1 min exposure, Alexidine eradicated biofilms at all concentrations except the lowest; after 5 min, all concentrations achieved complete eradication. Combination with NAC did not significantly enhance its antimicrobial activity.
Int J Oral Sci. 2013 Sep;5(3):146-9
Trichophyton rubrum
0.64 µg/ml
4 days
Evaluate the in vitro antifungal activity of AXD against T. rubrum, with an MIC80 of 0.64 µg/ml
Front Cell Infect Microbiol. 2022 Sep 2;12:958497
Trichophyton mentagrophytes
0.32 µg/ml
4 days
Evaluate the in vitro antifungal activity of AXD against T. mentagrophytes, with an MIC80 of 0.32 µg/ml
Front Cell Infect Microbiol. 2022 Sep 2;12:958497
Streptococcus mutans biofilm
0.2%, 0.5%, 1%, 2%
1 minute
To evaluate the antimicrobial activity of Alexidine against SM biofilm formed on dentin. All tested ALX concentrations (0.2%, 0.5%, 1%, 2%) achieved kill percentages higher than 99%, with 2% and 1% ALX showing eradication in most specimens.
Ann Clin Microbiol Antimicrob. 2014 Aug 20;13:41
alveolar macrophage (MH-S) cells
0.25 μM
6 h
Inhibited PLB activity by 66%, significantly reduced adhesion and internalization of yeast cells by MH-S cells, down-regulated phagocytosis-related genes (trl2, cd14) and inflammatory response genes (nfkb, tnf-a, il-1b)
BMC Microbiol. 2010 Sep 15;10:241
Alexidine 2HCl/阿来西定二盐酸盐 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
NOG mice
HCC xenograft model
Intraperitoneal injection
AD (0.25 mg/kg) and Era (15 mg/kg)
Twice weekly for 5 weeks
Evaluate the therapeutic efficacy of combined AD and Erastin treatment in HCC xenograft model
Cell Death Dis. 2025 Apr 6;16(1):257
Mice
High-fat diet-induced fatty liver model
Intravenous injection
1 mg/kg
Three times a week for three weeks
Improve lipid metabolism and insulin resistance
Nat Commun. 2017 Dec 22;8(1):2270
Male ICR mice
Diabetic mouse model
Topical application
20 µg
Once daily for 6 days
Evaluate the therapeutic efficacy of AXD in a diabetic mouse model of dermatophytosis, showing comparable outcomes to the standard care drug terbinafine with 100% clinical and mycological cure
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