Ketotifen fumarate blocks histamine1 (H1) receptors, stabilizes mast cells, and acts as an eosinophil inhibitor (decreases chemotaxis and activation of eosinophils). Ketotifen was safe and statistically effective in reducing ocular itching and hyperemia associated with allergic conjunctivitis. Ketotifen's rapid onset of action (within 15 minutes) and extended duration of action (at least 8 hours) make it a valuable treatment for allergic conjunctivitis[3]. Ketotifen is an orally active prophylactic agent for the management of bronchial asthma and allergic disorders. Unlike inhaled sodium cromoglycate, ketotifen ameliorates the symptoms of asthma, rhinitis and dermatitis when present together in atopic patients[4]. Subgroups of animals were treated twice daily for one week with or without ketotifen fumarate (5 mg/kg). Ketotifen fumarate attenuated the initiation and progression of gingivitis and reduced the oxidative stress, and inhibited NF-κB and p38 MAPK related with mast cells and macrophages accumulation[5]. In EAO (experimental autoimmune orchitis) model, KF significantly reduced severity of histopathological testicular damage compared to rats in the vehicle group. KF also reduced the number of testicular MC (Mast cells) compared to vehicle group[6].
Ketotifen fumarate salt/富马酸酮替芬 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MC/9 mast cells
100 µg/mL
24 hours
To evaluate the inhibitory effect of ketotifen on mast cell degranulation, results showed that ketotifen inhibited degranulation in a dose-dependent manner, with 100 µg/mL concentration reducing β-hexosaminidase release by more than 50%.
Clin Cancer Res. 2024 Jun 3;30(11):2582-2597
Ketotifen fumarate salt/富马酸酮替芬 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6OlaHsd mice
Fibrosarcoma and osteosarcoma models
Intraperitoneal injection
10 mg/kg
Once daily for 8 days
To evaluate the effect of ketotifen on tumor stiffness and vascular perfusion, results showed that 10 mg/kg dose significantly reduced tumor stiffness and improved vascular perfusion.
Clin Cancer Res. 2024 Jun 3;30(11):2582-2597
New Zealand white rabbits
Acidified pepsin-induced oesophagitis model
Intravenous injection
0.05 mg/kg
Administered 10 minutes before and during the exposure period
To evaluate the protective effects of ketotifen against OPIDN, results showed it significantly alleviated TOCP-induced symptoms.
Cell Discov. 2017 Aug 1;3:17024
Mice
NMO model
Oral
50 μM
1 day prior to and during the 3-day infusion
To investigate the effect of ketotifen fumarate salt on NMO lesions. Results showed that ketotifen fumarate salt significantly reduced lesion severity and eosinophil infiltration.
J Clin Invest. 2013 May;123(5):2306-16
Mice
Laser-induced choroidal neovascularization model
Intraperitoneal injection
25 mg/kg
Starting 48 h before laser burn and continued daily until the day before sacrifice
To assess the effect of mast cell stabilizer on choroidal neovascularization, results showed ketotifen fumarate significantly reduced CNV lesion size
J Neuroinflammation. 2024 Oct 1;21(1):247
Mice
Early life adversity model (NMSEW)
Intraperitoneal injection
20 mg/kg
30 min before each adult stress episode, for 3 consecutive days
Ketotifen prevented stress-induced reductions in sucrose preference and increases in cma1 expression in NMSEW females, but facilitated stress-induced sucrose anhedonia in NMSEW males and NH females.
Brain Behav Immun. 2022 Jul;103:73-84
Guinea pigs
Airway inflammation model
Intraperitoneal injection
2 mg/kg
Single dose, 30 minutes before mrIL-5 treatment
To investigate the effect of ketotifen fumarate salt on mrIL-5-induced airway inflammation. Results showed that ketotifen reduced the mrIL-5-induced increase in eosinophils, neutrophils, and epithelial cells.
Br J Pharmacol. 1992 Jan;105(1):19-22
Apoe−/− mice
Chronic allergic lung inflammation and atherosclerosis model
Nebulization
70 mg/5 mL
Daily for 3 months
To evaluate the therapeutic effects of ketotifen fumarate salt on chronic allergic lung inflammation and atherosclerosis. Results showed that ketotifen significantly reduced aortic arch lesion CD4+ and CD8+ T cells, mast cells, media SMC loss, lesion cell proliferation, angiogenesis, and apoptosis.
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