Ebastine is a second-generation histamine H1 receptor antagonist that is used to attenuate allergic inflammation. Ebastine was shown to significantly increase the proliferation of HFDPC (human follicle dermal papilla cells)[3]. Ebastine is a well-established second generation oral H1-antihistamine that is administered once daily at a dose of 10 - 20 mg and is available both as a standard tablet and as a fast-dissolving tablet that disintegrates in the mouth. Ebastine has been shown to relieve symptoms in patients with allergic rhinitis or urticaria in multiple clinical trials. Ebastine is generally well tolerated at recommended doses[4]. Pooled data from clinical efficacy trials of ebastine 1 - 30 mg/day administered for 2 - 3 weeks showed no clinically relevant cardiac effects as assessed by serial electrocardiographs and Holter monitoring[5]. Ebastine 10 mg daily is a well tolerated and effective treatment for allergic rhinitis and chronic idiopathic urticaria[6]. Ebastine 20 mg/day is indicated in patients with moderate and severe allergic symptoms, it has no relevant effects on the psychomotor performance[7].
Ebastine/依巴斯汀 细胞实验
Cell Line
Concentration
Treated Time
Description
References
U2OS cells
15.505 µM
48 h
Ebastine significantly inhibited the growth of U2OS cells and induced cell cycle arrest and apoptosis.
Int J Biol Sci. 2023 Jan 1;19(2):537-551.
MG63 cells
13.254 µM
48 h
Ebastine significantly inhibited the growth of MG63 cells and induced cell cycle arrest and apoptosis.
Int J Biol Sci. 2023 Jan 1;19(2):537-551.
MNNG cells
13.635 µM
48 h
Ebastine significantly inhibited the growth of MNNG cells and induced cell cycle arrest and apoptosis.
Int J Biol Sci. 2023 Jan 1;19(2):537-551.
Rat isolated heart
605.7 to 383.3 ng·mL⁻¹
130 min
To investigate the pharmacokinetics of ebastine in rat heart, showing that ebastine was metabolized to hydroxyebastine and further to carebastine.
Br J Pharmacol. 2011 Aug;163(8):1733-9.
NIH/3T3 cells
0.01-40 μM
48 h
Evaluate the sensitivity of EBA to normal cells, showing higher sensitivity to TNBC cells than normal cells
Cell Mol Life Sci. 2023 Apr 25;80(5):132.
4T1 cells
0-40 μM
24-48 h
Evaluate the effect of EBA on TNBC cell viability, showing concentration-dependent reductions in cell viability
Cell Mol Life Sci. 2023 Apr 25;80(5):132.
BT549 cells
0-40 μM
24-48 h
Evaluate the effect of EBA on TNBC cell viability, showing concentration-dependent reductions in cell viability
Cell Mol Life Sci. 2023 Apr 25;80(5):132.
MDA-MB-231 cells
0-40 μM
24-48 h
Evaluate the effect of EBA on TNBC cell viability, showing concentration-dependent reductions in cell viability
Cell Mol Life Sci. 2023 Apr 25;80(5):132.
HepG2 cells
5 or 10 μM
16 or 24 h
To investigate the effect of ebastine on MKRN1 protein levels, results showed that ebastine decreased MKRN1 protein levels, which was reversed by the proteasome inhibitor MG132.
Cell Mol Life Sci. 2025 Jan 31;82(1):66.
LAD2 human mast cells
3 μg/mL
20 h
To study the inhibitory effect of ebastine on MC degranulation, results showed ebastine significantly reduced the induction of inflammatory factors by MC degranulation
Virol Sin. 2024 Apr;39(2):309-318.
Ebastine/依巴斯汀 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
Subcutaneous transplantation model and lung metastasis model
Oral
0.5 mg/day and 1 mg/day
Once daily for 30/45 days
Ebastine significantly inhibited tumor growth and lung metastasis, with no obvious toxic effects observed.
Int J Biol Sci. 2023 Jan 1;19(2):537-551.
Wistar rats
Isolated heart perfusion model
Perfusion
7.8 to 12.1 mg
Single dose, 130 minutes duration
To evaluate the pharmacokinetics and negative inotropic effect of ebastine in rat heart, showing metabolism to hydroxyebastine and carebastine with significant negative inotropic effects.
Br J Pharmacol. 2011 Aug;163(8):1733-9.
Guinea pigs
Arrhythmogenicity model
Oral
20 mg/kg
Single dose, recorded for 4 hours
Evaluate the effect of ketoconazole on Ebastine-induced QTc interval prolongation; results showed Ebastine did not further prolong QTc interval after ketoconazole pretreatment
Br J Pharmacol. 1996 Sep;119(2):187-8
BALB/c mice
BCSC-enriched 4T1 allograft model
Intraperitoneal injection
20 mg/kg
Every other day for 34 days
Evaluate the effect of EBA on BCSC-enriched tumor growth, showing significant inhibition of tumor growth and metastasis
Cell Mol Life Sci. 2023 Apr 25;80(5):132.
Mice
High-fat-high-fructose diet (HFHFD)-induced MASH model
Intraperitoneal injection
1 and 5 mg/kg
Daily injections for 4 weeks
To investigate the protective effect of ebastine on HFHFD-induced MASH, results showed that ebastine significantly reduced the risk of MASH, with a decrease in MKRN1 expression and an increase in AMPK activity.
Cell Mol Life Sci. 2025 Jan 31;82(1):66.
CB17SCID mice
Triple-negative breast cancer (SUM159) xenograft model
Oral
30 mg/kg
5 days per week, for about 28 days
To evaluate the effect of ebastine on tumor growth and progression in triple-negative breast cancer
Mol Cancer Ther. 2020 Oct;19(10):2023-2033
C57BL/6N-ACE2em2(hACE2-WPRE, pgk-puro)/CCLA mice
SARS-CoV-2 infection model
Intraperitoneal injection
5 mg/kg
Daily administration, continued until 5 days post-infection
To study the protective effect of ebastine on SARS-CoV-2-induced tracheal injury, results showed ebastine significantly reduced MC degranulation and tracheal injury
Korea, Republic of
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Division of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Seoul Metropolitan Government, Seoul National University Boramae Medical Center
Seoul, Dongjak-Gu, Korea, Republic of, 156-707 收起 <<
Korea, Republic of
... 展开 >>
Division of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Seoul Metropolitan Government, Seoul National University Boramae Medical Center
Seoul, Dongjak-Gu, Korea, Republic of, 156-707 收起 <<
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