产品说明书

Alcaftadine

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Chemical Structure| 147084-10-4 同义名 : R89674;Lastacaft;trade name: Lastacaft
CAS号 : 147084-10-4
货号 : A717146
分子式 : C19H21N3O
纯度 : 99%+
分子量 : 307.389
MDL号 : MFCD09954106
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(130.13 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • H2 receptor

    H2 receptor, pKi:7.2

  • H1 receptor

    H1 receptor, pKi:8.5
描述 Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. It also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects. Alcaftadine was more effective than placebo and at least as effective as olopatadine 0.01% in preventing ocular itching at 15 minutes and at 16 hours after administration[3]. Over a range of formulations and concentrations (0.05%-0.5%), alcaftadine was well tolerated and subjects reported little or no discomfort or taste perversion in any treatment group. Topical administration of alcaftadine 0.25% ophthalmic solution was well tolerated and had an acceptable safety profile[4]. Once-daily alcaftadine 0.25% ophthalmic solution demonstrated greater efficacy in prevention of ocular itching compared with olopatadine 0.2% at 3 min post-CAC (conjunctival allergen challenge) (primary endpoint), and over all time points, 16 h post-treatment instillation. Alcaftadine and olopatadine both provided effective relief compared with placebo and were generally well tolerated[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01390961 Allergic Conjunctivitis Phase 4 Unknown January 2012 United States, California ... 展开 >> Milton M. Hom, OD, FAAO. Azusa, California, United States, 91702 收起 <<
NCT00889330 Allergic Conjunctivitis Phase 3 Completed - United States, Ohio ... 展开 >> Fairfield, Ohio, United States Mason, Ohio, United States 收起 <<
NCT00889330 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.25mL

0.65mL

0.33mL

16.27mL

3.25mL

1.63mL

32.53mL

6.51mL

3.25mL
参考文献

[1]Mahvan TD, Buckley WA, et al. Alcaftadine for the prevention of itching associated with allergic conjunctivitis. Ann Pharmacother. 2012 Jul-Aug;46(7-8):1025-32.

[2]Namdar R, Valdez C. Alcaftadine: a topical antihistamine for use in allergic conjunctivitis. Drugs Today (Barc). 2011 Dec;47(12):883-90.

[3]Namdar R, Valdez C. Alcaftadine: a topical antihistamine for use in allergic conjunctivitis. Drugs Today (Barc). 2011 Dec;47(12):883-90

[4]Bohets H, McGowan C, Mannens G, Schroeder N, Edwards-Swanson K, Shapiro A. Clinical pharmacology of alcaftadine, a novel antihistamine for the prevention of allergic conjunctivitis. J Ocul Pharmacol Ther. 2011 Apr;27(2):187-95

[5]McLaurin EB, Marsico NP, Ackerman SL, Ciolino JB, Williams JM, Villanueva L, Hollander DA. Ocular itch relief with alcaftadine 0.25% versus olopatadine 0.2% in allergic conjunctivitis: pooled analysis of two multicenter randomized clinical trials. Adv Ther. 2014 Oct;31(10):1059-71