LFA-1 (lymphocyte function-associated antigen-1) antagonist, used to treat ocular vascular complications. Lifitegrast\xa0 is a new type of T cell integrin antagonist designed to mimic the binding epitope of ICAM-1.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ANTAGONIST
Mechanism of action
Integrin alpha-L/beta-2 (LFA-1) antagonist
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
1.Giblin PA, Lemieux RM. (2006) LFA-1 as a key regulator of immune function: approaches toward the development of LFA-1-based therapeutics.. Curr Pharm Des, 12 (22):(2771-95). [PMID:16918410]
2.Lam H, Bleiden L, de Paiva CS, Farley W, Stern ME, Pflugfelder SC. (2009) Tear cytokine profiles in dysfunctional tear syndrome.. Am J Ophthalmol, 147 (2):(198-205. e1). [PMID:18992869]
3.Murphy CJ, Bentley E, Miller PE, McIntyre K, Leatherberry G, Dubielzig R, Giuliano E, Moore CP, Phillips TE, Smith PB et al.. (2011) The pharmacologic assessment of a novel lymphocyte function-associated antigen-1 antagonist (SAR 1118) for the treatment of keratoconjunctivitis sicca in dogs.. Invest Ophthalmol Vis Sci, 52 (6):(3174-80). [PMID:21330663]
4.Kapp TG, Rechenmacher F, Sobahi TR, Kessler H. (2013) Integrin modulators: a patent review.. Expert Opin Ther Pat, 23 (10):(1273-95). [PMID:24050747]
5.Sheppard JD, Torkildsen GL, Lonsdale JD, D'Ambrosio Jr FA, McLaurin EB, Eiferman RA, Kennedy KS, Semba CP, OPUS-1 Study Group. (2014) Lifitegrast ophthalmic solution 5.0% for treatment of dry eye disease: results of the OPUS-1 phase 3 study.. Ophthalmology, 121 (2):(475-83). [PMID:24289915]
6.Zhong M, Gadek TR, Bui M, Shen W, Burnier J, Barr KJ, Hanan EJ, Oslob JD, Yu CH, Zhu J et al.. (2012) Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.. ACS Med Chem Lett, 3 (3):(203-6). [PMID:24900456]
7.A-González N, Castrillo A. (2011) Liver X receptors as regulators of macrophage inflammatory and metabolic pathways.. Biochim Biophys Acta, 1812 (8):(982-94). [PMID:21193033]
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I2212040