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CAS No.: 1025967-78-5

立他司特 Catalog No. CSN21154

Synonyms: SAR 1118;SHP-606;brand name: Xiidra

Lifitegrast is a novel small molecule integrin antagonist which can inhibit an integrin, lymphocyte function-associated antigen 1 (LFA-1), from binding to intercellular adhesion molecule 1 (ICAM-1).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Integrins are cell surface receptors involved in the integration between extracellular and intracellular signals in many biological processes, including cytoskeletal organization and cell adhesion, migration, proliferation, differentiation, and survival. During an immune response, integrins mediate cell adhesion to the extracellular matrix, and cell-cell interactions (e.g., T cell activation), which are central to the pathology of many inflammatory diseases, including dry eye disease (DED)^[2]. Lifitegrast is a novel small molecule integrin antagonist that blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), thus interrupting the T cell-mediated inflammatory cycle^[2]. Lifitegrast demonstrated concentration-dependent inhibition of Jurkat cell attachment with an IC₅₀ value of 2.98 nM, suggesting it to be a potent antagonist of LFA-1/ICAM-1–mediated T-cell binding. Lifitegrast also demonstrated potent concentration-dependent inhibition of superantigen induced inflammatory cytokine release from human PBMCs, particularly the Th1 and Th2 T-cell cytokines, IFN-γ and IL-4, respectively. In normal healthy beagles, lifitegrast was well tolerated at concentrations as high as 10% with no apparent adverse effects on the cornea surface or overall ocular health^[3].
动物研究
剂量
Rat: 10 mg/kg^[2] (i.v.)

给药途径
i.v.

动物药代数据
Animal Rats^[2]
Dose 10 mg/eye
Administration i.v.
T_1/2β 36.2 h (male)
40.7 h (female)
V_d 21.2 L/kg (male)
21.3 L/kg (female)
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
NCT03287635	Dry Eye Disease	Phase 4	Recruiting	July 31, 2019	United States, Tennessee ... more >> Toyos Clinic Recruiting Nashville, Tennessee, United States, 37203 Contact: Melissa Toyos, MD 615-327-4015 mtoyos@toyosclinic.com Contact: Dillon OBrien 6153274015 dobrien@toyosclinic.com Principal Investigator: Melissa Toyos, MD Collapse <<
NCT00882687	Allergic Conjunctivitis	Phase 2	Completed	-	United States, Massachusetts ... more >> Ora Andover, Massachusetts, United States, 01810 Collapse <<
NCT00882687	-	-	Completed	-	-

更多
参考文献

[1] XIIDRA
[2] Perez VL, Pflugfelder SC, Zhang S, Shojaei A, Haque R. Lifitegrast, a Novel Integrin Antagonist for Treatment of Dry Eye Disease. Ocul Surf. 2016 Apr;14(2):207-15. doi: 10.1016/j.jtos.2016.01.001. Epub 2016 Jan 22. PMID: 26807723.
[3] Murphy CJ, Bentley E, Miller PE, McIntyre K, Leatherberry G, Dubielzig R, Giuliano E, Moore CP, Phillips TE, Smith PB, Prescott E, Miller JM, Thomas P, Scagliotti R, Esson D, Gadek T, O'Neill CA. 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. 2011 May 16;52(6):3174-80. doi: 10.1167/iovs.09-5078. PMID: 21330663.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6247 mL
- 8.1237 mL
- 16.2475 mL
- 5 mM
- 0.3249 mL
- 1.6247 mL
- 3.2495 mL
- 10 mM
- 0.1625 mL
- 0.8124 mL
- 1.6247 mL

技术信息

CAS号

1025967-78-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H24Cl2N2O7S

运输

蓝冰

分子量

615.48

别名

SAR 1118;SHP-606;brand name: Xiidra;立他司特

溶解度

DMSO	110.0 mg/mL (178.7 mM)
Water	insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03287635	Dry Eye Disease	Phase 4	Recruiting	July 31, 2019	United States, Tennessee ... more >> Toyos Clinic Recruiting Nashville, Tennessee, United States, 37203 Contact: Melissa Toyos, MD 615-327-4015 mtoyos@toyosclinic.com Contact: Dillon OBrien 6153274015 dobrien@toyosclinic.com Principal Investigator: Melissa Toyos, MD Collapse <<
NCT00882687	Allergic Conjunctivitis	Phase 2	Completed	-	United States, Massachusetts ... more >> Ora Andover, Massachusetts, United States, 01810 Collapse <<
NCT00882687	-	-	Completed	-	-
NCT00936520	Diabetic Macular Edema (DME) ... more >> Pars Plana Vitrectomy Collapse <<	Phase 1	Terminated(Preliminary analysi... more >>s showed little or no bioactivity.) Collapse <<	-	United States, Maryland ... more >> Johns Hopkins University Baltimore, Maryland, United States, 21287 Collapse <<
NCT00926185	-	-	Completed	-	-
NCT00926185	Dry Eye	Phase 2	Completed	-	United States, Connecticut ... more >> The Eye Care Group Waterbury, Connecticut, United States, 06708 United States, Maine Central Maine Eye Care Lewiston, Maine, United States, 04243 United States, Massachusetts Ora, Inc. (two locations) Andover, Massachusetts, United States, 01840 United States, North Carolina Mundorf Eye Center Charlotte, North Carolina, United States, 28204 United States, Tennessee Total Eye Care, P.A. Memphis, Tennessee, United States, 38119 Collapse <<
NCT01636206	-	-	Completed	-	-
NCT01636206	Dry Eye	Phase 3	Completed	-	-
NCT01421498	Dry Eye Kerat... more >>oconjunctivitis Sicca Collapse <<	Phase 3	Completed	-	United States, Connecticut ... more >> OPUS-1 Investigational Site Waterbury, Connecticut, United States, 06708 United States, Kentucky OPUS-1 Investigational Site Louisville, Kentucky, United States, 40405 United States, Maine OPUS-1 Investigational Site Augusta, Maine, United States, 04330 OPUS-1 Investigational Site Lewiston, Maine, United States, 04243 United States, Massachusetts OPUS-1 Investigational Site Andover, Massachusetts, United States, 01840 OPUS-1 Investigational Site Lancaster, Massachusetts, United States, 01523 OPUS-1 Investigational Site Quincy, Massachusetts, United States, 02169 OPUS-1 Investigational Site Wakefield, Massachusetts, United States, 01880 OPUS-1 Investigational Site Winchester, Massachusetts, United States, 01890 United States, New Hampshire OPUS-1 Investigational Site Derry, New Hampshire, United States, 03038 OPUS-1 Investigational Site Manchester, New Hampshire, United States, 03101 United States, Tennessee OPUS-1 Investigational Site Memphis, Tennessee, United States, 38119 United States, Virginia OPUS-1 Investigational Site Norfolk, Virginia, United States, 23502 Collapse <<
NCT02284516	Dry Eye Disease	Phase 3	Completed	-	-
NCT03408015	Ocular Discomfort ... more >> Ocular Inflammation Dry Eye Contact Lens Complication Keratoconjunctivitis Sicca Collapse <<	Phase 4	Not yet recruiting	December 30, 2019	United States, Alabama ... more >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35294 Collapse <<
NCT03691636	Dry Eye	Not Applicable	Recruiting	May 1, 2019	United States, Missouri ... more >> Comprehensive Eye Care Recruiting Washington, Missouri, United States, 63039 Contact: Michael Korenfeld, MD 636-390-3999 michaelkorenfeld@hotmail.com Principal Investigator: Michael Korenfeld, MD Sub-Investigator: Rita Hindmon Collapse <<
NCT03431272	Contact Lens Dry Eye	Phase 4	Withdrawn(no longer interest /... more >> resources to start study) Collapse <<	December 31, 2019	United States, Alabama ... more >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35294 Collapse <<
NCT03686878	Contact Lens ... more >>Contact Lens Discomfort Contact Lens Dryness Collapse <<	Phase 4	Completed	-	United States, Texas ... more >> Eye & Vision Richardson, Texas, United States, 75082 Collapse <<
NCT01421498	-	-	Completed	-	-
NCT03451396	Dry Eye	Phase 4	Completed	-	United States, Missouri ... more >> Lifelong Vision Foundation Chesterfield, Missouri, United States, 63017 Collapse <<
NCT02284516	-	-	Completed	-	-
NCT01743729	Dry Eye	Phase 3	Completed	-	-
NCT01743729	-	-	Completed	-	-

立他司特 Catalog No. CSN21154

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