In vitro: Lifitegrast is a novel small molecule integrin antagonist that inhibits T cell-mediated inflammation by blocking the binding of two important cell surface proteins (lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1), thus lessening overall inflammatory responses. Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. In vivo: Lifitegrast, has potent anti-inflammatory activity on corneal inflammation induced by antibiotic-killed P. aeruginosa and S. aureus in the presence of a silicone hydrogel lens with the optimal application being a 1% solution applied either 2 or 3 times prior. Topical application of lifitegrast to the corneal surface of healthy adults is safe and well tolerated. SAR 1118 ophthalmic drops administered thrice daily deliver therapeutic levels of SAR 1118 in the retina and can alleviate the retinal complications associated with diabetes.
|Preparation method||Lifitegrast potently inhibits human T-cell binding to human ICAM-1, T-cell activation and cytokine release, and formation of the immunologic synapse.|
|Animal models||dogs diagnosed with keratoconjunctivitis sicca|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||29 mg/mL in DMSO|
Development of lifitegrast: a novel T-cell inhibitor for the treatment of dry eye disease.
Semba CP, et al. Clin Ophthalmol. 2016 Jun 10;10:1083-94. PMID: 27354762.
Lifitegrast Ophthalmic Solution 5.0% versus Placebo for Treatment of Dry Eye Disease: Results of the Randomized Phase III OPUS-2 Study.
Tauber J, et al. Ophthalmology. 2015 Dec;122(12):2423-31. PMID: 26365210.
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Firategrast (SB-683699) is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist.
|Tirofiban hydrochloride monohydrate
Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist
GLPG0187 inhibited the progression of bone metastasis. Maximum efficacy of inhibition of bone metastasis was achieved when GLPG0187 was combined with the standard-of-care metastatic breast cancer treatments.
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