Keywords

• lifitegrast
• Lifitegrast, SAR 1118
• L-Phenylalanine,N-[[2-(6-benzofuranylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl]-3-(methylsulfonyl)-

Quick Details

• ProName: lifitegrast
• CasNo: 1025967-78-5
• Molecular Formula: C29H24Cl2N2O7S
• Appearance: Powder
• Application: Pharmaceutical Intermediates
• PackAge: Bottle.Box, Barrel
• Port: TIANJIN
• ProductionCapacity: 9000 Kilogram/Month
• Purity: 99
• LimitNum: 0

Superiority

Details

Description:

Increasing the ability of the eye to produce tears is a substitute for artificial tears Lifitegrast is a FDA approved drug for the treatment of keratoconjunctivitis sicca (dry eye syndrome). 

It is a tetrahydroisoquinoline derivative and lymphocyte function-associated antigen-1 ( LFA-1) antagonist that was discovered through the rational design process. The ophthalmic solution was approved in July, 2016 under the trade name Xiidra. It has shown to protect the corneal surface and alleviate the symptoms of dry eye syndrome with fast onset of action and well tolerated profile in both local and systemic setting.

Application:
Similar to other nitrites and organic nitrates, isosorbide dinitrate is converted to nitri c oxid e (NO), an active intermediate compound which activates the enzyme guanylate cyclase (atrial natriuretic peptide receptor A). This stimulates the synthesis of cyclic guanosine 3',5'-monophosphate (cGMP) which then activates a series of protein kinase-dependent phosphorylations in the smooth muscle cells, eventually resulting in the dephosphorylation of the myosin light chain of the smooth muscle fiber. The subsequent release of calcium ions results in the relaxation of the smooth muscle cells and vasodilation.