Lifitegrast, also known as SAR-1118, is an LFA-1 antagonist intended for the treatment of vascular complications of the eye. Lifitegrast 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.
Burnier, John; Gadek, Thomas; Naud, Frederic. Crystalline pharmaceutical LFA-1 inhibitors and methods of preparation and use thereof. WO 2009139817. (Assignee Sarcode Corporation, USA)
Burnier, John. Preparation of crystalline isoquinoline derivative as LFA-1 inhibitor. US 20110092707. (Assignee Sarcode Corporation, USA)
Zeller, James Robert; Venkatraman, Sripathy; Brot, Elisabeth C. A.; Iyer, Subashree; Hall, Michael. Method for preparation of N-benzofuranylcarbonyl-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinylcarbonyl-3-(methylsulfonyl)-L-phenylalanine as LFA-1 inhibitor and polymorph thereof. WO 2014018748. (Assignee Sarcode Bioscience Inc., USA)
Anon. S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4- tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl) propanoic acid. Volume 17. Issue 9A. Pages 1-2.( Journal; Patent)
Wu, Ming-Chih; Hsiao, Tsung-Yu. Process for preparing Lifitegrast and intermediates thereof. WO 2019004936. (Assignee Scinopharm Taiwan, Ltd., Taiwan; Scinopharm Singapore Pte, Ltd.)
Berzosa Rodriguez, Xavier; Marquillas Olondriz, Francisco. Process for preparing and purifying the LFA-1 antagonist Lifitegrast. WO 2019020580. (Assignee Interquim, S.A., Spain)
Rajan, Srinivasan Thirumalai; Eswaraiah, Sajja; Reddy, Ghojala Venkat; Reddy, Sagyam Rajeshwar; Srinivasulu, Rangineni; Rajashekar, Kommera. Processes for the preparation of (s)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl) propanoic acid and polymorphs thereof. WO 2019043724. (Assignee MSN Laboratories Private Limited, R&D Center, India)
