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Lifitegrast skeletal.svg
PronunciationXiidra /ˈzdrə/[1]
Trade namesXiidra
Other namesSAR-1118
  • N-{[2-(1-Benzofuran-6-ylcarbonyl)-5,7-dichloro-1,2,3,4-tetrahydro-6-isoquinolinyl]carbonyl}-3-(methylsulfonyl)-L-phenylalanine
Clinical data
Main usesDry eyes[2]
Side effectsBlurry vision, red eyes, headache, change in taste, itchiness[2]
  • AU: B1
  • US: N (Not classified yet)
Routes of
Eye drops
External links
Legal status
Chemical and physical data
Molar mass615.48 g·mol−1
3D model (JSmol)
  • CS(=O)(=O)c1cccc(c1)C[C@@H](C(=O)O)NC(=O)c2c(cc3c(c2Cl)CCN(C3)C(=O)c4ccc5ccoc5c4)Cl
  • InChI=1S/C29H24Cl2N2O7S/c1-41(38,39)20-4-2-3-16(11-20)12-23(29(36)37)32-27(34)25-22(30)13-19-15-33(9-7-21(19)26(25)31)28(35)18-6-5-17-8-10-40-24(17)14-18/h2-6,8,10-11,13-14,23H,7,9,12,15H2,1H3,(H,32,34)(H,36,37)/t23-/m0/s1

Lifitegrast, sold under the brand name Xiidra, is a medication used to treat dry eyes.[2] It is unclear if its benefits are greater than its harms.[3][4] It is used as eye drops.[2]

Common side effects include blurry vision, red eyes, headache, change in taste, and itchiness.[2] Safety in pregnancy is not clear.[5] It reduces inflammation by inhibiting T cells.[3]

Lifitegrast was approved for medical use in the United States in 2016.[2] It is not approved in either the United Kingdom or Europe.[3][4] In the United States it costs about 580 USD per month as of 2021.[6]

Medical uses


It is used as once drop twice per day of 5% solution.[2] Lifitegrast is supplied as an eye drop.

Side effects

Common side effects in clinical trials were eye irritation, discomfort, blurred vision, and dysgeusia (a distortion of the sense of taste).[7]


Mechanism of action

Lifitegrast inhibits an integrin, lymphocyte function-associated antigen 1 (LFA-1), from binding to intercellular adhesion molecule 1 (ICAM-1). This mechanism down-regulates inflammation mediated by T lymphocytes.[8][9]


Lifitegrast was initially designed and developed by SARcode Bioscience[10] which was acquired by Shire in 2013,[11] which submitted a new drug application to the US Food and Drug Administration (FDA) in March 2015. The FDA granted Shire a priority review a month later, and requested additional clinical data, which were supplied in January 2016; approval was granted on 11 July 2016.[12][13] Lifitegrast was approved by Health Canada in January 2018, and available in Canadian pharmacies as of March 2018.

Shire was acquired by Takeda Pharmaceutical Company in late 2018.[14] In May 2019 Novartis reached an agreement to purchase the assets associated with Lifitegrast. Novartis will pay Takeda an upfront payment of $3.4 billion, while the latter drugmaker is eligible for milestone payments of as much as $1.9 billion. Novartis noted that the drug amassed approximately $400 million in revenue in 2018.[15]

Society and culture


The medication is sold in the U.S. at a cost of $587 (USD) for 60 solution(s) ophthalmic solution 5% [16]


  1. "Patient information: Xiidra® (ZYE-druh) (lifitegrast ophthalmic solution) 5% for topical ophthalmic use" (PDF). Novartis. June 2020. Archived (PDF) from the original on 2021-02-13. Retrieved 2021-02-05.
  2. 2.0 2.1 2.2 2.3 2.4 2.5 2.6 "Lifitegrast Monograph for Professionals". Archived from the original on 5 March 2021. Retrieved 22 November 2021.
  3. 3.0 3.1 3.2 "Lifitegrast". SPS - Specialist Pharmacy Service. 8 February 2016. Archived from the original on 11 December 2021. Retrieved 23 November 2021.
  4. 4.0 4.1 "Xiidra: Withdrawal of the marketing authorisation application". Archived from the original on 14 November 2021. Retrieved 23 November 2021.
  5. "Lifitegrast ophthalmic (Xiidra) Use During Pregnancy". Archived from the original on 28 November 2020. Retrieved 23 November 2021.
  6. "Lifitegrast Prices, Coupons & Savings Tips - GoodRx". GoodRx. Archived from the original on 28 October 2016. Retrieved 23 November 2021.
  7. Patient information for xiidra.
  8. Tauber J, Karpecki P, Latkany R, Luchs J, Martel J, Sall K, et al. (December 2015). "Lifitegrast Ophthalmic Solution 5.0% versus Placebo for Treatment of Dry Eye Disease: Results of the Randomized Phase III OPUS-2 Study". Ophthalmology. 122 (12): 2423–31. doi:10.1016/j.ophtha.2015.08.001. PMID 26365210.
  9. Murphy CJ, Bentley E, Miller PE, McIntyre K, Leatherberry G, Dubielzig R, et al. (May 2011). "The pharmacologic assessment of a novel lymphocyte function-associated antigen-1 antagonist (SAR 1118) for the treatment of keratoconjunctivitis sicca in dogs". Investigative Ophthalmology & Visual Science. 52 (6): 3174–80. doi:10.1167/iovs.09-5078. PMID 21330663.
  10. Semba CP, Gadek TR (2016). "Development of lifitegrast: a novel T-cell inhibitor for the treatment of dry eye disease". Clinical Ophthalmology. 10: 1083–94. doi:10.2147/OPTH.S110557. PMC 4910612. PMID 27354762.
  11. "Shire To Acquire Sarcode Bioscience, Expands Presence In Ophthalmology". 25 March 2013. Archived from the original on 26 November 2017. Retrieved 16 September 2016.
  12. "FDA Approves Shire's Xiidra". 11 July 2016. Archived from the original on 17 August 2016. Retrieved 13 July 2016.
  13. Xiidra (lifitegrast) FDA Approval History Archived 2016-09-14 at the Wayback Machine
  14. "Takeda Completes Acquisition of Shire, Becoming a Global, Values-based, R&D-Driven Biopharmaceutical Leader". Takeda. January 8, 2019. Archived from the original on June 24, 2021. Retrieved May 13, 2019.
  15. "Novartis to acquire Xiidra, expanding front-of-eye portfolio and strengthening leadership in eye care". Novartis (Press release). May 9, 2019. Archived from the original on May 13, 2019. Retrieved May 13, 2019.
  16. "Xiidra Prices, Coupons & Patient Assistance Programs". Archived from the original on 17 January 2021. Retrieved 3 April 2021.

External links