Lifitegrast

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Lifitegrast
Names
PronunciationXiidra /ˈzaɪdrə/[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]
Pregnancy
category
  • AU: B1
  • US: N (Not classified yet)
Routes of
use		Eye drops
External links
AHFS/Drugs.comMonograph
MedlinePlusa616039
Legal
Legal status
Chemical and physical data
FormulaC29H24Cl2N2O7S
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
  • Key:JFOZKMSJYSPYLN-QHCPKHFHSA-N

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

Dosage

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 are the following:[7]

  • Eye irritation
  • Discomfort
  • Blurred vision
  • Dysgeusia ( distortion of the sense of taste)

Pharmacology

Mechanism of action of lifitegrast [8]

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.[9][10]

History

Lifitegrast was initially designed and developed by SARcode Bioscience[11] which was acquired by Shire in 2013,[12] 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.[13][14]

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.[15]

In 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.[16]

Society and culture

Cost

The medication is sold in the U.S. at a cost of $587 (USD) for 60 solution(s) ophthalmic solution 5% [17]

  • Lifitegrast costs (US)

    Lifitegrast costs (US)

  • Lifitegrast prescriptions (US)

    Lifitegrast prescriptions (US)

References

  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". Drugs.com. 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". Drugs.com. 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. ↑ Drugs.com: Patient information for xiidra.
  8. ↑ Perez, Victor L.; Pflugfelder, Stephen C.; Zhang, Steven; Shojaei, Amir; Haque, Reza (1 April 2016). "Lifitegrast, a Novel Integrin Antagonist for Treatment of Dry Eye Disease". The Ocular Surface. 14 (2): 207–215. doi:10.1016/j.jtos.2016.01.001. ISSN 1542-0124.
  9. ↑ 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.
  10. ↑ 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.
  11. ↑ 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.
  12. ↑ "Shire To Acquire Sarcode Bioscience, Expands Presence In Ophthalmology". 25 March 2013. Archived from the original on 26 November 2017. Retrieved 16 September 2016.
  13. ↑ "FDA Approves Shire's Xiidra". 11 July 2016. Archived from the original on 17 August 2016. Retrieved 13 July 2016.
  14. ↑ Drugs.com: Xiidra (lifitegrast) FDA Approval History Archived 2016-09-14 at the Wayback Machine
  15. ↑ "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.
  16. ↑ "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.
  17. ↑ "Xiidra Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 17 January 2021. Retrieved 3 April 2021.

External links

Identifiers:
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