Lifitegrast, sold under the brand name Xiidra (), is a medication for the treatment of signs and symptoms of dry eye, a syndrome called keratoconjunctivitis sicca. Lifitegrast reduces

inflammation Inflammation (from ) is part of the biological response of body tissues to harmful stimuli, such as pathogens, damaged cells, or irritants. The five cardinal signs are heat, pain, redness, swelling, and loss of function (Latin ''calor'', '' ...

by inhibiting inflammatory cell binding. It is often used as an alternative to

ciclosporin Ciclosporin, also spelled cyclosporine and cyclosporin, is a calcineurin inhibitor, used as an immunosuppressant medication. It is taken Oral administration, orally or intravenously for rheumatoid arthritis, psoriasis, Crohn's disease, nephr ...

(Ikervis, Restasis, Vevye, Verkazia or Cequa) for dry eye treatment including

meibomian gland Meibomian glands (also called tarsal glands, palpebral glands, and tarsoconjunctival glands) are sebaceous glands along the rims of the eyelid inside the tarsal plate. They produce meibum, an oily substance that prevents evaporation of the eye, ...

dysfunction and inflammatory dry eye.

Adverse effects

Common side effects in

clinical trial Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...

s were eye irritation, discomfort, blurred vision, and

dysgeusia Dysgeusia, also known as parageusia, is a distortion of the sense of taste. Dysgeusia is also often associated with ageusia, which is the complete lack of taste, and hypogeusia, which is a decrease in taste sensitivity. An alteration in taste or ...

(a distortion of the sense of taste).

Pharmacology

Lifitegrast is supplied as an

eye drop Eye drops or eyedrops are liquid drops applied directly to the surface of the eye usually in small amounts such as a single drop or a few drops. Eye drops usually contain saline to match the salinity of the eye. Drops containing only saline ...

Mechanism of action

Lifitegrast inhibits an

integrin Integrins are transmembrane receptors that help cell–cell and cell–extracellular matrix (ECM) adhesion. Upon ligand binding, integrins activate signal transduction pathways that mediate cellular signals such as regulation of the cell cycle, o ...

lymphocyte function-associated antigen 1 Lymphocyte function-associated antigen 1 (LFA-1) is an integrin found on lymphocytes and other leukocytes. LFA-1 plays a key role in emigration, which is the process by which leukocytes leave the bloodstream to enter the tissues. LFA-1 also mediates ...

(LFA-1), from binding to intercellular adhesion molecule 1 (ICAM-1). This mechanism down-regulates inflammation mediated by

T lymphocyte T cells (also known as T lymphocytes) are an important part of the immune system and play a central role in the adaptive immune response. T cells can be distinguished from other lymphocytes by the presence of a T-cell receptor (TCR) on their cell ...

History

Lifitegrast was initially designed by Sunesis and developed by SARcode Bioscience which was acquired by

Shire Shire () is a traditional term for an administrative division of land in Great Britain and some other English-speaking countries. It is generally synonymous with county (such as Cheshire and Worcestershire). British counties are among the oldes ...

in 2013, which submitted a

new drug application The Food and Drug Administration's (FDA) New Drug Application (NDA) is the vehicle in the United States through which drug sponsors formally propose that the FDA approve a new pharmaceutical for sale and marketing. Some 30% or less of initial ...

to the

US Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food ...

(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. 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 The is a Japanese multinational pharmaceutical company. It is the third largest pharmaceutical company in Asia, behind Sinopharm and Shanghai Pharmaceuticals, and one of the top 20 largest pharmaceutical companies in the world by revenue (t ...

in late 2018. In May 2019

Novartis Novartis AG is a Swiss multinational corporation, multinational pharmaceutical company, pharmaceutical corporation based in Basel, Switzerland. Novartis is one of the largest pharmaceutical companies in the world and was the eighth largest by re ...

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. In 2023, Novartis sold the assets to Bausch + Lomb for $1.75 billion and eligible for an additional $750 million in payments linked to future sales for Xiidra as well as two pipeline assets.

References

{{reflist, refs= {{cite journal , vauthors = Tauber J, Karpecki P, Latkany R, Luchs J, Martel J, Sall K, Raychaudhuri A, Smith V, Semba CP , display-authors = 6 , title = Lifitegrast Ophthalmic Solution 5.0% versus Placebo for Treatment of Dry Eye Disease: Results of the Randomized Phase III OPUS-2 Study , journal = Ophthalmology , volume = 122 , issue = 12 , pages = 2423–2431 , date = December 2015 , pmid = 26365210 , doi = 10.1016/j.ophtha.2015.08.001 , doi-access = free Ophthalmology drugs Alpha-Amino acids Benzosulfones Drugs developed by Takeda Pharmaceutical Company Drugs developed by Novartis Benzamides