Lifitegrast
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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 la, inflammatio) is part of the complex biological response of body tissues to harmful stimuli, such as pathogens, damaged cells, or irritants, and is a protective response involving immune cells, blood vessels, and molec ...
by inhibiting inflammatory cell binding. It is often used in conjunction with
ciclosporin Ciclosporin, also spelled cyclosporine and cyclosporin, is a calcineurin inhibitor, used as an immunosuppressant medication. It is a natural product. It is taken orally or intravenously for rheumatoid arthritis, psoriasis, Crohn's disease ...
(Ikervis, Restasis, 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 participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, diet ...
s were eye irritation, discomfort, blurred vision, and dysgeusia (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 facilitate 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 ...
, lymphocyte function-associated antigen 1 (LFA-1), from binding to intercellular adhesion molecule 1 (ICAM-1). This mechanism down-regulates inflammation mediated by
T lymphocyte A T cell is a type of lymphocyte. T cells are one of the important white blood cells 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 re ...
s.


History

Lifitegrast was initially designed 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 such as Australia and New Zealand. It is generally synonymous with county. It was first used in Wessex from the begin ...
in 2013, which submitted a new drug application 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, with partial American and British roots. It is the largest pharmaceutical company in Asia and one of the top 20 largest pharmaceutical companies in the world by revenue (top 10 followin ...
in late 2018. In May 2019
Novartis Novartis AG is a Swiss-American multinational pharmaceutical corporation based in Basel, Switzerland and Cambridge, Massachusetts, United States (global research).name="novartis.com">https://www.novartis.com/research-development/research-lo ...
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.


See also

* Restasis (ciclosporin eye drops for keratoconjunctivitis sicca)


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 = 2423–31 , date = December 2015 , pmid = 26365210 , doi = 10.1016/j.ophtha.2015.08.001 , doi-access = free Ophthalmology drugs Amino acids Benzosulfones Takeda Pharmaceutical Company brands Novartis brands Benzamides