Products
Lifitegrast was approved in the United States in 2016 and in many countries in December 2018 as single-dose eye drops (Xiidra, pronounced Saidra in English).
Structure and properties
Lifitegrast (C29H24Cl2N2O7S, Mr = 615.5 g/mol) is a tetrahydroisoquinoline derivative. It exists as a white powder that is soluble in water.
Effects
Lifitegrast (ATC S01XA25) has anti-inflammatory and selective immunosuppressive properties. The effects are due to competitive antagonism at lymphocyte function-associated antigen-1 (LFA-1), an integrin found on the surface of leukocytes (T cells). The binding blocks the interaction with the intercellular adhesion molecule-1 (ICAM-1). ICAM-1 is found on endothelial cells in blood vessels, among others, and is overexpressed in the disease. Lifitegrast administration inhibits T-cell adhesion to the endothelium, their extravasation from blood vessels into tissues, activation, proliferation, and thus the inflammatory response.
Indications
For the treatment of dry eye syndrome in adults in whom treatment with tear substitutes has been inadequate.
Dosage
According to the SmPC. Drops are placed in the eyes twice daily (morning and evening, every 12 hours). The effects are delayed after two weeks at the earliest. Contact lenses must be removed prior to application and may be reinserted 15 minutes after application. See also under Administering eye drops.
Contraindications
- Hypersensitivity
- Children and adolescents under 18 years
- Pregnancy and lactation (insufficient data).
For complete precautions, see the drug label and directions for use.
Interactions
Drug-drug interactions have not been reported to date.
Adverse effects
The most common possible adverse effects include eye irritation, eye pain, instillation site reactions, and taste disturbances.