How Do LFA-1 Antagonists Work?

Reviewed on 6/23/2021

What are LFA-1 antagonists and how do they work?

Lymphocyte function-associated antigen-1 (LFA-1) antagonists are ophthalmic medications that prevent eye inflammation caused by dry eyes. LFA-1 antagonists work by blocking LFA-1, a protein that activates the immune system’s T-cells, resulting in inflammation in the cornea and conjunctiva.

Cornea is the clear layer over the iris and pupil, and the conjunctiva is the protective membrane over the whites of the eyes and inner surface of eyelids. Tears of different compositions keep the eye surface moist and lubricated so the eyes are protected and eyelids can glide over the surface.

The eye surface can get dry when the eyes are not adequately lubricated with tears due to any reason such as aging, certain medical conditions, medications or eye surgery. Irritation from dry eyes stimulates the T-cells to initiate inflammation on the surface of the eye.

LFA-1, a protein molecule on T-cell membranes, interacts with a molecule known as intercellular adhesion molecule-1 (ICAM-1) on the cell surfaces of the cornea and conjunctiva, which results in the release of inflammatory proteins (cytokines). LFA-1 antagonists bind to LFA-1, block its interaction with ICAM-1, and prevent inflammation.

How are LFA-1 antagonists used?

LFA-1 antagonists are ophthalmic solutions administered topically in the eye to treat symptoms of inflammation from dry eye disease. Transient dryness in the eye from minor causes is usually mitigated with the use of artificial tears, but persistent dry eyes may require treatment with LFA-1 antagonists.

What are side effects of LFA-1 antagonists?

Side effects of LFA-1 antagonists may include the following:

Ocular side effects:

Systemic side effects:

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

What are names of some LFA-1 antagonist drugs?

Generic and brand name of the FDA-approved LFA-1 antagonist drugs is:

  • Ophthalmic lifitegrast (Xiidra)

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