Lifitegrast

What is lifitegrast used for?

Lifitegrast is a prescription medicine that is used to treat dry eyes.

Description

The chemical name for lifitegrast is (S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid. The molecular formula of lifitegrast is C29H24Cl2N2O7S and its molecular weight is 615.5 g/mol. The structural formula of lifitegrast is:

*Chiral center

Lifitegrast is a white to off-white powder, which is soluble in water.

Xiidra (lifitegrast ophthalmic solution) 5% is a lymphocyte function-associated antigen-1 (LFA-1) antagonist supplied as a sterile, clear, colorless to slightly brownish-yellow colored, isotonic solution of lifitegrast with a pH of 7.0-8.0, and an osmolality range of 200-330 mOsmol/kg.

Xiidra contains Active: lifitegrast 50 mg/mL; Inactives: sodium chloride, sodium phosphate dibasic anhydrous, sodium thiosulfate pentahydrate, and water for injection. Sodium hydroxide and/or hydrochloric acid (to adjust pH).

 Mechanism of Action

Lifitegrast binds to the integrin LFA-1, a cell surface protein found on leukocytes and blocks the interaction of LFA-1 with its cognate ligand intercellular adhesion molecule-1 (ICAM-1). ICAM-1 may be overexpressed in corneal and conjunctival tissues in DED. LFA-1/ICAM-1 interaction can contribute to the formation of an immunological synapse resulting in T-cell activation and migration to target tissues. In vitro studies demonstrated that lifitegrast may inhibit T-cell adhesion to ICAM-1 in a human T-cell line and may inhibit secretion of inflammatory cytokines in human peripheral blood mononuclear cells. The exact mechanism of action of lifitegrast in DED is not known.

Before taking lifitegrast, tell your doctor:

• If you are allergic to lifitegrast; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.

This medicine may interact with other drugs or health problems.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take lifitegrast with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take lifitegrast?

• Tell all of your health care providers that you take lifitegrast. This includes your doctors, nurses, pharmacists, and dentists.
• Use care when driving or doing other tasks that call for clear eyesight.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using lifitegrast while you are pregnant.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

How is lifitegrast best taken?

Use lifitegrast as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• For the eye only.
• Take out contact lenses before using lifitegrast. Lenses may be put back in 15 minutes after lifitegrast is given. Do not put contacts back in if your eyes are irritated or infected.
• Do not touch the container tip to the eye, lid, or other skin.
• Wash your hands before and after use.
• Do not open until you are ready to use.
• Use right after opening.
• Tilt your head back and drop drug into the eye.
• After use, keep your eyes closed. Put pressure on the inside corner of the eye. Do this for 1 to 2 minutes. This keeps the drug in your eye.
• Throw away any part left over after the dose is given.

What do I do if I miss a dose?

• Use a missed dose as soon as you think about it.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not use 2 doses at the same time or extra doses.

What are the side effects of lifitegrast that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

What are some other side effects of lifitegrast?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Eye irritation.
• Change in taste.
• Blurred eyesight.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out lifitegrast?

• Store at room temperature.
• Store unused containers in foil pouch until use.
• Protect from light.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.