Lifitegrast

Dry Eye Disease

Lifitegrast is specifically used to treat dry eye disease (keratoconjunctivitis sicca). This is a chronic condition that occurs when the eyes do not produce enough tears or when the tears evaporate too quickly, leading to a lack of lubrication and potential inflammation on the surface of the eye.

The medication is prescribed to help manage various symptoms associated with dry eye, including:

• A persistent gritty or sandy feeling in the eyes
• Stinging, burning, or general eye irritation
• Redness and discomfort
• Blurred vision related to dryness

Lifitegrast is intended for the ongoing management of these symptoms to improve eye comfort and protect the ocular surface. It is typically used when over-the-counter artificial tears do not provide sufficient relief for the underlying condition.

Mechanism of Action

Lifitegrast belongs to a class of drugs known as lymphocyte function-associated antigen-1 (LFA-1) antagonists. It works by targeting the underlying inflammation that often contributes to dry eye symptoms.

In dry eye disease, the surface of the eye can become inflamed due to the activity of certain white blood cells. Lifitegrast works by blocking specific protein interactions that drive this inflammatory process. The process involves the following steps:

• Binding to LFA-1: Lifitegrast binds to a protein called lymphocyte function-associated antigen-1 (LFA-1) found on the surface of white blood cells (leukocytes).
• Blocking ICAM-1 interaction: By binding to LFA-1, the medication prevents it from interacting with another protein called intercellular adhesion molecule-1 (ICAM-1). ICAM-1 is often found in high amounts on the surface of the eye in individuals with dry eye disease.
• Reducing inflammation: When these two proteins are prevented from connecting, the inflammatory response on the surface of the eye is decreased.

By reducing this inflammation, lifitegrast helps alleviate the irritation and discomfort associated with dry eye and may help improve the eye's ability to maintain a healthy tear film.

Common Side Effects

Many people using lifitegrast experience mild side effects. These often occur immediately after applying the eye drops and may include:

• Eye irritation, stinging, or burning
• Blurred vision
• An unusual, metallic, or salty taste in the mouth
• Redness or watering of the eyes
• Headache

Serious Side Effects

Seek medical attention right away if you notice signs of a serious reaction, such as:

• Symptoms of an allergic reaction, including hives, rash, or swelling of the face, lips, tongue, or throat
• Difficulty breathing or wheezing
• Severe eye pain or swelling
• Changes in vision that do not go away
• Eye discharge or crusting

Allergic Reactions

Serious hypersensitivity reactions have been reported with the use of lifitegrast. These reactions can occur shortly after administration or after long-term use. Symptoms of a serious reaction may include:

• Anaphylaxis (a severe, life-threatening allergic reaction)
• Angioedema (swelling under the skin, often around the eyes, lips, or tongue)
• Difficulty breathing or wheezing
• Skin rash, hives, or itching
• Swelling of the throat

If signs of a serious allergic reaction occur, the medication should be discontinued and medical attention sought immediately.

Eye Safety and Contamination

To prevent eye injury and avoid contaminating the medication, the tip of the single-use container should not touch the eye, eyelids, fingers, or any other surface. Because the medication is provided in single-use containers that do not contain preservatives, any remaining solution must be discarded immediately after a single application to both eyes.

Contact Lens Use

Contact lenses should be removed before administering lifitegrast ophthalmic solution. It is generally recommended to wait at least 15 minutes after using the drops before reinserting contact lenses.

Pregnancy and Breastfeeding

There is limited data regarding the use of lifitegrast in pregnant women or its presence in human breast milk. The potential risks and benefits should be discussed with a healthcare provider if pregnancy is planned or if breastfeeding.

Pregnancy

It is not known if lifitegrast will harm an unborn baby. There is a lack of adequate data from human studies to confirm its safety during pregnancy. Animal studies using high doses of the medication did not show evidence of harm to the developing fetus. Because the drug is applied topically to the eye, only a small amount enters the bloodstream, which may reduce potential exposure during pregnancy.

Breastfeeding

There is no information available on whether lifitegrast is present in human breast milk or how it might affect a breastfed infant. While the amount of medication absorbed into the body is low, individuals who are breastfeeding should consult with a healthcare professional to weigh the potential benefits against any unknown risks.

Available Forms

Lifitegrast is supplied as an ophthalmic solution, which is a liquid intended for use as eye drops. This medication is typically packaged in single-use containers. Each container holds enough liquid to treat both eyes one time.

Strengths

This medication is available in the following strength:

• Ophthalmic solution: 5%

The single-use containers are usually provided in foil pouches to protect the medication from light. Once a container is opened, it should be used immediately and then discarded, even if there is liquid remaining.

FDA Approval and Indications

Lifitegrast was approved by the U.S. Food and Drug Administration (FDA) in July 2016. It is the first medication in a class of drugs called lymphocyte function-associated antigen-1 (LFA-1) antagonists to receive approval for the treatment of both the signs and symptoms of dry eye disease.

Safety Communications and Monitoring

In 2020, the FDA identified a potential signal of a serious risk regarding reduced visual acuity associated with lifitegrast use, based on reports in the FDA Adverse Event Reporting System (FAERS). Following an evaluation of the available evidence, the FDA determined that no regulatory action or changes to the drug's labeling were required at that time.

There are currently no boxed warnings or Risk Evaluation and Mitigation Strategies (REMS) requirements for lifitegrast. It is available only by prescription and is intended for topical ophthalmic use.

Administration Instructions

Lifitegrast is an eye drop solution typically used twice a day, approximately 12 hours apart. It is supplied in individual, single-use containers that are stored inside a foil pouch. It is important to follow specific steps to ensure the medication is used safely and effectively.

• Wash your hands thoroughly before using the drops.
• Remove one single-use container from the foil pouch.
• Tap the container so the solution settles at the bottom.
• Twist off the tab to open the container.
• Tilt your head back and pull down the lower eyelid to create a small pocket.
• Place one drop into the pocket of the eye.
• Repeat the process for the other eye if instructed by your doctor.

Important Precautions

To prevent contamination and eye injury, do not let the tip of the container touch your eye, eyelashes, or any other surface. Each container is intended for a single dose in one or both eyes. You must discard the container and any remaining liquid immediately after use; do not save it for a later dose.

If you wear contact lenses, remove them before applying lifitegrast. You should wait at least 15 minutes after using the drops before reinserting your contact lenses. If you are using other eye medications, consult your healthcare provider about the proper timing for each product.