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Shire Lifitegrast For Dry Eye & Side Effects

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Reviewed by Nymark M, PhD on April 28, 2016

Lifitegrast is a product made by Shire that has been designed to address the symptoms of Dry Eye Syndrome (DES). This comes after the patent for Restasis, the only currently U.S. Food and Drug Administration (FDA)-approved treatment for DES, is set to expire. Lifitegrast has not yet been approved by the FDA but a New Drug Application (NDA) has been put forward, with supporting evidence.

What Is Shire Lifitegrast?

Some 25 million people in this country are estimated to suffer from DES, rising to around 60 million people globally. It leads to chronic pain, soreness, and irritation.

Lifitegrast is based on a molecule that has anti-inflammatory properties. It reduces cytokine release and T-cell activation. Restasis works in a similar way. Both address the process of inflammation that is found in people who suffer from DES.

Once eyes start to get dry, people experience irritation and redness because the ocular surface becomes inflamed. This inflammation, in turn, stops the proper production and function of the tear film, which means the eyes get even drier, resulting in further inflammation. This is why DES is classed as a chronic condition, as people who have it find themselves trapped in a cycle of irritation and inflammation.

Although not yet released to the public, Shire claims that Lifitegrast will work better than Restasis. While Restasis has been proven to be effective, it is very slow acting. This means patients often have to use it for several months before noticing any positive effect. This is because the life cycle of a T-cell is three months, and Restasis stops new T-cells from forming, rather than addressing those that are already there. According to Shire, however, Lifitegrast will work much more quickly. This means that it is much more likely that people will also stick to their treatment, as they could see results in as little as two weeks. Ophthalmologists are particularly excited about this, considering whether patients could perhaps use both for even quicker and better effects.

Lifitegrast Studies

A number of studies have been conducted to examine the effectiveness of Lifitegrast, all with similar results. The OPUS-3 trial has recently been completed, and an NDA has been submitted to and received by the FDA. The table below highlights the results of the various studies that have been conducted into Lifitegrast to date.

Trial Type of Study Details Results
OPUS-1
  • Placebo-controlled
  • 84 day study
  • Twice daily administration of ophthalmic solution 5.0%
  • Reduction in corneal fluorescent staining
  • Improvements in nasal and total lissamine scores
  • Improvement in eye dryness and ocular discomfort
OPUS-2
  • Randomized
  • Multicenter
  • Placebo-controlled
  • Double-masked
  • Parallel-arm
  • Twice-daily administration of Lifitegrast (5.0% ophthalmic solution) to placebo group and participant group
  • 718 participants in 31 locations
  • 84 days of administration
  • Five patient visits over 98 day period.
  • Dry eye improvement noticed compared to placebo group
  • No inferior corneal staining improvement
  • Improvement in symptoms
  • Lack of improvement in signs
  • No serious side effects
SONATA
  • Randomized
  • Prospective
  • Placebo-controlled
  • Double-masked
  • 360 study days
  • Patients felt better, but not physical improvement was noted.
OPUS-3
  • Placebo-controlled
  • 84 study days
  • Twice daily administration
  • Patients were known to suffer from dry eyes
  • Patients had all used artificial tears in the 30 days before starting the trial
  • Significant improvement in levels of discomfort.
  • Improvements noted after just two weeks of application.
  • Further improvements noted at day 42.

Reported Lifitegrast Side Effects

During the studies, no serious side effects were reported by participants. Some minor side effects were noted, however, as listed in the table below.

Trial Side Effects
OPUS-1
  • Transient intermittent instillation site symptoms (irritation, discomfort) primarily on the initial Lifitegrast dose at day 0
OPUS-2
  • Dysgeusia (bad after taste) (in 16.2% of people)
  • Instillation side reaction (in 7% of people)
  • Reduced visual acuity (in 5% of people)
SONATA
  • Instillation side irritation (in 15% of people)
  • Instillation site reaction (in 13.2% of people)
  • Reduced visual acuity (in 11.4% of people)
  • Dry eye (in 1.8% of people)
  • Dysgeusia (in 16.4% of people)
OPUS-3
  • No reported side effects listed.

Benefits of Lifitegrast Over Restasis

Restasis has a number of side effects, similar to those associated with Lifitegrast in the clinical trials. However, ophthalmologists feel that Lifitegrast has the potential to be much better than Restasis because:

  • A different inflammatory pathway is treated.
  • There is less potential for medication- and mechanistic-based toxicity.
  • Restasis is slow-active and often irritates the eyes. Lifitegrast irritates less and is much faster acting.
  • It has a pH of 7.0, which is the same as natural tear films.
  • It is aqueous soluble, which means it can be delivered through saline solutions.
  • It remains stable at room temperature for much longer than Restasis. This increases its shelf life and avoids wasting medication.

Next Steps

Shire has resubmitted their NDA to the FDA after completion of the OPUS-3 trial. They believe this trial has proven beyond doubt that the product is safe to use, as well as efficient, that benefits can be noted after just two weeks of application, and that these benefits continue to be present after longer use. Shire hopes to have approval this year, enabling them to launch it in the first quarter of 2017.

Shire has also indicated that the findings of the three OPUS studies and the Sonata study will be used to submit drug approval applications for Lifitegrast in markets outside of this country. The company feels that there is a significant need for a product of its kind both within the world of ophthalmology, and within the world of patients who suffer from DES. Shire is building up its presence in the ophthalmic world, and professionals are watching developments very closely.

Resources and References:

Lifitegrast Ophthalmic Solution 5.0% for Treatment of Dry Eye Disease: Results of the OPUS-1 Phase 3 Study – Phase 3 study of Lifitegrast dry eye treatment. (NCBI)

In the Dry-Eye Pipeline: Slow Progress – Treatments for dry eye that are currently in development. (Review of Ophthalmology)

Topical Integrin Antagonist Lifitegrast Safely Treats Dry Eye Disease – Report on Lifitegrast treatment for dry eye. (Ophthalmology Times)