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  • CLASSES

    Lymphocyte Function-Associated Antigen-1 (LFA-1) Antagonists

    DEA CLASS

    Rx

    DESCRIPTION

    Topical ophthalmic agent
    Lymphocycte function-association antigen-1 antagonist
    Used for dry eye disease

    COMMON BRAND NAMES

    XIIDRA

    HOW SUPPLIED

    XIIDRA Ophthalmic Sol: 5%

    DOSAGE & INDICATIONS

    For the treatment of xerophthalmia associated with dry eye disease (keratoconjunctivitis sicca).
    Ophthalmic dosage
    Adults and Adolescents 17 years and older

    Instill 1 drop into each eye twice daily (approximately 12 hours apart).

    MAXIMUM DOSAGE

    Adults

    2 drops/day in each eye.

    Geriatric

    2 drops/day in each eye.

    Adolescents

    17 years: 2 drops/day in each eye.
    < 17 years: Safety and efficacy have not been established.

    Children

    Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

    Renal Impairment

    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    ADMINISTRATION

    Ophthalmic Administration

    Each dose is packaged in a single-use container. Prior to use, containers should be stored in the original foil pouch.
    Wash hands before administering the drug.
    Remove contact lenses. Contact lenses my be reinserted 15 minutes after drug administration.
    Remove 1 single-use container from the foil pouch. Hold the container upright, and verify solution is at the bottom of the container. Open the container by twisting off the tab. Use caution to avoid touching the tip of the container to any surface.
    Tilt head backwards or lie down.
    Place the container close to the eye, without the eye touching the container tip. Gently squeeze to instill 1 drop onto lower eyelid and eye. Repeat process for the second eye. There is enough solution in each single-use container for both eyes.
    Discard the single-use container immediately after use.

    STORAGE

    XIIDRA :
    - Discard unused portion. Do not store for later use.
    - Store at 77 degrees F
    - Store unused product in foil pouch

    CONTRAINDICATIONS / PRECAUTIONS

    Contact lenses

    Lifitegrast should not be administered while wearing contact lenses. Contact lenses should be removed prior to administration of the drug. Lenses may be reinserted 15 minutes following administration of the drug.

    Pregnancy

    Data are not available regarding use of lifitegrast during human pregnancy. In animal studies, rats experienced an increase in mean preimplantation loss and an increased incidence of skeletal abnormalities when administered daily intravenous doses that produced exposures equivalent to 5,400-fold the human plasma exposure at the recommended human ophthalmic dose (RHOD). In addition, rabbits experienced an increased incidence of omphalocele when administered intravenous doses producing exposures 400-fold the human exposure at RHOD. However, since human exposure following ophthalmic administration is low, the applicability of animal findings to human fetal risk is unknown. Before administering lifitegrast during pregnancy, consider the benefits of treatment verse the potential risk to the infant.

    Breast-feeding

    No data are available regarding excretion of lifitegrast into human breast milk. However, because systemic drug concentrations are low following ophthalmic administration, significant amounts of the drug are not be expected to be excreted in breast milk. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    ADVERSE REACTIONS

    Severe

    visual impairment / Early / 5.0-25.0

    Moderate

    conjunctival hyperemia / Early / 1.0-5.0
    blurred vision / Early / 1.0-5.0

    Mild

    dysgeusia / Early / 5.0-25.0
    headache / Early / 1.0-5.0
    ocular irritation / Rapid / 1.0-5.0
    sinusitis / Delayed / 1.0-5.0
    ocular discharge / Delayed / 1.0-5.0
    lacrimation / Early / 1.0-5.0
    ocular pruritus / Rapid / 1.0-5.0

    DRUG INTERACTIONS

    There are no drug interactions associated with Lifitegrast products.

    PREGNANCY AND LACTATION

    Pregnancy

    Data are not available regarding use of lifitegrast during human pregnancy. In animal studies, rats experienced an increase in mean preimplantation loss and an increased incidence of skeletal abnormalities when administered daily intravenous doses that produced exposures equivalent to 5,400-fold the human plasma exposure at the recommended human ophthalmic dose (RHOD). In addition, rabbits experienced an increased incidence of omphalocele when administered intravenous doses producing exposures 400-fold the human exposure at RHOD. However, since human exposure following ophthalmic administration is low, the applicability of animal findings to human fetal risk is unknown. Before administering lifitegrast during pregnancy, consider the benefits of treatment verse the potential risk to the infant.

    No data are available regarding excretion of lifitegrast into human breast milk. However, because systemic drug concentrations are low following ophthalmic administration, significant amounts of the drug are not be expected to be excreted in breast milk. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    MECHANISM OF ACTION

    The exact mechanism of action of lifitegrast in the treatment of dry eye disease is unknown. It is theorized that the mechanism involves blocking the interaction between lymphocyte function-associated antigen-1 (LFA-1) and its ligand intracellular adhesion molecule-1 (ICAM-1). ICAM-1, which may be overexpressed in corneal and conjunctival tissues of patients with dry eye disease, binds to the LFA-1, a surface protein found on lymphocytes. This interaction contributes to the formation of an immunological synapse that results in T-cell activation and migration to target tissues. In vitro data suggests that by blocking this interaction, lifitegrast inhibits T-cell adhesion to ICAM-1 and may inhibit secretion of inflammatory cytokines in human peripheral blood mononuclear cells.

    PHARMACOKINETICS

    Lifitegrast is administered topically to the eyes. Pharmacokinetic data are limited.
     
    Affected cytochrome P450 isoenzymes: None

    Other Route(s)

    Ophthalmic Route
    During one pharmacokinetic study, lifitegrast tough concentrations were measured in 47 patients with dry eye disease who were administered 1 drop twice daily via the ophthalmic route for 180 and 360 days. Measurable concentrations (i.e., greater than 0.5 ng/mL) were obtained in 9 of the 47 patients (19%), and ranged from 0.55 ng/mL to 3.74 ng/mL.