XIIDRA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XIIDRA (XIIDRA).
Lifitegrast is a lymphocyte function-associated antigen-1 (LFA-1) antagonist that binds to the I domain of LFA-1, blocking its interaction with intercellular adhesion molecule-1 (ICAM-1). This inhibits T-cell adhesion and migration, reducing inflammation in dry eye disease.
| Metabolism | Lifitegrast is not metabolized; it is eliminated primarily via renal excretion of unchanged drug. |
| Excretion | Primarily hepatic metabolism with biliary excretion; renal excretion accounts for <1% of unchanged drug. |
| Half-life | Terminal half-life is approximately 1.5 hours; supports twice-daily dosing for sustained ocular surface effects. |
| Protein binding | ~99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Not well characterized in systemic circulation; due to ocular administration, systemic Vd is not clinically relevant; estimated at 0.6 L/kg based on IV studies in animals. |
| Bioavailability | Ophthalmic: Low systemic bioavailability due to local administration (negligible systemic exposure). |
| Onset of Action | Ocular: Improvement in tear production observed as early as 2 weeks of twice-daily dosing. |
| Duration of Action | Duration of action supports twice-daily dosing; continued treatment required to maintain increased tear production. |
1 drop of 5% ophthalmic solution in each eye twice daily (approximately 12 hours apart).
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dose adjustment required for any degree of renal impairment. |
| Liver impairment | No dose adjustment required for any Child-Pugh class. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment required; same as adult dosing. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XIIDRA (XIIDRA).
| Breastfeeding | It is unknown if lifitegrast is excreted in human milk. After topical ocular administration, systemic exposure is minimal (plasma Cmax < 0.5 ng/mL), but no data on milk concentrations are available. The M/P ratio has not been determined. Caution should be exercised when administered to a nursing woman, weighing the low risk of infant exposure against the benefit of treatment. |
| Teratogenic Risk | Xiidra (lifitegrast) is classified as FDA Pregnancy Category B. Animal reproduction studies did not demonstrate fetal harm at doses up to 600 times the human ophthalmic dose. There are no adequate and well-controlled studies in pregnant women; however, systemic exposure is negligible due to low bioavailability (plasma concentrations below the limit of quantitation 0.5 ng/mL after topical ocular administration). Therefore, risk is considered minimal across all trimesters. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to lifitegrast or any excipient"]
| Precautions | ["Instillations may cause transient blurred vision or eye irritation","Contains benzalkonium chloride; caution with contact lens use","Not for injection","Discontinue if hypersensitivity occurs"] |
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| Fetal Monitoring | No specific maternal or fetal monitoring is required due to negligible systemic absorption. Standard prenatal care is sufficient. |
| Fertility Effects | In animal studies, lifitegrast did not impair fertility in male or female rats at oral doses up to 1000 mg/kg/day (approximately 4200 times the human ophthalmic dose). No human data on reproductive impact are available, but systemic exposure from topical use is minimal, suggesting no clinically significant effect on fertility. |