Lifitegrast Eye Drops in Healthy Subjects：Phase I Study

Qilu Pharmaceutical Co., Ltd.24 enrolled

Overview

This is a single-center, randomized, double-blind, single-dose, two-period crossover Phase I clinical trial designed to: * Compare the pharmacokinetic (PK) profiles of Lifitegrast Ophthalmic Solution and Xiidra® in plasma and tears following single-dose administration in healthy subjects. * Evaluate the safety and tolerability of Lifitegrast Ophthalmic Solution in healthy subjects. A total of 24 healthy subjects will be randomized into two treatment sequences (Group A: T/R; Group B: R/T). The study duration per subject will be approximately 36 days, including: * Screening Period (Day -21 to Day -1) * Treatment Periods (Day 1, followed by a 7-day washout period, then Day 8 or early termination) * Safety Follow-up (Day 15, 7 days after the last dose). On Day 1 of Cycle 1, one study eye will be selected and designated for all subsequent tear PK sampling. Treatment assignments: * Group A: Lifitegrast (T) on Day 1, then Xiidra® (R) on Day 8. * Group B: Xiidra® (R) on Day 1, then Lifitegrast (T) on Day 8. Each subject will receive one drop of the assigned medication (either Lifitegrast or Xiidra®) in each eye from the same single-dose container. Blood and tear samples will be collected per protocol for PK analysis, including parameters such as Cmax, AUC0-∞, AUC0-t, Tmax, T1/2, λz, and AUC\_%Extrap. The PK profiles between the two treatments will be compared to evaluate bioequivalence and assess the safety of Lifitegrast Ophthalmic Solution.

Study Type

INTERVENTIONAL

Allocation

RANDOMIZED

Purpose

TREATMENT

Masking

QUADRUPLE

Enrollment

Conditions

Dry Eye Syndromes

Eligibility

Sex: ALLMin age: 18 YearsMax age: 50 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: * Subjects must meet all the following criteria to be eligible: * Healthy, aged 18-50 (inclusive), all genders. * Signed informed consent pre-screening; comprehension of study and ability to complete it per protocol. * BMI 19-27 kg/m² (inclusive); ≥45 kg for females, ≥50 kg for males. * Bilateral best-corrected visual acuity ≥4.7 (5m, 5-point logMAR). * No reported eye discomfort/abnormalities 1 month before randomization. * No history of dry eye disease, as assessed by the investigator. * No history of ocular inflammation (e.g., allergic conjunctivitis, uveitis) per investigator judgment. * Use effective contraception during study and 30 days post-last dose: Females: non-pregnant, non-lactating; premenopausal use approved methods, no egg donation. Males with fertile partners: vasectomy (≥30 days, no viable sperm) or approved contraception, no sperm donation. * Non-smoker, remain smoke-free during study. * No excessive alcohol (\>14 units/week) or illicit drug use history; abstain from both during study. Exclusion Criteria: * Subjects will be excluded if they meet any of the following: * History or current diseases/conditions (e.g., circulatory, endocrine disorders) that pose risks or interfere with the study, as judged by the investigator. * Blood donation or loss \>300 mL within 56 days before randomization; no blood donation during the study. * Allergy to study medications (e.g., lifitegrast, excipients). * Prior participation in non - placebo lifitegrast clinical trials. * Clinically significant abnormal test results: Vital signs: ear temp \>37.7℃ or \<35.4℃; pulse \>100 or \<60 bpm; systolic BP ≥150 or \<90 mmHg; diastolic BP ≥90 or \<50 mmHg. ECG: QTcF ≥450 ms (male), ≥460 ms (female). Lab tests: abnormal blood/urine, coagulation, infectious markers, drug/alcohol screenings. Abnormal abdominal ultrasound or eye exams. * Intraocular/laser eye surgery within 12 months, other eye surgeries within 3 months before screening, or planned eye surgery during the study. * Use of ophthalmic drugs (incl. artificial tears), anticholinergics, oral/nasal steroids within 1 month before screening or during the study. * Tobacco/nicotine use within 6 months before randomization. * Contact lens use within 1 month before randomization or during the study. * Prescription/OTC/herbal medications within 2 weeks or 5 half - lives (longer) before randomization or during the study. * Pregnancy, lactation, or positive pregnancy test at screening. * Participation in drug/device trials within 30 days or 5 half - lives (longer) before screening, or planned participation during the study affecting results. * Conditions increasing risks, affecting compliance, or deemed unsuitable by the investigator (e.g., needle phobia).