Dry Eye Syndromes
Conditions
Brief summary
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.
Interventions
DRUGXiidra
Administered on Day 1 to subjects in Group B, and on Day 8 to subjects in Group A as part of a crossover study design.
DRUGLifitegrast
Administered on Day 1 to subjects in Group A, and on Day 8 to subjects in Group B as part of a crossover study design.
Sponsors
Qilu Pharmaceutical Co., Ltd.
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
QUADRUPLE (Subject, Caregiver, Investigator, Outcomes Assessor)
Eligibility
Sex/Gender
ALL
Age
18 Years to 50 Years
Healthy volunteers
Yes
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).
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Peak Plasma Concentration (Cmax) | Day 1 & Day 8: Pre-dose, 10, 20, 30, 45 minutes, and 1 hour post-administration. | Evaluated in plasma and tears. |
| Area Under the Plasma Concentration-Time Curve (AUC0-∞) | Day 1 & Day 8: Pre-dose, 10, 20, 30, 45 minutes, and 1 hour post-administration. | Evaluated in plasma and tears. |
| Area Under the Plasma Concentration-Time Curve (AUC0-t) | Day 1 & Day 8: Pre-dose, 10, 20, 30, 45 minutes, and 1 hour post-administration. | Evaluated in plasma and tears. |
| Time to Peak Plasma Concentration (Tmax) | Day 1 & Day 8: Pre-dose, 10, 20, 30, 45 minutes, and 1 hour post-administration. | Assessment: Evaluated in plasma and tears. |
| 5. Terminal Phase Half-Life (T1/2) | Day 1 & Day 8: Pre-dose, 10, 20, 30, 45 minutes, and 1 hour post-administration. | Evaluated in plasma and tears |
| Elimination Rate Constant (λz) | Day 1 & Day 8: Pre-dose, 10, 20, 30, 45 minutes, and 1 hour post-administration. | Evaluated in plasma and tears. |
| Percentage Extrapolated AUC (AUC_%Extrap) | Day 1 & Day 8: Pre-dose, 10, 20, 30, 45 minutes, and 1 hour post-administration | Evaluated in plasma and tears. |
Countries
China
Outcome results
None listed