Pharmacokinetics, Pharmacodynamics, Safety and Tolerability of OC-01 in Adult Chinese With Dry Eye Disease

An Open-Label, Multiple-Dose Clinical Study to Evaluate the Pharmacokinetics, Pharmacodynamics, Safety and Tolerability of OC-01 (Varenicline Solution) Nasal Spray in Adult Chinese Subjects With Dry Eye Disease

The objective of this study is to evaluate the pharmacokinetics (PK) in adult Chinese subjects with dry eye disease (DED)1 after bilateral nasal spray administration of OC-01 (varenicline solution) Nasal Spray at a concentration of 0.6 mg/mL.

Study Overview

• Status: Completed
• Conditions: Dry Eye Disease
• Intervention / Treatment: Drug: Varenicline Tartrate Nasal Spray

• Study Type: Interventional
• Enrollment (Actual): 9
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Shanghai, China
    • Huashan Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 16 years and older (Adult, Older Adult)
• Accepts Healthy Volunteers: No

Description

Inclusion Criteria:

Have used and/or desired to use an artificial tear substitute for dry eye symptoms within 6 months prior to the Screening Visit

Exclusion Criteria:

• Have had any intraocular surgery (such as cataract surgery) or extraocular surgery in either eye within three months or refractive surgery (e.g., laser-assisted in-situ keratomileusis, laser epithelial keratomileusis, photorefractive keratectomy or corneal implant) within 12 months of the Screening Visit
• Have a history or presence of any ocular disorder or condition in either eye that would, in the opinion of the Investigator, likely interfere with the interpretation of the study results or participant safety such as significant corneal or conjunctival scarring; pterygium or nodular pinguecula; current ocular infection, acute conjunctivitis, or inflammation not associated with dry eye; anterior (epithelial) basement membrane corneal dystrophy or other clinically significant corneal dystrophy or degeneration; ocular herpetic infection; evidence of keratoconus; etc. Blepharitis not requiring treatment and mild meibomian gland disease that are typically associated with DED are allowed.
• Have a systemic condition or disease not stabilized or judged by the Investigator to be incompatible with participation in the study (e.g., current systemic infection, uncontrolled autoimmune disease, uncontrolled immunodeficiency disease, history of myocardial infarction or heart disease, etc.)
• Have a known hypersensitivity to any of the procedural agents or investigational product components
• Have any condition or history that, in the opinion of the investigator, may interfere with study compliance, outcome measures, safety parameters, and/or the general medical condition of the subject.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: OC-01	Drug: Varenicline Tartrate Nasal Spray; Intranasal delivery of OC-01 (varenicline solution) 0.6 mg/mL twice a day (BID) for 28 days.; Other Names: OC-01 (varenicline solution) Nasal Spray

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax of varenicline after the first dosing at Visit 1 [Day 1] and after the last dosing at Visit 3 [Day 28], respectively.	To evaluate the Cmax of varenicline in adult Chinese with dry eye disease (DED) after the first dosing at Visit 1 [Day 1] and after the last dosing at Visit 3 [Day 28], respectively.	Visit 1 [Day 1]: From predose of the 1st dosing to 12 hours post-dose. Visit 3 [Day 28]: From predose of the last dosing to 120 hours post-dose.
Tmax of varenicline after the first dosing at Visit 1 [Day 1] and after the last dosing at Visit 3 [Day 28], respectively.	To evaluate the Tmax of varenicline in adult Chinese subjects with DED after the first dosing at Visit 1 [Day 1] and after the last dosing at Visit 3 [Day 28], respectively.	Visit 1 [Day 1]: From predose of the 1st dosing to 12 hours post-dose. Visit 3 [Day 28]: From predose of the last dosing to 120 hours post-dose.
AUCtau(Area under the concentration-time curve during a dosing interval) of varenicline after the first dosing at Visit 1 [Day 1] and after the last dosing at Visit 3 [Day 28], respectively.	To evaluate the AUCtau of varenicline in adult Chinese subjects with DED after the first dosing at Visit 1 [Day 1] and after the last dosing at Visit 3 [Day 28], respectively.	Visit 1 [Day 1]: From predose of the 1st dosing to 12 hours post-dose. Visit 3 [Day 28]: From predose of the last dosing to 120 hours post-dose.
AUC0-last(Area under the concentration-time curve from time 0 to the time of the last measured non-zero concentration) of varenicline after the first dosing at Visit 1 [Day 1] and after the last dosing at Visit 3 [Day 28], respectively.	To evaluate the AUC0-last of varenicline in adult Chinese subjects with DED after the first dosing at Visit 1 [Day 1] and after the last dosing at Visit 3 [Day 28], respectively.	Visit 1 [Day 1]: From predose of the 1st dosing to 12 hours post-dose. Visit 3 [Day 28]: From predose of the last dosing to 120 hours post-dose.
T1/2 of varenicline after the last dosing at Visit 3 [Day 28]	To evaluate the T1/2 of varenicline after the last dosing at Visit 3 [Day 28] in adult Chinese subjects with DED.	Visit 3 [Day 28]: From predose of the last dosing to 120 hours post-dose
λz of varenicline after the last dosing at Visit 3 [Day 28]	To evaluate the λz of varenicline after the last dosing at Visit 3 [Day 28] in adult Chinese subjects with DED.	Visit 3 [Day 28]: From predose of the last dosing to 120 hours post-dose

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Change from baseline in Schirmer's Test Score (STS) at Visit 1 [Day 1], Visit 2 [Day 14] and Visit 3 [Day 28]	To assess the Schirmer's Test Score (STS) using Schirmer's strips in adult Chinese subjects with DED after bilateral nasal spray administration of OC-01 (varenicline solution) Nasal Spray at a concentration of 0.6 mg/mL. For STS, the minimum value is 0.0mm, the maximum value is 35.0mm, the higher scores of change mean a better outcome.	From Day 1 to Day 28
Change from baseline in Eye Dryness Score (EDS) at Visit 2 [Day 14] and Visit 3 [Day 28]	To assess the Eye Dryness Score (EDS) using a Visual Analog Scale (VAS) in adult Chinese subjects with DED after bilateral nasal spray administration of OC-01 (varenicline solution) Nasal Spray at a concentration of 0.6 mg/mL. For EDS, the minimum value is 0mm, the maximum value is 100mm, the higher scores of change mean a worse outcome.	From Day 14 to Day 28

Collaborators and Investigators

• Sponsor: Ji Xing Pharmaceuticals (Shanghai) Co., Ltd.
• Collaborators: Oyster Point Pharma, Inc.
• Investigators: Principal Investigator: LU, Doctor, Huashan Hospital; Principal Investigator: ZHANG, Doctor, Huashan Hospital; Study Director: DING, Ji Xing Pharmaceuticals (Shanghai) Co., Ltd.

Study record dates

Study Major Dates

• Study Start (Actual): December 7, 2022
• Primary Completion (Actual): April 27, 2023
• Study Completion (Actual): April 27, 2023

Study Registration Dates

• First Submitted: September 27, 2022
• First Submitted That Met QC Criteria: October 11, 2022
• First Posted (Actual): October 12, 2022

Study Record Updates

• Last Update Posted (Actual): May 1, 2023
• Last Update Submitted That Met QC Criteria: April 28, 2023
• Last Verified: April 1, 2023

More Information

Terms related to this study

• Keywords: Dry Eye Disease; OC-01 (Varenicline Solution)
• Additional Relevant MeSH Terms: Lacrimal Apparatus Diseases; Keratoconjunctivitis; Conjunctivitis; Conjunctival Diseases; Keratitis; Corneal Diseases; Eye Diseases; Dry Eye Syndromes; Keratoconjunctivitis Sicca; Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Cholinergic Agents; Nicotinic Agonists; Cholinergic Agonists; Varenicline
• Other Study ID Numbers: JX03003

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: Yes