Evaluate the Safety, Tolerance, and Pharmacokinetic Profiles of Timolol Maleate Gel

NCT06824948 | Completed Phase 1

• 2 other identifiers: ASN001C001CRC-C1824
• Study Type: interventional
• Target: 28
• Locations: 1 country
• Sites: 1

Brief Summary

The goal of this clinical trial is to to evaluate the safety, tolerance, and pharmacokinetic profiles of Timolol Maleate Gel in healthy Chinese adult subjects. The main questions aim to answer are:

• The pharmacokinetic endpoints: Single dose:Tmax, Cmax, etc. Multiple doses:AUC0-t, AUC0-inf, λz, t1/2, etc.
• The safety and tolerance endpoints: Physical examination, vital signs, 12-lead ECG, laboratory tests (hematology, blood biochemistry and urinalysis), adverse events, local tolerance. Researchers will compare TM gel to a placebo (a look-alike substance that contains no drug) to see if TM gel works to treat IH.

Conditions

Healthy Subjects

Outcome Measures

Primary Outcomes (8)

• Local tolerance

  Local tolerance will be evaluated by an investigator or designated evaluator (e.g., dermatologist) using the blinding method.The intensity (e.g., No evidence of irritation;Minimal erythema that is barely perceptible;Definite erythema that is readily visible and minimal edema or minimal papular response;Erythema and papules, et al) of the skin response is assessed on a 8 point scale.Other response score is assessed from "A" to "H".

  13 Days

• Adverse events

  Frequency, severity and relatedness of adverse events

  Throughout study completion, an average 13 days

• Vital signs (blood pressure)

  Number of participants with clinically significant changes in vital signs (blood pressure)

  the screening phase, Day -1, Day 1, 3, 6, 9, 12, and Day 13.

• Vital signs (temperature)

  Number of participants with clinically significant changes in vital signs (temperature)

  the screening phase, Day -1, Day 1, 3, 6, 9, 12, and Day 13.

• Vital signs (pulse rate)

  Number of participants with clinically significant changes in vital signs (pulse rate)

  the screening phase, Day -1, Day 1, 3, 6, 9, 12, and Day 13.

• Laboratory tests

  Number of participants with clinical laboratory abnormalities (including hematology, blood biochemistry and urinalysis).

  the screening phase, the baseline phase, and on Days 6 and 13.

• Physical examinations

  Number of participants with clinically significant changes in physical examinations.

  the screening phase, baseline phase and on Day 13

• 12-lead ECG

  Number of participants with clinically significant changes in 12-lead ECG.

  the screening phase, baseline phase, Day 1, 3, 6, 9, 12, and Day 13.

Secondary Outcomes (7)

• Tmax

  Day1 to Day13

• Cmax

  Day1 to Day13

• AUC0-t

  Day1 to Day13

• AUC0-inf

  Day1 to Day13

• λz

  Day1 to Day13

Study Arms (3)

Group 2-0.5%TM

EXPERIMENTAL

Participants will be randomized to receive 0.5%TM or matching placebo 2 times a day.

Drug: Timolol Maleate Gel; Drug: Placebo

Group 3-0.5%TM

EXPERIMENTAL

Participants will be randomized to receive 0.5%TM or matching placebo 3 times a day.

Drug: Timolol Maleate Gel; Drug: Placebo

Group 1-0.5%TM

EXPERIMENTAL

Participants will be randomized to receive 0.5%TM or matching placebo 1 time a day.

Drug: Timolol Maleate Gel; Drug: Placebo

Interventions

Timolol Maleate Gel DRUG

A 2-day washout phase follows 1 dose on Day 1, the subjects are applied with 0.5% timolol maleate gel one time a day during Day 3-Day 12.

Group 1-0.5%TM

Placebo DRUG

A 2-day washout phase follows 1 dose on Day 1, the subjects are applied with placebo one time a day during Day 3-Day 12.

Group 1-0.5%TM

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy adult male or female subjects aged 18-55 years (including the cut point, subject to the time of signing the ICF);
• Subjects with the body mass index (BMI) of 19-26 kg/m2 (including the cut point), where the body weight should be ≥ 50 kg for male subjects and ≥ 45 kg for female subjects;
• Subjects who have no pregnancy plan, voluntarily adopt effective birth controls, and have no sperm donation or egg donation plan during the study until 3 months after the last dose. For specific birth controls, see Appendix 1: Birth Control, Definition of Female Subjects of Childbearing Age, and Contraception Requirements;
• Subjects fully understand the study objective, nature, methods and possible adverse reactions, voluntarily become subjects, and sign the ICFs;
• Subjects who have no skin damage or scar or skin disease at the administration site; Subjects who can complete the trial as required in the protocol.

You may not qualify if:

• Subjects who are allergic to timolol maleate and similar drugs;
• Subjects who have any difficulty in venous blood collection;
• Subjects who have cardiogenic shock, Grade I or Grade III atrioventricular block, cardiac failure, sinus bradycardia, hypotension, and CS as assessed by the study physician;
• Subjects who have bronchial asthma, airway sensitive disease, ventilation difficult or other pulmonary disorders;
• Subjects who have had a history of drug abuse in the past five years or used drugs within the 3 months before the study; or subjects who are positive in the drug abuse screening test in the screening phase;
• Subjects who have smoked more than 5 cigarettes a day within the 3 months before screening;
• Subjects who have consumed more than 14 units of alcohol (1 unit of alcohol = 360 mL beer or 45 mL 40% spirits or 150 mL wine) weekly within 6 months before the screening or have taken alcohol-containing products 48 h pre-dose, or were or positive in the alcohol breath test in the screening phase and/or the baseline phase;
• Subjects who have used any drug that induces or inhibits liver metabolic enzymes within 28 days pre-dose in the study;
• Subjects who have used any Rx, OTC or Chinese herbal medicine within 14 days pre-dose in the study;
• Subjects who have took food or drink (such as grapefruit) containing enzymes that can induce or inhibit liver metabolism within 7 days pre-dose in the study;
• Subjects who have ingested any food or drink containing caffeine or xanthine (e.g., coffee, tea, chocolate) during the period at 48 ho pre-dose to completion of the last PK blood sampling;
• Subjects who have diseases or factors with clinical abnormalities, including but not limited to neurological, cardiovascular, blood, liver, kidney, gastrointestinal, respiratory, metabolic, endocrine, immune, skeletal system diseases or other factors;
• Results of the vital signs assessment, physical examinations, laboratory test, 12-lead electrocardiogram and chest radiograph showed CS;
• Subjects who are human immunodeficiency virus (HIV) antibody positive, hepatitis B surface antigen positive, hepatitis C virus antibody positive, or syphilis antibody positive;
• Female subjects who are positive for pregnancy test in the screening phase or the baseline phase or who are breastfeeding;

Sponsors & Collaborators

• Auson Pharmaceuticals Inc.: lead

Study Sites (1)

Shanghai Xuhui District Central Hospital

Shanghai, Shanghai Municipality, 200031, China

Location

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: QUADRUPLE
• Who Masked: PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: January 23, 2025
• First Posted: February 13, 2025
• Study Start: October 12, 2018
• Primary Completion: December 12, 2018
• Study Completion: December 12, 2018
• Last Updated: February 13, 2025

Record last verified: 2025-02

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)