Study of Single and Multiple Ascending Doses of ZE46-0134 in Healthy Volunteers

NCT ID: NCT06399315

Last Updated: 2025-12-09

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 112 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2023-07-28
• Study Completion Date: 2025-08-26

Brief Summary

This is a clinical study aiming to assess pharmacokinetics and biomarker evidence of ZE46-0134 efficacy in Healthy Volunteers after single and multiple daily doses of the study drug

Detailed Description

This is a Phase 1, double-blind, placebo-controlled, dose escalation study to evaluate the safety, tolerability, PK, PD of orally administered ZE46-0134 in Healthy Volunteers. The study will be conducted in 2 parts: a single ascending dose (SAD) part at up to 6 dose levels and a multiple ascending dose (MAD) part at up to 5 dose levels. Evaluation of dose levels will be conducted in a sequential fashion with lower dose levels evaluated first in the sequence. Dosing in each cohort will start with two sentinel participants with one of the two sentinels randomised to receive ZE46-0134 and the other randomised to receive placebo. The food-effect will be investigated in SAD part and safety/PK of co-administration with rabeprazole will be investigated in MAD part.

Conditions

AML

Study Design

• Allocation Method: RANDOMIZED
• Intervention Model: SEQUENTIAL
• Primary Study Purpose: TREATMENT
• Blinding Strategy: DOUBLE

Study Groups

Level 3 Single dose

Dose level 3. SAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Level 2 Single dose after food

Dose level 2 with a fat meal. SAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Level 4 Single dose

Dose level 4. SAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Level 1 Multiple doses

Dose level 1. MAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Level 1 Multiple doses + rabeprazole

Dose level 2. MAD study part. 6 participants will receive the study drug and 2 participants will receive placebo. The drug is co-administered with rabeprazole

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Rabeprazole, 20mg oral

Intervention Type: DRUG

Rabeprazole 20 mg daily will be administered for 2 prior ZE46-0134 and 7 co-administered

Level 2 Multiple doses

Dose level 2. MAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Level 3 Single dose with itraconazole

Dose level 3. SAD study part. 6 participants will receive the study drug and 2 participants will receive placebo, in conjunction with itraconazole

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Itraconazole (200 mg)

Intervention Type: DRUG

Itraconazole 200 mg BID

Level 5 Single dose

Dose level 5. SAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Level 6 Single dose

Dose level 6. SAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Level 3 Multiple doses

Dose level 3. MAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Level 4 Multiple doses

Dose level 4. MAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Level 5 Multiple doses

Dose level 5. MAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Level 1 Single dose

Dose level 1. SAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Level 2 Single dose

Dose level 2. SAD study part. 6 participants will receive the study drug and 2 participants will receive placebo

Group Type: EXPERIMENTAL

ZE46-0134 or placebo

Intervention Type: DRUG

The patients will receive ZE46-0134 or placebo

Interventions

ZE46-0134 or placebo

The patients will receive ZE46-0134 or placebo

Intervention Type: DRUG

Rabeprazole, 20mg oral

Rabeprazole 20 mg daily will be administered for 2 prior ZE46-0134 and 7 co-administered

Intervention Type: DRUG

Itraconazole (200 mg)

Itraconazole 200 mg BID

Intervention Type: DRUG

Other Intervention Names

lomonitininb

Eligibility Criteria

Inclusion Criteria

• 1. Must have given written informed consent before any study-related activities are carried out and must be able to understand the full nature and purpose of the trial, including possible risks and adverse effects.

2. Adult males and females, 18 to 55 years of age (inclusive) at screening. 3. Body mass index (BMI) ≥ 18.5 and ≤ 32.0 kg/m2, with a body weight (to 1 decimal place) ≥ 50.0 kg at screening.

4. Medically healthy without clinically significant abnormalities (in the opinion of the Investigator) at the screening visit and prior to dosing

Exclusion Criteria

1. History or presence of significant cardiovascular, pulmonary, hepatic, renal, haematological, gastrointestinal, endocrine, immunologic, dermatologic or neurological disease, including any acute illness or major surgery within the past 3 months determined by the PI to be clinically significant.

2. Acute infections within 4 weeks prior to screening or current infection that requires systemically absorbed antibiotic, antifungal, antiparasitic or antiviral medications.

3. Presence or history of any abnormality or illness, including gastrointestinal surgery, which in the opinion of the PI may affect absorption, distribution, metabolism or elimination of the study drug.

4. Any history of malignant disease in the last 5 years (excludes surgically resected skin squamous cell or basal cell carcinoma).

5. Any screening laboratory result outside the normal laboratory reference range (as confirmed upon repeated testing) and deemed clinically significant by the PI.

6. Presence of clinically relevant immunosuppression from, but not limited to, immunodeficiency conditions such as common variable hypogammaglobulinemia

• Minimum Eligible Age: 18 Years
• Maximum Eligible Age: 55 Years
• Eligible Sex: ALL
• Accepts Healthy Volunteers: Yes

Sponsors

Lomond Therapeutics Holdings, Inc.

INDUSTRY

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Locations

Linear Clinical Research Ltd

Perth, Nedlands, Australia

Countries

Australia

Other Identifiers

CT-2023-CTN-03208-1

Identifier Type: OTHER

Identifier Source: secondary_id

ZE46-0134-0001

Identifier Type: -

Identifier Source: org_study_id