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

NCT06399315 | Completed Phase 1

• 2 other identifiers: ZE46-0134-0001CT-2023-CTN-03208-1
• Study Type: interventional
• Target: 112
• Locations: 1 country
• Sites: 1

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

Conditions

AML

Outcome Measures

Primary Outcomes (1)

• Plasma concentration

  Plasma concentration, ng/mL

  72 hours for SAD, 10 days for MAD

Secondary Outcomes (4)

• Incidence of AEs

  8 days in SAD part, 17 days for MAD part

• Incidence of drug-related AEs

  8 days in SAD part, 17 days for MAD part

• Incidence of SAEs

  8 days in SAD part, 17 days for MAD part

• Incidence of lab deviations

  Time Frame: 8 days in SAD part, 17 days for MAD part

Study Arms (14)

Level 1 Single dose

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Level 2 Single dose

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Level 3 Single dose

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Level 2 Single dose after food

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Level 4 Single dose

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Level 1 Multiple doses

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Level 1 Multiple doses + rabeprazole

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo; Drug: Rabeprazole, 20mg oral

Level 2 Multiple doses

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Level 3 Single dose with itraconazole

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo; Drug: Itraconazole (200 mg)

Level 5 Single dose

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Level 6 Single dose

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Level 3 Multiple doses

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Level 4 Multiple doses

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Level 5 Multiple doses

EXPERIMENTAL

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

Drug: ZE46-0134 or placebo

Interventions

Itraconazole (200 mg) DRUG

Itraconazole 200 mg BID

Level 3 Single dose with itraconazole

ZE46-0134 or placebo DRUG

The patients will receive ZE46-0134 or placebo

Also known as: lomonitininb

Level 1 Multiple doses; Level 1 Multiple doses + rabeprazole; Level 1 Single dose; Level 2 Multiple doses; Level 2 Single dose; Level 2 Single dose after food; Level 3 Multiple doses; Level 3 Single dose; Level 3 Single dose with itraconazole; Level 4 Multiple doses; Level 4 Single dose; Level 5 Multiple doses; Level 5 Single dose; Level 6 Single dose

Rabeprazole, 20mg oral DRUG

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

Level 1 Multiple doses + rabeprazole

Eligibility Criteria

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

You may qualify if:

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

You may not qualify if:

• 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.
• Acute infections within 4 weeks prior to screening or current infection that requires systemically absorbed antibiotic, antifungal, antiparasitic or antiviral medications.
• 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.
• Any history of malignant disease in the last 5 years (excludes surgically resected skin squamous cell or basal cell carcinoma).
• Any screening laboratory result outside the normal laboratory reference range (as confirmed upon repeated testing) and deemed clinically significant by the PI.
• Presence of clinically relevant immunosuppression from, but not limited to, immunodeficiency conditions such as common variable hypogammaglobulinemia

Sponsors & Collaborators

• Lomond Therapeutics Holdings, Inc.: lead

Study Sites (1)

Linear Clinical Research Ltd

Perth, Nedlands, WA 6009, Australia

Location

MeSH Terms

Interventions

Rabeprazole; Itraconazole

Intervention Hierarchy (Ancestors)

2-Pyridinylmethylsulfinylbenzimidazoles; Sulfoxides; Sulfur Compounds; Organic Chemicals; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Benzimidazoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Triazoles; Azoles; Piperazines

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Masking Details: Double-Blind, Placebo-Controlled
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 1, 2024
• First Posted: May 3, 2024
• Study Start: July 28, 2023
• Primary Completion: June 30, 2025
• Study Completion: August 26, 2025
• Last Updated: December 9, 2025

Record last verified: 2025-12

Locations

AU (1)