A Phase I, Cross-over Study Comparing the Relative Bioavailability of Laroprovstat Plus Ezetimibe Fixed Combination Drug Products Versus Their Single Therapy Products in Healthy Adults

NCT07622433 | Not Yet Recruiting Phase 1 FDA Drug

• 1 other identifier: D7963C00001
• Study Type: interventional
• Target: 18
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to assess how well laroprovstat and ezetimibe combined in a single tablet to be taken by mouth works and what the body does to the drug (pharmacokinetics) compared with laroprovstat and ezetimibe individual tablets to be taken by mouth (relative bioavailability) as well as to see if there is any effect of eating compared to fasting (food effect) in healthy adults.

Conditions

Healthy Participants

Keywords

Fixed Combination Drug Products; Bioavailability; Pharmacokinetics; Cross-over study; Hyperlipidemia; Dyslipidemia; Relative bioavailability; Food effect; Oral Formulations

Outcome Measures

Primary Outcomes (3)

• Area under concentration-time curve from time 0 to infinity (AUCinf)

  To evaluate the relative bioavailability between the FCDPs and the STPs of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe.

  Day 1 to 11 of Treatment Periods 1, 2, 3, and 4 (each treatment period is 11 days)

• Area under concentration-curve from time 0 to the last quantifiable concentration (AUClast)

  To evaluate the relative bioavailability between the FCDPs and the STPs of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe.

  Day 1 to 11 of Treatment Periods 1, 2, 3, and 4 (each treatment period is 11 days)

• Maximum observed drug concentration (Cmax)

  To evaluate the relative bioavailability between the FCDPs and the STPs of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe.

  Day 1 to 11 of Treatment Periods 1, 2, 3, and 4 (each treatment period is 11 days)

Secondary Outcomes (7)

• Plasma Time to reach maximum observed concentration (tmax)

  Day 1 to 11 of Treatment Periods 1, 2, 3, and 4 (each treatment period is 11 days)

• Terminal elimination half-life (t½λz)

  Day 1 to 11 of Treatment Periods 1, 2, 3, and 4 (each treatment period is 11 days)

• Apparent total body clearance (CL/F)

  Day 1 to 11 of Treatment Periods 1, 2, 3, and 4 (each treatment period is 11 days)

• Apparent volume of distribution based on the terminal phase (Vz/F)

  Day 1 to 11 of Treatment Periods 1, 2, 3, and 4 (each treatment period is 11 days)

• AUCinf

  Day 1 to 11 of Treatment Periods 1, 2, 3, and 4 (each treatment period is 11 days)

Study Arms (4)

Treatment A

EXPERIMENTAL

Each participant will receive single dose treatment of laroprovstat/ezetimibe FCDP test formulation in a fasted state.

Drug: Laroprovstat/ezetimibe FCDP

Treatment B

EXPERIMENTAL

Each participant will receive single dose treatment of laroprovstat plus ezetimibe single therapy product (STP) reference formulations in a fasted state.

Drug: Laroprovstat STP; Drug: Ezetimibe STP

Treatment C

EXPERIMENTAL

Each participant will receive single dose treatment of laroprovstat/ezetimibe FCDP test formulation in a fed state.

Drug: Laroprovstat/ezetimibe FCDP

Treatment D

EXPERIMENTAL

Each participant will receive single dose treatment of laroprovstat/ezetimibe FCDP test formulation (slow variant) in a fasted state.

Drug: Laroprovstat/ezetimibe FCDP-slow variant

Interventions

Laroprovstat/ezetimibe FCDP DRUG

Laroprovstat/ezetimibe will be administered orally.

Treatment A; Treatment C

Laroprovstat STP DRUG

Laroprovstat will be administered orally.

Treatment B

Ezetimibe STP DRUG

Ezetimibe will be administered orally.

Treatment B

Laroprovstat/ezetimibe FCDP-slow variant DRUG

Laroprovstat/ezetimibe slow variant will be administered orally

Treatment D

Eligibility Criteria

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

You may qualify if:

• Healthy male and female participants aged 18 to 55 years at the time of signing consent.
• All females must have a negative pregnancy test at the Screening Visit and on admission to the study site.
• Females of childbearing potential must not be lactating and if heterosexually active must agree to use an approved method of highly effective contraception.
• Have a Body mass index (BMI) between 18 and 30 kg/m2 inclusive and weigh at least 50 kg.

You may not qualify if:

• History of any clinically important disease or disorder.
• History or presence of gastrointestinal, hepatic, or renal disease or any other condition known to interfere with absorption, distribution, metabolism, or excretion of drugs.
• History of severe allergy/hypersensitivity or ongoing clinically important allergy/hypersensitivity to drugs with a similar chemical structure or class to laroprovstat or ezetimibe.
• Treatment with any lipid lowering therapy or laroprovstat within the 3 months prior to the Screening Visit.
• Treatment with drugs for reduction or inhibition of Proprotein convertase subtilisin/kexin type 9 (PCSK9) within the last 12 months prior to the Screening Visit or inclisiran at any time.

Sponsors & Collaborators

• AstraZeneca: lead

Study Sites (1)

Research Site

Brooklyn, Maryland, 21225, United States

Location

Related Links

• THANK YOU CARD

MeSH Terms

Conditions

Hyperlipidemias; Dyslipidemias

Condition Hierarchy (Ancestors)

Lipid Metabolism Disorders; Metabolic Diseases; Nutritional and Metabolic Diseases

Central Study Contacts

AstraZeneca Clinical Study Information Center

CONTACT

1-877-240-9479; information.center@astrazeneca.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: Each participant will be randomly assigned to one of the 3 treatment sequences: ABCD, BCAD or CABD.

Study Record Dates

• First Submitted: May 28, 2026
• First Posted: June 3, 2026
• Study Start: June 10, 2026
• Primary Completion (Estimated): September 7, 2026
• Study Completion (Estimated): September 7, 2026
• Last Updated: June 4, 2026

Record last verified: 2026-06

Data Sharing

• IPD Sharing: Will share
• Time Frame: AstraZeneca will meet or exceed data availability as per the commitments made to the EFPIA PhRMA Data Sharing Principles. For details of our timelines, please rerefer to our disclosure commitment at https://astrazenecagrouptrials.pharmacm.com/ST/Submission/Disclosure.
• Access Criteria: When a request has been approved AstraZeneca will provide access to the anonymized individual patient-level data via secure research environment Vivli.org. Signed Data Usage Agreement (non-negotiable contract for data accessors) must be in place before accessing requested information.

Locations

US (1)