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Active, Not Recruiting

NCT Number: NCT07622433

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

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.

Active, Not Recruiting

This study is active but is not currently recruiting participants.

Key information

Conditions

Healthy Participants Dyslipidemias Hyperlipidemias Lipid Metabolism Disorders Metabolic Diseases Nutritional and Metabolic Diseases

Age range

18 year–55 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Research Site

Brooklyn, Maryland, 21225, United States

About this study

This is a randomized, open-label, 4-period, single-dose, cross-over study.

The study will comprise of a screening period, 4 treatment periods, and 3 washout periods. The following treatments will be given during the study:

  • Treatment A: laroprovstat/ezetimibe fixed combination drug product (FCDP) test formulation in fasted state
  • Treatment B: laroprovstat tablet plus ezetimibe reference formulations in fasted state
  • Treatment C: laroprovstat/ezetimibe FCDP test formulation in fed state
  • Treatment D: laroprovstat/ezetimibe FCDP test formulation-slow variant in fasted state

Participants will be randomly assigned to either of the 3 treatment sequences: ABCD, BCAD, or CABD.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • 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.

Exclusion criteria

  • 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.

Treatment and study plan

Laroprovstat/ezetimibe FCDP

Drug

Laroprovstat/ezetimibe will be administered orally.

Laroprovstat STP

Drug

Laroprovstat will be administered orally.

Ezetimibe STP

Drug

Ezetimibe will be administered orally.

Laroprovstat/ezetimibe FCDP-slow variant

Drug

Laroprovstat/ezetimibe slow variant will be administered orally

Primary outcomes

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

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

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

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

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

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

  3. Maximum observed drug concentration (Cmax)

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

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

Secondary outcomes

  1. Plasma Time to reach maximum observed concentration (tmax)

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

    To examine the pharmacokinetic (PK) profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as FCDPs or STPs.

  2. Terminal elimination half-life (t½λz)

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

    To examine the PK profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as FCDPs or STPs.

  3. Apparent total body clearance (CL/F)

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

    To examine the PK profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as FCDPs or STPs.

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

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

    To examine the PK profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as FCDPs or STPs.

  5. AUCinf

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

    To examine the effect on the PK profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as an FCDP with a high-fat meal compared to when administered as an FCDP in the fasted state.

  6. AUClast

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

    To examine the effect on the PK profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as an FCDP with a high-fat meal compared to when administered as an FCDP in the fasted state.

  7. Cmax

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

    To examine the effect on the PK profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as an FCDP with a high-fat meal compared to when administered as an FCDP in the fasted state.

Sponsors and collaborators

Lead sponsor

AstraZeneca

Industry

Registry information

Official study title

A Phase I, Randomized, Open-label, 4-period, 4-treatment, Single-dose, Cross-over Study to Assess the Relative Bioavailability of Laroprovstat/Ezetimibe Fixed Combination Drug Products to the Single Therapy Products in Healthy Adults

Important dates

Study start
2026
Primary completion
2026
Study completion
2026
First posted
Jun 3, 2026
Registry last updated
Jul 28, 2026

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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