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

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

Status

Active, not recruiting

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT07622433

Enrollment

Registered

2026-06-03

Start date

2026-06-10

Completion date

2026-09-07

Last updated

2026-07-28

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Participants

Keywords

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

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.

Detailed description

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.

Interventions

DRUGLaroprovstat/ezetimibe FCDP

Laroprovstat/ezetimibe will be administered orally.

DRUGLaroprovstat STP

Laroprovstat will be administered orally.

DRUGEzetimibe STP

Ezetimibe will be administered orally.

DRUGLaroprovstat/ezetimibe FCDP-slow variant

Laroprovstat/ezetimibe slow variant will be administered orally

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

TREATMENT

Masking

NONE

Intervention model description

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

Eligibility

Sex/Gender

ALL

Age

18 Years to 55 Years

Healthy volunteers

Yes

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.

Design outcomes

Primary

Measure	Time frame	Description
Area under concentration-time curve from time 0 to infinity (AUCinf)	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.
Area under concentration-curve from time 0 to the last quantifiable concentration (AUClast)	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.
Maximum observed drug concentration (Cmax)	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

Measure	Time frame	Description
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)	To examine the pharmacokinetic (PK) profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as FCDPs or STPs.
Terminal elimination half-life (t½λz)	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.
Apparent total body clearance (CL/F)	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.
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)	To examine the PK profiles of laroprovstat, ezetimibe (unconjugated), ezetimibe-glucuronide, and total ezetimibe when administered as FCDPs or STPs.
AUCinf	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.
AUClast	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.
Cmax	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.

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Jul 29, 2026