Evaluating Bioequivalence of a Fixed Dose Combination Versus Individual Tablets of Bempedoic Acid, Ezetimibe, and Rosuvastatin

NCT07182383 | Completed Phase 1

• 2 other identifiers: DSE-BMP-0002-CIS-MA2024-519850-35-00
• Study Type: interventional
• Target: 58
• Locations: 1 country
• Sites: 1

Brief Summary

The recommended first-line treatment of cardiovascular disease is a statin monotherapy; however, combination therapies represent an opportunity for an individualized, patient centered approach to lower low density lipoprotein cholesterol (LDL-C) and reduce atherosclerotic cardiovascular disease risk in patients unable to reach individualized serum LDL-C levels. This study will test the bioequivalence of a test fixed dose combination (FDC) vs the co-administration of individual tablets.

Conditions

Healthy Subjects

Keywords

Healthy Subjects; Bioequivalence

Outcome Measures

Primary Outcomes (2)

• Pharmacokinetic Parameter Area Under the Curve (AUC)

  Area under the curve (AUC) from time of dosing (t=0h) to time 72 hours (AUC72h) or AUC from time of dosing (t=0h) to the time of last measurable (non-zero) concentration (AUClast) will be assessed using noncompartmental methods

  Pre-dose (t=0h), and at 0.17 hours (10 minutes), 0.5 hours, 0.75 hours, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 10 hours, 12 hours, 24 hours (Day 2), 48 hours (Day 3), and 72 hours (Day 4) post-dose

• Pharmacokinetic Parameter Maximum Observed Concentration (Cmax)

  Maximum observed concentration will be assessed.

  Pre-dose (t=0h), and at 0.17 hours (10 minutes), 0.5 hours, 0.75 hours, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 10 hours, 12 hours, 24 hours (Day 2), 48 hours (Day 3), and 72 hours (Day 4) post-dose

Secondary Outcomes (5)

• Pharmacokinetic Parameters (AUCinf and AUClast/AUCinf)

  Pre-dose (t=0h), and at 0.17 hours (10 minutes), 0.5 hours, 0.75 hours, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 10 hours, 12 hours, 24 hours (Day 2), 48 hours (Day 3), and 72 hours (Day 4) post-dose

• Pharmacokinetic Parameter Time to Reach Maximum Observed Concentration (Tmax)

  Pre-dose (t=0h), and at 0.17 hours (10 minutes), 0.5 hours, 0.75 hours, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 10 hours, 12 hours, 24 hours (Day 2), 48 hours (Day 3), and 72 hours (Day 4) post-dose

• Pharmacokinetic Parameter Terminal Half-life (t1/2)

  Pre-dose (t=0h), and at 0.17 hours (10 minutes), 0.5 hours, 0.75 hours, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 10 hours, 12 hours, 24 hours (Day 2), 48 hours (Day 3), and 72 hours (Day 4) post-dose

• Pharmacokinetic Parameter First Order Rate Constant Associated With The Terminal Portion of the Concentration-Time Curve (Kel)

  Pre-dose (t=0h), and at 0.17 hours (10 minutes), 0.5 hours, 0.75 hours, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, 6 hours, 8 hours, 10 hours, 12 hours, 24 hours (Day 2), 48 hours (Day 3), and 72 hours (Day 4) post-dose

• Number of Participants Reporting Treatment-emergent Adverse Events (TEAEs)

  Baseline to end of study, up to approximately 2 months

Study Arms (2)

Test Formulation

EXPERIMENTAL

Healthy participants who are randomized to receive the fixed dose triplet combination with bempedoic acid 180 mg/ezetimibe 10 mg/rosuvastatin 20 mg (test formulation).

Drug: Bempedoic acid; Drug: Ezetimibe; Drug: Rosuvastatin

Reference Formulation

ACTIVE COMPARATOR

Healthy participants who are randomized to receive co-administration of bempedoic acid 180 mg + ezetimibe 10 mg + rosuvastatin 20 mg (reference formulation).

Drug: Bempedoic acid; Drug: Ezetimibe; Drug: Rosuvastatin

Interventions

Bempedoic acid DRUG

180 mg film coated tablet administered individually or as FDC Component of FDC

Also known as: Nilemdo®

Reference Formulation; Test Formulation

Ezetimibe DRUG

10 mg tablet administered individually or as FDC Component of FDC

Also known as: Ezetrol®

Reference Formulation; Test Formulation

Rosuvastatin DRUG

20 mg film coated tablet administered individually or as FDC Component of FDC

Also known as: Crestor®

Reference Formulation; Test Formulation

Eligibility Criteria

• Age: 18 Years - 60 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy male and female participants ≥18 and ≤60 years, at the time of signing the informed consent.
• Body mass index (BMI) ≥18.5 and ≤30.0 kg/m\^2.
• Female participants of childbearing potential agree to undergo pregnancy tests resulting in negative results, non-lactating status, and agree to use accepted contraceptive method from at least 4 weeks prior to admission to the first study period until the end of the study, and if with a non-vasectomized nor infertile male partner, agree to use an appropriate method of contraception (i.e., abstinence, hormonal, intrauterine device, bilateral tubal occlusion).
• No clinically relevant diseases captured in medical history.
• No clinically relevant abnormalities on physical examination.
• No clinically relevant abnormalities on vital signs.
• No clinically relevant abnormalities on 12-lead electrocardiogram (ECG).
• No clinically relevant abnormalities on clinical laboratory tests.
• Aspartate aminotransferase (AST) and alanine aminotransferase (ALT) ≤1.5 times the upper limit of normal range (ULN).
• Estimated renal creatinine clearance (CrCl) above the lower limit of normal range, based on creatinine clearance calculation by the Cockcroft-Gault formula and normalized to an average body surface area of 1.73 m\^2.
• Willingness to accept and comply with all study procedures and restrictions.
• Non-smoker or ex-smoker (i.e., someone who abstained from using tobacco- or nicotine-containing products for at least 3 months prior to Screening).
• Ability to comprehend and willingness to freely sign the informed consent.

Sponsors & Collaborators

• Daiichi Sankyo: lead

Study Sites (1)

Research Site

Porto, 4250-449, Portugal

Location

MeSH Terms

Interventions

8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid; Ezetimibe; Rosuvastatin Calcium

Intervention Hierarchy (Ancestors)

Azetidines; Azetines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Sulfonamides; Amides; Organic Chemicals; Fluorobenzenes; Hydrocarbons, Fluorinated; Hydrocarbons, Halogenated; Hydrocarbons; Sulfones; Sulfur Compounds; Pyrimidines

Study Design

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

Study Record Dates

• First Submitted: September 11, 2025
• First Posted: September 19, 2025
• Study Start: September 29, 2025
• Primary Completion: November 24, 2025
• Study Completion: November 24, 2025
• Last Updated: December 16, 2025

Record last verified: 2025-12

Data Sharing

• IPD Sharing: Will not share

Locations

PT (1)