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

NCT07201545 | Completed Phase 1

• 2 other identifiers: DSE-BMP-0004-CIS-MA2024-519852-10-00
• 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 low density lipoprotein cholesterol (LDL-C) lowering and atherosclerotic cardiovascular disease risk reduction in patients unable to reach individualized serum LDL-C levels. This study will test the bioequivalence of a test fixed dose combination (FDC) product versus the co-administered individual reference products.

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) postdose

• 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) postdose

Secondary Outcomes (6)

• Pharmacokinetic Parameters (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) postdose

• Pharmacokinetic Parameters (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) postdose

• 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) postdose

• 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) postdose

• 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) postdose

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 as FDC or co-administered with ezetimibe Component of FDC

Also known as: Nilemdo®

Reference Formulation; Test Formulation

Ezetimibe DRUG

10 mg tablet administered as FDC or co-administered with bempedoic acid 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, and if with a non-vasectomized nor infertile male partner, agree to use an appropriate method of contraception.
• 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) above 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)

BlueClinical Phase I BlueClinical - Investigação e Desenvolvimento em Saúde, Lda.

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 23, 2025
• First Posted: October 1, 2025
• Study Start: October 7, 2025
• Primary Completion: December 10, 2025
• Study Completion: December 10, 2025
• Last Updated: December 18, 2025

Record last verified: 2025-12

Data Sharing

• IPD Sharing: Will not share

Locations

PT (1)