Investigating the Effect of Food on the Bioavailability of a Fixed Dose Combination of Obicetrapib and Ezetimibe

A Study to Assess the Effect of Food on the Bioavailability of Obicetrapib and Ezetimibe After Administration of a Fixed-Dose Combination Formulation of Obicetrapib/Ezetimibe, 10 mg/10 mg in Healthy Adult Subjects

This study will assess the effect of food on the bioavailability of obicetrapib and ezetimibe after a single-dose administration of a fixed-dose combination formulation of obicetrapib/ezetimibe, 10 mg/10 mg in healthy adult male and female subjects under fasted and fed conditions.

Study Overview

• Status: Active, not recruiting
• Conditions: Healthy Volunteer Study
• Intervention / Treatment: Drug: Fixed-Dose Combination (FDC) Tablet

Detailed Description

This is an open-label, single-dose, randomized, two-treatment, two-period, two-sequence crossover relative bioavailability study under fasted and fed conditions. It will assess the effect of food on the bioavailability of obicetrapib and ezetimibe after a single-dose administration of a fixed-dose combination formulation of obicetrapib/ezetimibe, 10 mg/10 mg in healthy adult male and female subjects under fasted and fed conditions. The screening period will be up to 28 days. Patients that are eligible will enter the clinical facility at least 10.5 hours prior to dosing. Depending on their randomization patients will be fed or fasted prior to dosing. They will remain confined for at least 24 hours. After leaving confinement, patients will return to the clinic 9 times for blood draws. At least 56 days after the first dosing, patients will return to the clinic and go through the same process. Those previously fed before dosing will be fasted and those previously fasted will be fed. Patients will return 9 times after their second confinement for additional blood draws.

• Study Type: Interventional
• Enrollment (Estimated): 28
• Phase: Phase 1

Contacts and Locations

• Study Contact: Name: Linda Angeline; Phone Number: 702.435.3902; Email: info@novumprs.com

Study Locations

• United States
  • Nevada
    • Las Vegas, Nevada, United States, 89121
      • NOVUM

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: Adult; Older Adult
• Accepts Healthy Volunteers: Yes

Description

Key Inclusion Criteria:

• Males and Females aged 18 to 65.
• Body Mass Index (BMI) of 18.5-29.9 kg/m², inclusive.
• Females of childbearing potential must be willing to use approved method of birth control.
• Blood pressure 90/60 - 140/90 mmHg, inclusive.
• Hemoglobin level above lower limit of normal.
• Good health.

Key Exclusion Criteria:

• Females who are pregnant, lactating or likely to become pregnant during the study.
• History of allergy, sensitivity to obicetrapib, ezetimibe or any components of the study products, or history of any drug hypersensitivity or intolerance that may compromise the safety of the subject.
• Significant history or current evidence of chronic infectious disease, system disorders, organ dysfunction especially hypothyroidism, renal or hepatic disorders, cardiovascular disorders, respiratory disorders, diabetes or obesity.
• Clinically significant history or presence of gastrointestinal disease or history of malabsorption within the last year.
• History of psychiatric disorders occurring within the last two years that required the subject to be hospitalized or treated with medication.
• Presence of a medical condition requiring regular treatment with prescription drugs.
• Use of statins, cyclosporine, fibrates (e.g., fenofibrate), bile acid seuqstrants (e.g., cholestyramine), or coumarin anticoagulants within 30 days before initial dosing.
• Use of pharmacologic agents known to significantly induce or inhibit drug-metabolizing enzymes (especially inducers and inhibitors of CYP3A4) within 30 days before initial dosing.
• Use of any drug that can alter the absorption of other drugs by affecting gastrointestinal motility or by changing the gastric pH, in the opinion of the Investigator, within 14 days before initial dosing.
• Use of any drug that can increase or decrease the metabolism and excretion of the study drug, within 14 days before initial dosing.
• Receipt of any drug as part of a research study within 30 days before initial dosing.
• Previous participation in a research study with obicetrapib.
• Drug or alcohol addiction requiring treatment in the 12 months before initial dosing.
• History of excessive alcohol consumption (on average more than 14 units of alcohol/week) during the past 12 months.
• Donation or significant loss of whole blood (480 mL or more) within 30 days or plasma within 14 days before initial dosing.
• Positive test results for HIV, Hepatitis B surface antigen, or Hepatitis C antibody.
• Positive test results for drugs of abuse at screening.
• If female, has a positive pregnancy test at screening.
• Use of tobacco- or nicotine-containing products within 30 days before initial dosing.
• Difficulty swallowing tablets or capsules whole.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: FDC Tablet Fed + Fast; Participants will receive a single Obicetrapib/Ezetimibe, 10 mg/10 mg FDC Tablet in a fed condition on Day 1 of treatment followed by a single Obicetrapib/Ezetimibe, 10 mg/10 mg FDC Table in a fasted condition after, at a minimum, a 56 day washout.	Drug: Fixed-Dose Combination (FDC) Tablet; Obicetrapib/Ezetimibe FDC tablet
Experimental: FDC Tablet Fast + Fed; Participants will receive a single Obicetrapib/Ezetimibe, 10 mg/10 mg FDC Tablet in a fasted condition on Day 1 of treatment followed by a single Obicetrapib/Ezetimibe, 10 mg/10 mg FDC Table in a fed condition after, at a minimum, a 56 day washout.	Drug: Fixed-Dose Combination (FDC) Tablet; Obicetrapib/Ezetimibe FDC tablet

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax	Maximum measured plasma concentration following each treatment.	528.00 hours
AUC0-t	Area under the plasma concentration versus time curve from time zero to the time of the last measurable plasma concentration, as calculated by linear trapezoidal method.	528.00 hours
AUC0-∞	Area under the plasma concentration versus time curve from time zero to infinity where AUC0-∞ = AUC0-t + Ct/λz. Ct is the last measurable concentration and λz is the terminal rate constant.	528.00 hours

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Tmax	Time of the maximum measured plasma concentration. If the maximum value occurs at more than one time point, Tmax is defined as the first time point with this value.	528.00 hours
Tlag	Time delay in achieving Tmax	528.00 hours
λz	First order rate constant associated with the terminal (log-linear) portion of the curve.	528.00 hours
t½	The terminal half-life will be calculated as ln(2)/λz.	528.00 hours
CL/F	Apparent oral systemic clearance, calculated as Dose/AUC0-∞	528.00 hours
Vd/F	Apparent volume of distribution during terminal phase, calculated as Dose/(AUC0-∞ × λz)	528.00 hours
R2 adjusted	Goodness of fit statistic for the terminal phase, adjusted for the number of points used in the estimation of λz.	528.00 hours
AUC_%Extrap_obs	The residual area in percentage will be determined by the formula, [(AUC0-∞-AUC0-t)/AUC0-∞] × 100.	528.00 hours

Collaborators and Investigators

• Sponsor: NewAmsterdam Pharma

Study record dates

Study Major Dates

• Study Start (Actual): January 20, 2024
• Primary Completion (Estimated): April 1, 2024
• Study Completion (Estimated): April 1, 2024

Study Registration Dates

• First Submitted: September 17, 2023
• First Submitted That Met QC Criteria: September 17, 2023
• First Posted (Actual): September 22, 2023

Study Record Updates

• Last Update Posted (Estimated): January 23, 2024
• Last Update Submitted That Met QC Criteria: January 20, 2024
• Last Verified: January 1, 2024

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Antimetabolites; Anticholesteremic Agents; Hypolipidemic Agents; Lipid Regulating Agents; Ezetimibe
• Other Study ID Numbers: OBEZ-103

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No