Pharmacokinetics Study of Azelaprag (BGE-105) in Older Adult Healthy Volunteers

Study Overview
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Brief Summary
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This study is a single-dose, open-label, randomized crossover study to evaluate the PK of azelaprag in older adult healthy volunteers.

Detailed Description
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This study is a single-dose, open-label, randomized crossover study to evaluate the PK of azelaprag in older adult healthy volunteers. The study will enroll approximately 16 participants.

Official Title
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A Phase 1, Single-dose, Open-label, Randomized Crossover Study to Evaluate the Pharmacokinetics and Safety of Azelaprag in Older Adult Healthy Volunteers

Conditions
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Healthy Volunteer Study

Intervention / Treatment
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* Drug: Azelaprag


Participation Criteria
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Eligibility Criteria
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Key Inclusion Criteria: Patients who meet ALL the following inclusion criteria will be eligible to participate in the study: Healthy male or female volunteers ≥ 60 years of age No history or evidence of clinically relevant medical disorders Body mass index (BMI) between 18 and 40 kg/m2 Acceptable physical examination findings, including vital signs, and electrocardiogram (ECG) Acceptable clinical laboratory values Female participants of non-childbearing potential Key Exclusion Criteria: Currently receiving treatment with another investigational drug or investigational device within 30 days (or 5 half-lives, whichever is longer) Current or previous malignancy within 5 years, with the exception of non-melanoma skin cancers, cervical or breast ductal carcinoma in situ, or adenocarcinoma of the prostate Positive test result for COVID (rapid test), human immunodeficiency virus (HIV) antibodies, hepatitis B surface antigen (HBsAg), or hepatitis C (HCV) antibodies Use of any medications that might affect the metabolism of the study drug as assessed by the Investigator and Sponsor and use of any herbal supplements, vitamins, or nutritional supplements within the 14 days prior to the dose day of each dosing period or during study participation. Planned elective surgery within 30 days prior to Screening, during the study period or before the participant's red blood cell (RBC) have returned to normal levels Systolic blood pressure > 150 mm Hg or < 90 mm Hg or diastolic blood pressure > 95 mm Hg or < 60 mm Hg Unwilling or unable to abstain from the use of nicotine or tobacco containing products (including but not limited to snuff, chewing tobacco, cigars, cigarettes, pipes, or nicotine patches) or the use of cannabis or marijuana Positive urine drug screen or alcohol breath test at screening and/or known history of drug or alcohol abuse within 1 year prior to screening History or evidence of any other clinically significant disorder, condition, or disease, that, in the opinion of the investigator or Sponsor medical monitor, if consulted, would pose a risk to participant safety, or interfere with the study evaluation, procedures, or completion Concurrent or previous use of aspirin within 14 days and NSAIDs within 3 days before the dose day of each dosing period.

Ages Eligible for Study
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Minimum Age: 60 Years

Sexes Eligible for Study
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All

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

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


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: 4-way Crossover<br>Study Part 1: Participants will receive a single Dose A or B on Day 1 and then followed by a crossover to a single Dose B or A on Day 8. Optional Study Part 2: If Part 2 is required, participants may receive a single Dose C or D on Day 1 and then followed by a crossover a single dose D or C on Day 8. | Drug: Azelaprag<br>* oral, apelin receptor (APJ) agonist<br>* Other names: BGE-105;|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Pharmacokinetics of azelaprag (BGE-105) after oral administration - AUC0-t | Assessment of PK parameter, area under the curve (AUC) from time 0 to time of the last observed serum concentration (AUC0-t) | Predose and post dose to 144 hours after each dose received | 
| Pharmacokinetics of azelaprag (BGE-105) after oral administration - AUC0-inf | Assessment of PK parameter, UAC from time 0 to infinity (AUC0-inf) | Predose and post dose to 144 hours after each dose received | 
| Pharmacokinetics of azelaprag (BGE-105) after oral administration - Cmax | Assessment of PK parameter, maximum observed serum concentration (Cmax) | Predose and post dose to 144 hours after each dose received | 
| Pharmacokinetics of azelaprag (BGE-105) after oral administration - Tmax | Assessment of PK parameter, time to reach Cmax (Tmax) | Predose and post dose to 144 hours after each dose received | 
| Pharmacokinetics of azelaprag (BGE-105) after oral administration - T1/2 | Assessment of PK parameter, terminal elimination half-life (T1/2) | Predose and post dose to 144 hours after each dose received | 
| Oral bioavailability of azelaprag after oral administration - Total body clearance | Assessment of PK parameter, Total body clearance (CL) | Predose and post dose to 144 hours after each dose received | 
| Oral bioavailability of azelaprag after oral administration - Volume of distribution | Assessment of PK parameter, volume of distribution (Vz) | Predose and post dose to 144 hours after each dose received | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Safety of azelaprag after oral administration - TEAEs | Number of participants with treatment emergent adverse events (TEAEs) | First dose to Day 21 |