Pharmacokinetics of AUX-001 40mg Once-daily in Healthy Subjects Under Fasting and Fed Conditions

NCT06249581 | Active Not Recruiting Early Phase 1 DMC

• 1 other identifier: 2023-506085-31-00
• Study Type: interventional
• Target: 16
• Locations: 1 country
• Sites: 1

Brief Summary

Exploratory, single-dose, open-label, pharmacokinetic study to establish uptake, plasma levels safety and tolerability of orally administered AUX-001 on an empty stomach (i.e, fasting) as well as after a meal (i.e. fed) in healthy volunteers.

Conditions

Chronic Stable Angina

Keywords

Pharmacokinetics; Bioavailability; Safety; Tolerability; Fasting; Fed

Outcome Measures

Primary Outcomes (6)

• Area under the curve over 24 hours [AUC0-24h)] of nicorandil under fasting conditions

  Total nicorandil plasma concentration over 24 hours under fasting conditions

  24 hours

• Area under the curve over 24 hours [AUC0-24h)] of nicorandil under fed conditions

  Total nicorandil plasma concentration over 24 hours under fed conditions

  24 hours

• Maximum Plasma Concentration [Cmax] of nicorandil under fasting conditions

  Peak plasma concentration under fasting conditions in mcg/ml

  24 hours

• Maximum Plasma Concentration [Cmax] of nicorandil under fed conditions

  Peak plasma concentration under fed conditions in mcg/ml

  24 hours

• 24 hour Area Under the Curve [AUC0-24h] of N-(2-hydroxyethyl) nicotinamide under fasting conditions

  24 hour Total Plasma Concentration of nicorandil's main metabolite under fasting conditions

  24 hours

• 24h hour Area Under the Curve [AUC0-24h] of N-(2-hydroxyethyl) nicotinamide under fed conditions

  Total Plasma Concentration of nicorandil's main metabolite under fed conditions

  24 hours

Secondary Outcomes (2)

• Treatment-emergent adverse events [TEAE] under fasting conditions

  24 hours

• Treatment-emergent adverse events [TEAE] under fed conditions

  24 hours

Study Arms (2)

Arm A: fasting

EXPERIMENTAL

AUX-001 40mg QD

Drug: AUX-001 40mg once-daily

Arm B: fed

EXPERIMENTAL

AUX-001 40mg QD

Drug: AUX-001 40mg once-daily

Interventions

AUX-001 40mg once-daily DRUG

AUX-001 (extended-release nicorandil) 40mg QD (once-daily)

Also known as: Food effect

Arm A: fasting; Arm B: fed

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Free written informed consent signed and dated prior to any procedure required by the study.
• Male or female subject between 18 and 55years, inclusive, at the time of signing the informed consent.
• Body mass index (BMI) of 18.0 to 31.0 kg/m2, inclusive.
• 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 EKG.
• No clinically relevant abnormalities on laboratory tests.
• Neg. test results on anti-HIV-1Ab and anti-HIV-2Ab, HbsAG and anti-HCVAb
• Non-smoker or ex-smoker
• Willingness to accept and comply with all study procedures and restrictions.
• Female subject of a) non-child-bearing potential or b) of childbearing potential and agrees to use an accepted, highly effective contraceptive method until the end of the study.

You may not qualify if:

• Known hypersensitivity/allergy reaction to the study drug substance or any of the excipients.
• Known severe hypersensitivity reaction to any other drug.
• Any medical condition (e.g., gastrointestinal, renal or hepatic, including peptic ulcer, inflammatory bowel disease or pancreatitis) or surgical condition (e.g., cholecystectomy, gastrectomy) that may affect drug pharmacokinetics (absorption, distribution, metabolism or excretion) or subject's safety.
• History of glucose-6-phosphate dehydrogenase deficiency.
• History of severe hypotension or shock.
• History of acute pulmonary edema, heart failure, coronary artery disease or myocardial infarction.
• History of orthostatic hypotension, collapse, fainting, syncope, or vasovagal reaction.
• History of substance or alcohol abuse within the previous 2 years.
• Use of contact lenses.
• SBP \<95 mmHg and/or DBP \<45 mmHg.
• Serum transaminases alanine aminotransferase (ALT) or aspartate aminotransferase (AST) above the upper limit of the normal range.
• Estimated renal creatinine clearance (CLCr) below 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 m2.
• Positive result in drugs-of-abuse or ethanol tests.
• Use of a depot injection or an implant of any drug (except for contraceptives) within the previous 6 months.
• Average weekly alcohol consumption of \>14 units for males and \>7 units for females within the previous 6 months.

Sponsors & Collaborators

• Auxilius Pharma sp.z.o.o.: lead

Study Sites (1)

BlueClinical

Porto, 4250-449, Portugal

Location

MeSH Terms

Conditions

Angina, Stable; Fasting; Lecithin Cholesterol Acyltransferase Deficiency

Condition Hierarchy (Ancestors)

Angina Pectoris; Myocardial Ischemia; Heart Diseases; Cardiovascular Diseases; Vascular Diseases; Chest Pain; Pain; Neurologic Manifestations; Signs and Symptoms; Pathological Conditions, Signs and Symptoms; Feeding Behavior; Behavior; Hypoalphalipoproteinemias; Hypolipoproteinemias; Lipid Metabolism, Inborn Errors; Metabolism, Inborn Errors; Genetic Diseases, Inborn; Congenital, Hereditary, and Neonatal Diseases and Abnormalities; Dyslipidemias; Lipid Metabolism Disorders; Metabolic Diseases; Nutritional and Metabolic Diseases

Study Officials

• Marlene Fonseca, MD

  Blueclinical, Ltd.

  PRINCIPAL INVESTIGATOR

• Uwe P Tigör, MD

  Auxilius Pharma

  STUDY DIRECTOR

Study Design

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

Model Details: Single-dose clinical trial with healthy volunteers sequentially using a single dose of AUX-001 under fasting and thereafter under fed conditions

Study Record Dates

• First Submitted: December 20, 2023
• First Posted: February 8, 2024
• Study Start: November 27, 2023
• Primary Completion: February 8, 2024
• Study Completion: February 10, 2024
• Last Updated: February 12, 2024

Record last verified: 2024-02

Data Sharing

• IPD Sharing: Will not share

Locations

PT (1)