A Phase I, Single-Centre, Open, Randomized, Two-Way Crossover Study to Evaluate the Pharmacokinetics of the Extended-Release Test Formulation of AZD0837 Compared to the Extended-Release AZD0837 Reference Formulation After Repeated Dosing in Healthy Volunteers
Overview
- Phase
- Phase 1
- Intervention
- AZD0837
- Conditions
- Healthy
- Sponsor
- AstraZeneca
- Enrollment
- 36
- Locations
- 1
- Primary Endpoint
- To evaluate the pharmacokinetics of AZD0837 and the active metabolite AR-H067637XX for the extended-release test formulation of AZD0837 compared to the ER reference formulation.
- Status
- Completed
- Last Updated
- 16 years ago
Overview
Brief Summary
The aims of this study are to evaluate the pharmacokinetics, safety and tolerability of the oral doses of the extended-release test- and reference formulations of AZD0837 in healthy volunteers both in fasting and fed conditions.
Investigators
Eligibility Criteria
Inclusion Criteria
- •Healthy subject aged between 18 to 45 years inclusive
- •Body mass index (BMI) between 19 to 30 kg/m2 inclusive
- •Body weight between 50 to 100 kg inclusive
- •Women must be either post-menopausal, permanently sterilised or, if of childbearing potential, must have a negative pregnancy test before intake of study medication and use a reliable form of contraception before and during participation in the study.
Exclusion Criteria
- •Significant illness (including ongoing or history of liver disease), trauma or surgical procedures from 2 weeks before the pre-entry visit until the first administration of Investigational Product
- •Clinical significant abnormalities in clinical chemistry, haematology or urinalysis result including positive result on screening tests for serum hepatitis B surface antigen, hepatitis C antibody or HIV or positive F-Hb result pre-entry
- •History of bleeding disturbance (including extensive menstrual bleedings) or thrombotic disorder
- •Clinically significant medical history, as judged by the investigator, including psychiatric disorders or severe allergies.
Arms & Interventions
HAB
AZD0837 test- (in session 1) and reference- (in session 2) formulation with heavy breakfast
Intervention: AZD0837
HBA
AZD0837 reference- (in session 1) and test- (in session 2) formulation with heavy breakfast
Intervention: AZD0837
LAB
AZD0837 test- (in session 1) and reference- (in session 2) formulation with light breakfast
Intervention: AZD0837
LBA
AZD0837 reference- (in session 1) and test- (in session 2) formulation with light breakfast
Intervention: AZD0837
Outcomes
Primary Outcomes
To evaluate the pharmacokinetics of AZD0837 and the active metabolite AR-H067637XX for the extended-release test formulation of AZD0837 compared to the ER reference formulation.
Time Frame: Intense PK-sampling during 5 pre- defined study days for PK profiling. In 2 of the study days the subjects will have a breakfast before intake of the Investigational Product.
Secondary Outcomes
- To evaluate the PK of the intermediate metabolite AR-H069927XX(Since the metbolite will be evaluated from the AZD0837-samples the time frame is the same as above.)
- Safety variables (ECG, pulse, blood pressure, safety lab, physical examination, adverse events)(ECG & physical examination at start and end of study. Pulse and blood pressure predose day 1 and every day 2 h post dose. Adverse events collected during the whole study. Safety lab at a few timepoints but APTT will be checked on 4 h post dose on day 1.)
- Measurement of plasma concentrations of 4 beta-hydroxycholesterol to investigate whether AZD0837 affects the level of CYP3A4(Once predose on day 1, session 1 and once predose on day 5, session 2)