Pharmacokinetics of Extended-Release Test- and Reference Formulations of AZD0837

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: AZD0837

• Registration Number: NCT00878618
• Lead Sponsor: AstraZeneca

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.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2009-03-31
• Study Start: 2009-04
• Study First Submitted QC: 2009-04-08
• Study First Posted: 2009-04-09
• Study Completion: 2009-05
• Status Verified: 2009-06
• Last Update Submitted: 2009-06-02
• Last Update Posted: 2009-06-03

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 36

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.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
HAB	AZD0837	AZD0837 test- (in session 1) and reference- (in session 2) formulation with heavy breakfast
LAB	AZD0837	AZD0837 test- (in session 1) and reference- (in session 2) formulation with light breakfast
HBA	AZD0837	AZD0837 reference- (in session 1) and test- (in session 2) formulation with heavy breakfast
LBA	AZD0837	AZD0837 reference- (in session 1) and test- (in session 2) formulation with light breakfast

Primary Outcome Measures

Name	Time	Method
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.	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 Outcome Measures

Name	Time	Method
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

Trial Locations

Locations (1)

Research Site; 🇸🇪 Uppsala, Sweden