Official Title: “A Randomized, Blinded, Placebo-Controlled Study to Investigate the Safety, and Pharmacokinetics of Single and Repeat Dose Escalation of the Oral YAK3/DYRK3 Inhibitor GSK626616AC in Healthy Subjects”

This is a first time in human study to investigate the safety of GSK626616AC given as oral single and repeat doses in healthy subjects. An additional group of subjects will be assessed to determine the effect of several drugs given at the same time as GSK626616.

Study Type: Interventional

Study Design: Treatment, Randomized, Single Blind, Placebo Control, Single Group Assignment, Safety Study

Primary:

• adverse events at end of each cohort end of each cohort
• hematology/chemistry/urinalysis at end of each cohort end of each cohort
• physical examination at end of each cohort end of each cohort
• vital signs and electrocardiogram (ECG) at end of each cohort end of each cohort

Secondary:

• GSK626616 pharmacokinetics at end of each cohort end of each cohort
• hemoglobin at end of each cohort end of each cohort
• red blood cell measurements at end of each cohort end of each cohort
• estimates of CYP enzyme activity at end of study end of study
• mRNA levels in peripheral blood at end of study end of study

Inclusion Criteria:

• Age 18 to 55 years healthy subjects
• Hemoglobin values of 13.5-17.0 g/dL for males or 12.0-15.5 g/dL for females.
• Females cannot be pregnant.

Exclusion Criteria:

• Cannot have exposure to greater than 4 new chemical entities within 12 months.
• Cannot have a clinical history of current alcohol, or illicit drug use which, in the judgment of the Investigator, would interfere with the subject's ability to comply with the dosing schedule.
• Cannot have a history of regular use of tobacco- or nicotine-containing products within 3 months.
• Must not have received a blood transfusion or had a donation of blood within 3 months prior to study entry.
• Cannot use be taking prescription, non-prescription or illicit drugs.

Lead Sponsor: GlaxoSmithKline

GSK Clinical Trials Call Center

Adelaide  5000 Australia

GSK Clinical Trials Call Center

Randwick  2031 Australia

GSK Clinical Trials Call Center

Brisbane  4028 Australia

Overall Clinical Trial Officials and Contacts

GSK Clinical Trials, MD Study Director GlaxoSmithKline  

Information obtained from ClinicalTrials.gov on July 23, 2008

Link to the current ClinicalTrials.gov record. http://clinicaltrials.gov/show/NCT00443170

Study ID Number: YAK106752

ClinicalTrials.gov Identifier: NCT00443170

Health Authority: Australia: Department of Health and Ageing Therapeutic Goods Administration