Intravenous Microdose Pharmacokinetic (PK) Study With [14C]-GSK2239633

• Register: ClinicalTrials.gov
• Last refreshed on: 16 December 2017
• Main ID: NCT01086462
• Date of registration: 18/02/2010
• Prospective Registration: No
• Primary sponsor: GlaxoSmithKline
• Public title: Intravenous Microdose Pharmacokinetic (PK) Study With [14C]-GSK2239633
• Scientific title: A Microdose Study to Describe the Intravenous Pharmacokinetics of [14C]-GSK2239633 in Healthy Male Subjects
• Date of first enrolment: January 21, 2010
• Target sample size: 6
• Recruitment status: Completed
• URL: https://clinicaltrials.gov/show/NCT01086462
• Study type: Interventional
• Study design: Intervention model: Single Group Assignment. Primary purpose: Other. Masking: None (Open Label).
• Phase: Phase 1

Countries of recruitment

Netherlands

Contacts

• Name: GSK Clinical Trials
• Affiliation: GlaxoSmithKline

Key inclusion & exclusion criteria

Inclusion Criteria:

- Healthy subjects are defined as individuals who in the opinion of the Investigator are
free from clinically significant cardiac, pulmonary, gastrointestinal, hepatic, renal,
haematological, endocrine, neurological and psychiatric disease or malignancy as
determined by medical history, physical examination, laboratory studies, and other
tests (including ECG). Subjects with values outside the normal range which are deemed
to be clinically relevant should always be excluded from enrollment.

- Male between 18 and 50 years of age inclusive, at the time of signing the informed
consent.

- Subject must agree to use one of the contraception methods listed in Section 8.1. of
the protocol. This criterion must be followed from the time of screening until 90 days
after the follow up

- Body weight >or= 50 kg and BMI within range 18.5-29.9 kg/m2 (inclusive).

- Capable of giving written informed consent, which includes compliance with the
requirements and restrictions listed in the consent form

- Single QTcF <450 msec; or QTcF <480 msec in subjects with Bundle Branch Block

- Lifelong non-smokers or ex-smokers of greater than 6 months and <5 pack year history.
Pack years = (cigarettes per day smoked/20) x number of years smoked.

- AST, ALT, alkaline phosphatase and bilirubin 1.5 x
ULN acceptable if bilirubin is fractionated and direct bilirubin <35%)

Exclusion Criteria:

- A positive pre-study Hepatitis B surface antigen or positive Hepatitis C antibody
within 3 months of screening

- Current or chronic history of liver disease, or known hepatic or biliary abnormalities

- A positive pre-study drug/alcohol screen

- A positive test for HIV antibody

- History of regular alcohol consumption within 6 months of study defined as an average
weekly intake of >12 units/week for males. One unit is equivalent to 8g of alcohol; a
half-pint (~250ml) of beer, 1 glass (100ml) of wine or 1 (35 ml) measure of spirits.

- Urinary cotinine levels indicative of smoking or history or regular use of tobacco- or
nicotine-containing products (including snuff, nicotine-containing gum) within 6
months prior to screening

- The subject has participated in a clinical trial and has received an investigational
product within the following time period prior to first dosing: 60 days, 5 half-lives
or twice the duration of the biological effect of investigational product (whichever
is longer)

- Exposure to more than four new chemical entities within 12 months prior to the first
dosing day

- Participation in a clinical trial involving administration of 14C-labelled compounds
within last 12 months

- Use of prescription or non-prescription drugs, including vitamins, herbal and dietary
supplements (including St John's Wort) within 14 days or 5 half-lives prior to the
first dose of study medication, unless in the opinion of the Investigator and Medical
Monitor the medication will not interfere with study procedures or compromise subject
safety.

- History of sensitivity to any of the study medications, or components thereof or a
history of drug or other allergy that, in the opinion of the investigator or GSK
Medical Monitor, contraindicates their participation

- Where participation in the study would result in donation of blood or blood products
in excess of 500 mL within a 56 day period

- Unwillingness or inability to follow procedures outlined in the protocol

- Subject is mentally or legally incapacitated

- A calculated creatinine clearance (Cockroft and Gault formula) of <90 mL/min

- History of sensitivity to heparin or heparin-induced thrombocytopenia

- Consumption of red wine, seville oranges, grapefruit or grapefruit juice from 7 days
prior to the first dose of study medication



Age minimum: 18 Years
Age maximum: 50 Years
Gender: Male

Health Condition(s) or Problem(s) studied

Asthma

Intervention(s)

Drug: GSK2239633

Primary Outcome(s)

Pharmacokinetics (AUC0-inf, Cmax, AUC0-t, t1/2, clearance, volume of distribution) of [14C]-GSK2239633 and total drug-related material [Time Frame: 48 hours]

Secondary ID(s)

114041

Source(s) of Monetary Support

Please refer to primary and secondary sponsors