A Pharmacokinetic and Bioavailability Study of 28431754 (Canagliflozin) in Healthy Male Volunteers
The purpose of this study is to evaluate the absolute oral bioavailability (how fast and how much study drug is absorbed in the body) of a single 300-mg oral dose of canagliflozin in healthy male volunteers.
|Study Design:||Endpoint Classification: Bio-availability Study
Intervention Model: Single Group Assignment
Masking: Open Label
|Official Title:||An Open-Label, Single-Dose Study to Assess the Absolute Oral Bioavailability and Pharmacokinetics of JNJ-28431754 (Canagliflozin) Administered as a 300-mg Oral Tablet and an Intravenous Microdose of 10 Mcg 14C-canagliflozin in Healthy Male Subjects|
- Protocol-specified pharmacokinetic parameters from blood samples to assess the absolute bioavailabilty of a 300-mg oral dose of canagliflozin [ Time Frame: Predose on Day 1 up to 72 hours postdose ] [ Designated as safety issue: No ]
- Protocol-specified pharmacokinetic parameters from blood samples to evaluate the pharmacokinetics of a single 300-mg oral dose of canagliflozin administered with a single 10-mcg intravenous dose of 14C canagliflozin [ Time Frame: Predose on Day 1 up to 72 hours postdose ] [ Designated as safety issue: No ]
- Measurement of 14C radioactivity from total urine and feces output to evaluate the extent of biliary excretion of a single 10-mcg intravenous dose of 14C canagliflozin [ Time Frame: Day 1 through 72 hours after initiation of the intravenous infusion ] [ Designated as safety issue: No ]
- The number and type of adverse events reported [ Time Frame: Time of screening up to 5 to 7 days after completion of all study related procedures on Day 4 ] [ Designated as safety issue: No ]
|Study Start Date:||May 2010|
|Study Completion Date:||June 2010|
Canagliflozin On Day 1 all patients will receive a single 300-mg tablet of canagliflozin with 8 ounces of water followed 105 minutes later by a 15-minute intravenous infusion dose (15 mL) of 10 mcg of 14C-canagliflozin (200 nCi).
On Day 1, all patients will receive a single 300-mg tablet of canagliflozin with 8 ounces of water followed 105 minutes later by a 15-minute intravenous infusion dose (15 mL) of 10 mcg of 14C-canagliflozin (200 nCi).
This is an open-label (the patient will know the identity of the treatment they receive), single-dose, single-center study to evaluate the absolute oral bioavailability (the rate and extent at which the drug is absorbed in the body and reaches blood circulation) of a 300-mg tablet of canagliflozin. Approximately 9 healthy men (referred to as healthy male volunteers) will receive a single 300-mg tablet of canagliflozin with an 8 ounce glass of water followed 105 minutes later by a 15 minute intravenous (iv) infusion (administration directly in the vein) of a very small dose (ie, 10 micrograms [mcg]) of canagliflozin that has been combined with a radioactive carbon isotope referred to as 14C canagliflozin. The radiolabelled 10 mcg dose of canagliflozin will act as a tracer to measure the total amount of canagliflozin that is absorbed and metabolized in the body. After dosing, blood, urine and feces samples will be collected for pharmacokinetic and safety evaluations at specified timepoints for up to 72 hours. The primary outcome measure in the study is to determine the absolute bioavailability of a single 300 mg dose of canagliflozin by estimation of protocol-specified standard plasma pharmacokinetic parameters (parameters that measure the absorption, distribution, metabolism, and elimination of drug by the body) from blood samples obtained during the study. During the study, the safety of a single oral 300-mg dose of canagliflozin administered together with a single iv 10-mcg infusion dose of 14C-canagliflozin will be evaluated by monitoring adverse events and findings from clinical laboratory test values, physical examination results, 12 lead ECGs and vital signs measurements reported. On Day 1, each healthy volunteer will take a single 300-mg canagliflozin tablet orally (by mouth) with 8 ounces of water in the morning followed by a 15-minute intravenous infusion of 10 mcg 14C-canagliflozin (200 nCi) (equivalent to 0.666 mcg/mL of canagliflozin). Healthy volunteers will fast at least 10 hours before dosing and until at least 4 hours after oral administration and will not be allowed to drink water from 2 hours before and up to 4 hours after study drug administration.
|Study Director:||Johnson & Johnson Pharmaceutical Research & Development, L.L. C. Clinical Trial||Johnson & Johnson Pharmaceutical Research & Development, L.L.C.|