NCT01267071

A Study to Evaluate the Pharmacokinetics and Absolute Bioavailability of GSK962040 Given as an Oral Dose Simultaneously With an Intravenous Microtracer Dose of [14C]-GSK962040 in Healthy Volunteers

A Single Dose, Open Label, Nonrandomized, Study to Evaluate the Pharmacokinetics and Absolute Bioavailability of GSK962040 Given as an Oral Dose Simultaneously With an Intravenous Microtracer Dose of [14C]-GSK962040 in Healthy Volunteers

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 8 (actual)
• Sponsor: GlaxoSmithKline · Industry
• Sex: Male
• Age: 18 Years – 65 Years
• Healthy volunteers: Accepted

Summary

The purpose of this study is to determine the absolute oral bioavailability and intravenous pharmacokinetics of GSK962040. The oral dose of 50 mg has been selected because it was well tolerated following single oral administration and it is considered to be within therapeutic dose range. The need to characterize the intravenous disposition of GSK962040 is in anticipation of drug use in special populations such as critically.

Detailed description

GSK962040 is a selective non-peptide motilin receptor agonist which is being developed for the treatment of conditions associated with slow rates of gastric emptying. The purpose of this study is to determine the absolute bioavailability and the metabolic profile of GSK962040. Subjects will be administered a single oral dose of 50 mg followed by a single intravenous dose of 10 mL containing 100 microgram (not more than 270 nCi, 10 kBq) 14C GSK962040, administered by infusion over 15 minutes, beginning at 90 min after administration of the oral dose (approximate Cmax). The oral dose of 50 mg was well tolerated following single oral administration and is predicted to be a therapeutic dose. There is need to characterize GSK962040 disposition in anticipation of drug use in special populations such as critically ill patients. The intravenous (infused) microdose (100 microgram) is 500-fold lower than the oral dose, therefore exposure to GSK962040 originating from the infused microdose is considered negligible.

Conditions

• Gastroparesis

Interventions

Type	Name	Description
DRUG	A	GSK962040 (50 mg, SD, oral)
DRUG	B	14C GSK962040 (100 μg, SD, iv)

Timeline

• Start date: 2010-06-14
• Primary completion: 2010-09-01
• Completion: 2010-09-01
• First posted: 2010-12-24
• Last updated: 2017-06-09

Locations

1 site across 1 country: United Kingdom