A Study to Investigate the Recovery, Excretion, and Pharmacokinetics of 14C -GSK1322322 After an Intravenous and an Oral Dose

NCT01663389 | Completed Phase 1

• 1 other identifier: 112167
• Study Type: interventional
• Target: 5
• Locations: 1 country
• Sites: 1

Brief Summary

This is a phase 1, non-randomized, open label, single-dose, two-period, cross-over study. This study will utilize 14C radiolabeled GSK1322322 to investigate the recovery, excretion, and pharmacokinetics of GSK1322322 in 6 healthy adult male subjects through the sampling of blood, urine, and feces. Each subject will participate in the study for approximately 7 to 8 weeks i.e., 30 day screening period, two dosing periods (approximately 8 days each) and a follow up visit. The subjects will be admitted to the clinical unit on Day 1 of the first treatment period and remain in the unit for up to approximately 16 days through the end of the second treatment period. On Day 1 of Period 1, each subject will receive 14C radiolabeled GSK1322322 as a single therapeutic intravenous (IV) dose (1000 milligrams \[mg\]). When the total radioactivity is \<1% of the administered dose in all subjects, Period 2 dosing will begin (approximately 8 days after the IV dose). On Day 1 of Period 2, each subject will receive single therapeutic oral solution dose (1200 mg). Blood, urine, bile and fecal samples will be collected during both the periods. The subject may be discharged from the unit as early as Day 8 of Period 2. Subjects will visit the study unit for the follow-up visit 7 to 10 days following discharge from the unit.

Conditions

Infections, Bacterial

Keywords

mass balance; radiolabel; oral; IV; GSK1322322; healthy volunteer; antibiotic

Outcome Measures

Primary Outcomes (2)

• Plasma pharmacokinetic (PK) parameters of GSK1322322 and radiolabeled compound following single IV or oral solution dose: AUC(0-infinity), AUC(0-t), Cmax, tmax, t1/2 for IV and oral solution regimens and CL and Vss for IV regimen only

  Plasma PK parameters will be statistically summarized by treatment. Plasma concentration-time data will be analyzed by non-compartmental methods. Following PK parameters will be studied: Area under the concentration-time curve (AUC) from time zero (pre-dose) extrapolated to infinite time \[AUC(0-infinity)\], AUC(0-t), maximum observed concentration (Cmax), time of occurrence of Cmax (tmax), terminal phase half-life (t1/2) for IV and oral solution regimens and systemic clearance (CL) and volume of distribution (Vss) for IV regimen only.

  Day 1 through Day 8 of Period 1 and Period 2 (16 days)

• Percent total recovery of radioactivity in urine and feces in each interval and cumulative

  Total recovery of radioactivity in urine and feces (as a percentage of total radioactive dose in each interval and cumulative)

  Day 1 through Day 8 (and additional days, if required) of Period 1 and Period 2 (16 days or more)

Secondary Outcomes (1)

• Safety parameters including adverse events, clinical laboratory tests, concomitant medications, electrocardiograms, and vital signs

  Duration of the study (56 days)

Study Arms (2)

GSK1322322 1000 mg IV

EXPERIMENTAL

On Day 1 of Period 1, after an overnight fast, subjects will receive GSK1322322 1000 mg IV single dose (containing approximately 45.5 microcurie \[μCi\] radioactive 14C-GSK1322322) for intravenous infusion over 60 minutes.

Drug: GSK1322322 1000 mg containing radioactive 14C-GSK1322322

GSK1322322 1200 mg Oral Solution

EXPERIMENTAL

On Day 1 of Period 2, after an overnight fast, subjects will receive GSK1322322 1200 mg oral solution single dose (containing approximately 54.5 μCi radioactive 14C-GSK1322322).

Drug: GSK1322322 1200 mg containing radioactive 14C-GSK1322322

Interventions

GSK1322322 1000 mg containing radioactive 14C-GSK1322322 DRUG

GSK1322322 1000 mg is a mesylate salt powder for injection containing 45.5 μCi radioactive 14C-GSK1322322 1000 mg as free base.

GSK1322322 1000 mg IV

GSK1322322 1200 mg containing radioactive 14C-GSK1322322 DRUG

GSK1322322 1200 mg is a mesylate salt powder for oral solution containing 54.5 μCi radioactive 14C-GSK1322322 1200 mg as free base.

GSK1322322 1200 mg Oral Solution

Eligibility Criteria

• Age: 30 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy male subjects between 30 and 55 years of age, with body weight between 60 to 80 kilograms (kg) and a history of regular bowel movements
• Male subjects with female partners of child-bearing potential must agree to use one of the contraception methods from first dose of study medication until the final follow up visit
• Alanine aminotransferase (ALT), alkaline phosphatase and bilirubin =\<1.5x upper limit of normal
• QT interval by Bazett's correction formula (QTcB) \<450 millisecond (msec); or QTcB \<480 msec in subjects with Bundle Branch Block
• Available to complete the study and return for follow-up visits if necessary
• Capable of giving written informed consent

You may not qualify if:

• Any condition that could interfere with the accurate assessment and recovery of radioactivity \[14C\]
• Participation in a clinical trial involving administration of radiolabeled 14C-labelled compound(s) within the last 12 months
• Any condition which impairs the absorption, distribution, metabolism or excretion of the investigational product
• Subjects with a history of cholecystectomy
• Subject has received a total body radiation dose of greater than 5.0 millisievert (mSv) or exposure to significant radiation during 1 year before dosing
• The subject has a positive: drug/alcohol, Hepatitis, HIV screen
• Abuse of alcohol
• History of liver disease, or known hepatic or biliary abnormalities
• The subject has recently received an investigational product
• Donation of more than 500 mL blood within a 56 day period
• Unwillingness or inability to follow the procedures outlined in the protocol
• Use of prescription or non-prescription drugs
• Subject is mentally or legally incapacitated
• History of sensitivity to heparin or heparin-induced thrombocytopenia
• Smoking or history or regular use of tobacco or nicotine-containing products

Sponsors & Collaborators

• GlaxoSmithKline: lead

Study Sites (1)

GSK Investigational Site

Minneapolis, Minnesota, 55404, United States

Location

Related Links

• Results for study 112167 can be found on the GSK Clinical Study Register.
• Researchers can use this site to request access to anonymised patient level data and/or supporting documents from clinical studies to conduct further research.

MeSH Terms

Conditions

Bacterial Infections

Interventions

GSK1322322

Condition Hierarchy (Ancestors)

Bacterial Infections and Mycoses; Infections

Study Officials

• GSK Clinical Trials

  GlaxoSmithKline

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 19, 2012
• First Posted: August 13, 2012
• Study Start: August 10, 2012
• Primary Completion: October 5, 2012
• Study Completion: October 5, 2012
• Last Updated: June 12, 2017

Record last verified: 2017-06

Data Sharing

• IPD Sharing: Will share

Locations

US (1)