NCT02202187

A Single Oral Escalating Dose Study of GSK2140944 in Healthy Volunteers

A Randomized, Single Blind, Placebo Controlled Study to Evaluate Safety, Tolerability, and Pharmacokinetics of Single Escalating Oral Doses of GSK2140944 in Healthy Adult Subjects

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 48 (actual)
• Sponsor: GlaxoSmithKline · Industry
• Sex: All
• Age: 18 Years – 60 Years
• Healthy volunteers: Accepted

Summary

GSK2140944 belongs to the Bacterial Type II Topoisomerase Inhibitor (BTI) class of antibiotics. GSK2140944 has demonstrated in vitro and in vivo activity against Gram positive including methicillin resistant Staphylococcus aureus (MRSA) and Gram-negative pathogens associated with respiratory tract, skin and soft tissue infections including isolates resistant to existing classes of antimicrobials. This is a First Time in Human (FTIH) study to assess the safety, tolerability, and pharmacokinetics of single oral doses of GSK2140944 in healthy volunteers. This study will be a single-blind, randomized, placebo-controlled, dose-rising study in healthy subjects. The proposed single doses will range from 100 mg to 3000 mg.

Detailed description

GSK2140944 belongs to the Bacterial Type II Topoisomerase Inhibitor (BTI) class of antibiotics which is being developed for treatment of Gram positive \[including methicillin resistant Staphylococcus aureus (MRSA)\] and Gram-negative pathogens associated with respiratory tract and skin and soft tissue infections including isolates resistant to existing classes of antimicrobials. Study BTZ114595 will be the first administration of GSK2140944 in humans. This study will examine the safety, tolerability, and pharmacokinetics of escalating single oral doses of GSK2140944. The predicted clinical target for efficacy, based on preclinical efficacy models, is an AUC(0-24) of 16-30 μg.h/mL. This study aims to explore the safety and tolerability at and above target exposures in order to establish a therapeutic window for this compound. This study will investigate the safety, tolerability, and pharmacokinetics of escalating single oral doses of GSK2140944. This will be a randomized, placebo-controlled, single-blind study to determine safety, tolerability, and single dose pharmacokinetic (PK) profile of GSK2140944 in healthy subjects. The projected single escalating doses of GSK2140944 will range from a starting dose of 100 mg to a maximum dose of 3000 mg. The current plan is to administer the study drug after an overnight fast, but based on emerging PK and safety data, it may be necessary to administer the study drug under fed state to better understand safety, tolerability or PK of GSK2140944. Any decision to remove or modify fasting requirements will be made by the GSK Study Team and the investigator based on joint review of the emerging safety, tolerability and preliminary pharmacokinetic data from prior dose-levels.

Conditions

• Infections, Respiratory Tract

Interventions

Type	Name	Description
DRUG	GSK2140944	Investigational Study Drug
OTHER	Placebo	Placebo

Timeline

• Start date: 2011-09-26
• Primary completion: 2012-02-15
• Completion: 2012-02-15
• First posted: 2014-07-28
• Last updated: 2017-06-12

Locations

1 site across 1 country: United States