A Single Oral Escalating Dose Study of GSK2140944 in Healthy Volunteers
Condition: Infections, Respiratory Tract
MeSH terms: Respiratory Tract Infections
Study type: Interventional
Phase: Phase 1

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.
    

Intervention name(s): GSK2140944; Placebo
Intervention type(s): Drug; Other
Intervention description(s): Investigational Study Drug; Placebo
Intervention MeSH terms: Gepotidacin
Allocation: Randomized
Intervention model: Parallel Assignment
Masking: Single (Participant)
Primary purpose: Other