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Evaluation of the Safety, Tolerability and Pharmacokinetics of Repeat Oral Doses of GSK580416

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT00680485
Recruitment Status : Terminated
First Posted : May 20, 2008
Last Update Posted : January 20, 2017
Information provided by (Responsible Party):

Brief Summary:
This study will evaluate the safety, tolerability and exposure of repeat escalating oral doses, a loading dose/maintenance dose regimen of GSK580416 and when co administered with ketoconazole, a PGP/CYP3A4 inhibitor.

Condition or disease Intervention/treatment Phase
Bacterial Infection Infections, Bacterial Drug: GSK580416 oral tablets (250 mg) Ketoconazole oral tablets (200 mg) Phase 1

Detailed Description:
A three part study in healthy adult subjects to evaluate the safety, tolerability and pharmacokinetics of repeat escalating oral doses of GSK580416; the safety, tolerability, and pharmacokinetics of GSK580416 following a loading dose regimen; and the effect of ketoconazole on the pharmacokinetics of GSK580416

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Study Type : Interventional  (Clinical Trial)
Enrollment : 96 participants
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: A Three Part Study in Healthy Adult Subjects to Evaluate the Safety, Tolerability and Pharmacokinetics of Repeat Escalating Oral Doses of GSK580416; the Safety, Tolerability, and Pharmacokinetics of GSK580416 Following a Loading Dose Regimen; and the Effect of Ketoconazole on the Pharmacokinetics of GSK580416
Study Start Date : June 2007
Actual Primary Completion Date : October 2007
Actual Study Completion Date : October 2007

Resource links provided by the National Library of Medicine

Primary Outcome Measures :
  1. Safety and tolerability of GSK580416 doses determined from clinical safety and tolerability data from all adverse event reporting, 12-lead ECGs, vital signs, nursing/physician observation, and safety laboratory tests

Secondary Outcome Measures :
  1. Pharmacokinetics of GSK580416 as determined by AUC, Cmax, tmax, half-life, and Ct.

Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 64 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • Healthy adults (as determined by medical evaluation including history, physical exam, vital signs, laboratory tests, and cardiac monitoring)
  • Aged 18-60yrs, with BMI of 19-31kg/m2.
  • Females must be of non-childbearing potential.
  • QTc < 450 msec at screening.
  • Subjects must be able to give consent and comply with restrictions of study.

Exclusion Criteria:

  • Clinically significant CNS, cardiac, pulmonary, metabolic, renal, hepatic or GI condition or history that may place the subject at an unacceptable risk or may interfere with absorption, distribution, metabolism, or excretion of drug.
  • Positive urine drug screen.
  • Positive urine test for alcohol.
  • Positive HIV or Hep B and/or C assay.
  • History of regular tobacco use within 3 monts prior to screening or cotinine levels indicative of smoking at screening.
  • History of regular alcohol consumption (14 units/week for women and 21 units/week for men).
  • History of drug abuse or dependence within 12 months of study.
  • Participation in another drug trial within 30 days of first dose.
  • Exposure to more than 4 new chemical entities within 12 months of first dose.
  • Use of prescription and non-prescription drugs including vitamins, dietary supplements, herbals within 7 days of first dose or St. John's Wort within 28 days of the first dose.
  • Consumption of red wine, Seville oranges, grapefruit, or grapefruit juices within 14 days of first dose.
  • Donation of blood in excess of 500 mL within 56 days of dosing. No blood donation is allowed 30 days prior to study participation.
  • A positive immunochemical fecal occult blood test at screening.
  • History of sensitivity to any of the study medications.
  • History of sensitivity to heparin or heparin-induced thrombocytopenia.
  • History of orthostatic hypotension or orthostatic hypotension at screening.

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its identifier (NCT number): NCT00680485

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Australia, South Australia
GSK Investigational Site
Adelaide, South Australia, Australia, 5000
Sponsors and Collaborators
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Study Director: GSK Clinical Trials GlaxoSmithKline
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Responsible Party: GlaxoSmithKline Identifier: NCT00680485    
Other Study ID Numbers: OPS108221
First Posted: May 20, 2008    Key Record Dates
Last Update Posted: January 20, 2017
Last Verified: January 2017
Keywords provided by GlaxoSmithKline:
ketoconazole interaction
oral dose
Additional relevant MeSH terms:
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Communicable Diseases
Bacterial Infections
Antifungal Agents
Anti-Infective Agents
14-alpha Demethylase Inhibitors
Cytochrome P-450 Enzyme Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Steroid Synthesis Inhibitors
Hormone Antagonists
Hormones, Hormone Substitutes, and Hormone Antagonists
Physiological Effects of Drugs
Cytochrome P-450 CYP3A Inhibitors