Study Of Pharmacokinetics and Pharmacodynamics Effects Of GSK256073A On Healthy Volunteers

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: NCT00488449
Recruitment Status : Completed
First Posted : June 20, 2007
Last Update Posted : June 4, 2012
Information provided by (Responsible Party):

Brief Summary:
The purpose of this study is to compare the effects of single and repeat doses of GSK256073 with placebo in HVT subjects.

Condition or disease Intervention/treatment Phase
Healthy Subjects Dyslipidaemias Drug: GSK256073A tablets Phase 1

Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 56 participants
Allocation: Randomized
Intervention Model: Parallel Assignment
Masking: Single
Primary Purpose: Diagnostic
Official Title: A Two-Part Study to Evaluate Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single and Repeat Oral Doses of GSK256073A, in a Randomized, Single-Blind, Dose Escalation Study in Healthy Adult Subjects
Study Start Date : June 2007
Actual Primary Completion Date : November 2007
Actual Study Completion Date : November 2007

Primary Outcome Measures :
  1. AEs, 12-Lead ECG, vital signs, nursing/physician observation, safety lab tests, flushing [ Time Frame: throughout the study (Parts A &B) ]
  2. AUC and Cmax [ Time Frame: throughout the study (Part A & B) ]
  3. Measures of accumulation ratios [ Time Frame: throughout the study (Ro, Rp, and Rs)[Part B] ]

Secondary Outcome Measures :
  1. Tmax, t½, Ae, and CLr (Parts A & B) Cmax, ss, Ct, t½, Ae, CLr, and accumulation ratios (Part B) [ Time Frame: throughout the study ]
  2. PD response: NEFA and TG (6 and 24 hours post- dose) [ Time Frame: (6 and 24 hours post- dose) ]
  3. LDL, HDL, ApoA1, ApoA2, Apo B and Lp(a) [ Time Frame: on Days 1, 14, and 15. ]
  4. Levels of GSK256073 to derive pharmacokinetic parameters following repeat dose administration.
  5. Lipid levels [ Time Frame: on Days 1, 14, and 15 ]

Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 55 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes

Inclusion criteria:

  • Healthy Adult males or females between 18 and 55 years of age, inclusive.
  • Female subjects must be of non-childbearing potential
  • Body weight > 50 kg (110 pounds) and body mass index (BMI) 19 and 31 where:
  • Subjects with QTc < 450 msec at screening (or QTc < 480 msec for subjects with Bundle Branch Block).
  • A signed and dated written informed consent prior to admission to the study.
  • The subject is able to understand and comply with protocol requirements, instructions and protocol-stated restriction

Exclusion criteria:

  • Systolic blood pressure < 100 mmHg or 150 mmHg and/or diastolic blood pressure = 100 mmHg at screening.
  • History of significant cardiac arrhythmias
  • Active peptic ulcer disease (PUD) and/or history of PUD within 1 year.
  • A serum uric acid concentration 8mg/dL
  • Screening test positive for H. Pylori using the non-radioactive breath test
  • History of gout and/or hyperuricemia
  • History of Gilbert's syndrome
  • A serum creatinine concentration above the normal reference range
  • History of kidney stones
  • PT and/or aPTT above the reference range
  • History of recurrent indigestion, stomach upset or diarrhea
  • Liver function tests (LFTs) or creatinine phosphokinase (CPK) 1.5X ULN
  • Screening stool test positive for occult blood
  • Screening peripheral blood smear with abnormal RBCs
  • CBC, MCV, and/or reticulocyte count corrected for haemoglobin level above the reference range at screening
  • Reduced G6PD activity
  • Serum haptoglobin outside the reference range at screening
  • Total serum LDH > 1.25% above the ULN at screening
  • Positive HIV, Hepatitis B or Hepatitis C at screening
  • The subject has a positive pre-study urine drug/ serum alcohol screen.
  • History of alcohol consumption exceeding, on average, 7 drinks/week for women or 14 drinks/week for men within 6 months of the first dose of study medication or a positive alcohol test at screening
  • History of use of tobacco or nicotine containing products within 6 months of screening or a positive urine cotinine screen
  • Use of prescription (including hormone replacement therapy) or non-prescription drugs and vitamins within 7 days or 5 half-lives prior to administration of study medication. An exception is acetaminophen which is allowed at doses of 2g/day.
  • Use of dietary/herbal supplements within 14 days prior to treatment with study medication
  • Treatment with an investigational drug within 30 days or 5 half-lives (whichever is longer) prior to dosing.
  • Exposure to more than four new chemical entities within 12 months prior to the first dosing day.
  • History of sensitivity to any of the study medications, or components thereof or a history of drug or other allergy that, in the opinion of the physician responsible, contraindicates their participation.
  • Where participation in study would result in donation of blood in excess of 500 mL within a 56 day period.
  • Unwillingness of male subjects to use a condom/spermicide
  • Pregnant or nursing women.
  • History of flushing (>1 episode annually).
  • Fasting blood glucose 110 mg/dl and/or history of type I or type II DM
  • History of intra-ocular pathology
  • History of recurrent gum bleeding
  • History of bleeding haemorrhoids

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): NCT00488449

United States, Maryland
GSK Investigational Site
Baltimore, Maryland, United States, 21225
Sponsors and Collaborators
Study Director: GSK Clinical Trials GlaxoSmithKline

Responsible Party: GlaxoSmithKline Identifier: NCT00488449     History of Changes
Other Study ID Numbers: HMA110015
First Posted: June 20, 2007    Key Record Dates
Last Update Posted: June 4, 2012
Last Verified: February 2011

Keywords provided by GlaxoSmithKline:
Dose Escalation

Additional relevant MeSH terms:
Lipid Metabolism Disorders
Metabolic Diseases