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A Phase I Rheumatoid Arthritis Study in Healthy Volunteers

Phase 1
Completed
Conditions
Arthritis, Rheumatoid
Interventions
Drug: Placebo
Registration Number
NCT00539760
Lead Sponsor
GlaxoSmithKline
Brief Summary

GSK182771 is a domain antibody targeting the interleukin (IL)-1 receptor which is being developed for the treatment of rheumatoid arthritis. This study is being done in healthy volunteers to verify the safety and tolerability of GSK182771

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
45
Inclusion Criteria
  • Healthy adult men or women as determined by a responsible physician, based on a medical evaluation including history, physical examination, laboratory tests and cardiac assessment.
  • Female subjects of non-childbearing potential.
  • Male subjects must agree to abstain from or agree to use adequate contraception, in addition to having their female partner use another form of contraception. This criterion must be followed from the time of the first dose of study medication until Pharmacokinetic levels are determined to be below the LLQ.
  • Men or women who are between 18 and 55 years of age, inclusive.
  • Body Mass Index (BMI) within the range of 18-35 kilogram per meter square (kg/m^2) inclusive.
  • Capable of giving written informed consent, which includes compliance with the requirements and restrictions listed in the consent form
Exclusion Criteria
  • The subject has a positive pre-study urine drug/urine alcohol screen. A minimum list of drugs that will be screened for includes amphetamines, barbiturates, cocaine, opiates, cannabinoids and benzodiazepines.
  • A history of regular alcohol consumption averaging >7 drinks/week for females or >14 drinks/week for males. One drink is equivalent to (12 g alcohol) = 5 ounces [150 milliliter (mL)] of wine or 12 ounces (360 mL) of beer or 1.5 ounces (45 mL) of 80 proof distilled spirits
  • The subject is unwilling to abstain from alcohol consumption from 48 hour prior to dosing until discharge from the clinic, and for 48 hour prior to all other out-patient clinic visits.
  • Smoked or used tobacco or nicotine-containing products within the previous 6 months prior to the first dose of current study medication.
  • The subject has participated in a clinical trial and has received a drug or a new chemical entity within 30 days or 5 half-lives, or twice the duration of the biological effect of any drug (whichever is longer) prior to the first dose of current study medication.
  • Previous exposure to or treatment with PEGylated molecules.
  • Use of anti-Tumor Necrosis Factor (anti-TNF) drugs within 60 days prior to dosing.
  • Use of prescription or non-prescription drugs, including vitamins, herbal and dietary supplements (including St John's Wort) within 7 days , or 5 half-lives (whichever is longer) prior to the first dose of study medication, unless in the opinion of the Investigator and GSK Medical Monitor the medication will not interfere with the study procedures or compromise subject safety.
  • History of sensitivity to any of the study medications, or components thereof, or a history of drug or other allergy (including antibiotics) which, in the opinion of the investigator and/or GSK Medical Monitor, contraindicates the subject's participation.
  • Positive pregnancy test at Screening or on Day -1 (females only).
  • Any clinically significant abnormality identified on the screening medical assessment or examination, or ECG.
  • Any white blood cell (WBC) or neutrophil count outside the normal range at screening or on Day -1.
  • History of significant cardiac, pulmonary, metabolic, renal, hepatic, or gastrointestinal conditions that in the opinion of the investigator and/or GSK Medical Monitor, places the subject at an unacceptable risk as participant in this trial.
  • History of any autoimmune or current inflammatory conditions including rheumatoid arthritis or any other joint disease.
  • History of malignancy, except for surgically cured basal cell carcinoma or cured cervical carcinoma (> 2 yrs prior to dosing).
  • Currently has asthma or history of chronic obstructive pulmonary disease (COPD).
  • Current evidence of ongoing or acute infection.
  • The subject has a history of repeated, chronic or opportunistic infections which, in the opinion of the investigator and/or GSK Medical Monitor, places the subject at an unacceptable risk as a participant in this trial.
  • History of Mycobacterium tuberculosis or any other previous Mycobacterium infection.
  • A positive pre-study Hepatitis B surface antigen, positive Hepatitis C antibody, or human immunodeficiency virus (HIV) antibody testing result.
  • History of a severe allergic reaction, angio-edema, anaphylaxis or immunodeficiency
  • History of elevated blood pressure or blood pressure >140/90 millimeters of mercury (mmHg) at screening.
  • Corrected QT interval (QTc) > 450 milliseconds.
  • Where participation in study would result in donation of blood in excess of 500 mL within 56 days of starting the study.
  • Subject whose calculated creatinine clearance is less than 80 mL/min
  • Liver function tests above the upper limit of normal at screening (alkaline transaminase (ALT), aspartate transaminase (AST) or bilirubin).
  • Chronic liver or biliary disease, history of Gilbert's syndrome in a previous clinical study or at screening.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Subjects receiving GSK 1827771 in sub-cohort Xa (Cohort 1-5)GSK1827771Eligible subjects will receive GSK1827771 with the starting dose of 0.3 milligram (mg)
Subjects receiving placebo in sub-cohort Xa (Cohort 1-5)PlaceboEligible subjects will receive placebo matching to GSK1827771
Subjects receiving GSK 1827771 in sub-cohort Xb (Cohort 1-5)GSK1827771Eligible subjects will receive GSK1827771 via injection
Subjects receiving placebo in sub-cohort Xb (Cohort 1-5)PlaceboEligible subjects will receive placebo matching to GSK1827771
Subjects receiving GSK 1827771 in sub-cohort Xc (Cohort 1-5)GSK1827771Eligible subjects will receive GSK1827771 via injection
Subjects receiving placebo in sub-cohort Xc (Cohort 1-5)PlaceboEligible subjects will receive placebo matching to GSK1827771
Primary Outcome Measures
NameTimeMethod
Number of subjects with abnormal urinalysis findingsUp to 29 days

Urine samples will be collected at specific time points as a measure of safety

Number of subjects with abnormal electrocardiogram (ECG) findingsUp to 29 days

12-lead ECG measurements will be performed in a supine position after at least 5 minutes of rest as a measure of safety

Number of subjects with abnormal blood pressure valuesUp to 29 days

Systolic and diastolic blood pressure will be measured in a supine position after at least 5 minutes of rest as a measure of safety.

Number of subjects with abnormal heart rate valuesUp to 29 days

Heart rate will be measured in a supine position after at least 5 minutes of rest as a measure of safety.

Number of subjects with abnormal respiratory rate valuesUp to 29 days

Respiratory rate will be measured in a supine position after at least 5 minutes of rest as a measure of safety.

Number of subjects with abnormal body temperature findingsUp to 29 days

Body temperature will be measured in a supine position after at least 5 minutes of rest as a measure of safety.

Number of subjects with abnormal clinical chemistry findingsUp to 29 days

Blood samples will be collected at specific time points as a measure of safety

Number of subjects with abnormal clinical hematology findingsUp to 29 days

Blood samples will be collected at specific time points as a measure of safety

Number of subjects with adverse events (AEs)Up to 29 days

An adverse event is any untoward medical occurrence in a patient or clinical investigation subject, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product.

Secondary Outcome Measures
NameTimeMethod
Titer of anti-PEGUp to 29 days

Antibodies to PEG components of GSK1827771 will be measured.

Titer of anti-dAbUp to 29 days

Antibodies to dAb components of GSK1827771 will be measured.

Plasma concentrations of GSK1827771Pre-dose, 0.25, 0.5, 1, 2, 4, 8, 12, 24 hours post-dose on Day 1; in morning and evening on Day 2-7; in morning on Day 14, 21, 28

Blood samples will be collected at specific time points for calculating plasma concentrations of GSK1827771

Titer of anti-GSK1827771Up to 29 days

Blood samples for determination of anti-GSK1827771 antibodies will be taken at specific time points.

Exploratory biomarker levels in bloodUp to 29 days

Blood samples will be taken for exploratory biomarker analysis

Maximum plasma concentration (Cmax) of GSK1827771Pre-dose, 0.25, 0.5, 1, 2, 4, 8, 12, 24 hours post-dose on Day 1; in morning and evening on Day 2-7; in morning on Day 14, 21, 28

Blood samples will be collected at specific time points for calculating Cmax of GSK1827771

Area under the curve (AUC) of GSK1827771Pre-dose, 0.25, 0.5, 1, 2, 4, 8, 12, 24 hours post-dose on Day 1; in morning and evening on Day 2-7; in morning on Day 14, 21, 28

Blood samples will be collected at specific time points for calculating AUC of GSK1827771

Frequency of anti-GSK1827771Up to 29 days

The presence of anti-GSK1827771 binding antibodies will be assessed using an immunoelectrochemiluminescence screening assay (ECL).

Frequency of anti-PEGUp to 29 days

Antibodies to PEG components of GSK1827771 will be measured.

Frequency of anti-dAbUp to 29 days

Antibodies to dAb components of GSK1827771 will be measured.

Change from Baseline response of whole blood to ex vivo stimulation with IL-1 alpha or IL-1 betaBaseline and up to 29 days

Blood samples will be collected for assessment of pharmacodynamic activity of GSK1827771 at specific time points

Trial Locations

Locations (1)

GSK Investigational Site

🇺🇸

Baltimore, Maryland, United States

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