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Efficacy and Safety Study of R935788 Tablets to Treat Rheumatoid Arthritis (Taski-3)

Phase 2
Completed
Conditions
Rheumatoid Arthritis
Interventions
Registration Number
NCT00665626
Lead Sponsor
Rigel Pharmaceuticals
Brief Summary

The purpose of this study is to determine whether the Spleen Tyrosine Kinase (Syk) Inhibitor, R935788 (R788) at a dose of 100 mg, tablet, orally, twice-a-day is effective in the treatment of Rheumatoid Arthritis in patients who have 'failed' a biologic therapy.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
219
Inclusion Criteria
  • Patients must give written informed consent by signing an IRB/EC-approved Informed Consent Form (ICF) prior to admission to this study.
  • Males and females, 18 years of age or older, with active RA for at least 12 months prior to Day 1 dosing
  • Are currently receiving or previously had received a biologic therapy with an inhibitor of TNF, rituximab, abatacept, or anakinra at an approved labeled dose for ≥3 months prior to Day 1 dosing and are designated as biologic therapy failures for lack of efficacy, safety, or tolerability.
  • Patients may receive stable doses of methotrexate (MTX), azathioprine (not in combination with MTX), leflunomide (not in combination with MTX), sulfasalazine, chloroquine, hydroxychloroquine, gold, NSAIDs (including COX2 inhibitors), minocycline, or doxycycline. The dose must have been stable for at least 30 days prior to Day 1 dosing and must not be changed during the washout, screening and treatment periods, unless dictated by tolerability requirements. Patients who are taking MTX must have been receiving weekly MTX doses (7.5-25 mg/week) for a minimum of 3 months prior to Day 1 dosing and must be receiving a stable MTX dose, with no change in route, for the previous 6 weeks prior to Day 1 dosing. Patients who are receiving MTX must also be receiving folic or folinic acid supplementation at a stable dose for at least 6 weeks prior to Day 1 dosing.
  • Females of childbearing potential must be fully informed of the potential for R788 to adversely affect the fetus and, if sexually active, must agree to use a well established method of birth control during the study (oral contraceptive, mechanical barrier, long acting hormonal agent). These patients must not be lactating and must have a negative urine pregnancy test at the time of randomization and at each laboratory determination.
  • The patient must otherwise be in good health as determined by the Investigator on the basis of medical history, physical examination, and laboratory screening tests during the screening period. See exclusion criteria for specific exclusions.
  • In the Investigator's opinion, the patient has the ability to understand the nature of the study and any hazards of participation, and to communicate satisfactorily with the Investigator and to participate in, and to comply with, the requirements of the entire protocol.
Exclusion Criteria
  • The patient has a history of, or a concurrent, clinically significant illness, medical condition (other than arthritis) or laboratory abnormality that, in the Investigator's opinion, could affect the conduct of the study. Specifically, excluded are patients with the following:

    1. uncontrolled or poorly controlled hypertension;
    2. other autoimmune disease (psoriatic arthritis, lupus, mixed connective disorder) or arthritis syndromes (gout, Lyme disease, Reiter's syndrome);
    3. recent serious surgery or infectious disease;
    4. recent history ( of, or treatment for, a malignancy other than nonmelanomatous skin cancer, or any history of lymphoma;
    5. Hepatitis B;
    6. Hepatitis C;
    7. interstitial pneumonitis or active pulmonary infection on chest x-ray
    8. Tuberculosis (TB)
    9. known laboratory abnormalities
  • The patient has a history of substance abuse, drug addiction or alcoholism. Patients may consume up to 4 units of alcohol per week; however, alcohol should be avoided in the 72 hours prior to lab assessments. Patients who cannot reliably comply with this should be excluded. A unit of alcohol is defined as the following: Beer=12 oz or 355 mL; wine = 5 oz or 148 mL; sweet dessert wine=3 oz or 89 mL; 80 proof distilled spirits= 1.5 oz or 44 mL.

  • The patient has been treated previously treated with R788 under a different protocol.

  • The patient has a pacemaker, aneurysm clip or other contraindication to MRI.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Arm 1Fostamatinib disodium (R935788)Fostamatinib disodium (R935788) 100 mg tablet, orally, twice-a-day
Arm 2PlaceboPlacebo, orally, twice-a-day
Primary Outcome Measures
NameTimeMethod
American College of Rheumatology 20 (ACR20) Response at 3 Months3 months

The number of participants with greater than or equal to 20% improvement in tender and swollen joint counts, AND in any 3 of the following: physician's assessment of disease activity, patient's assessment of disease activity, patient's assessment of pain, Health Assessment Questionnaire-Disability Index (HAQ-DI); and CRP or ESR, after 3 months

Secondary Outcome Measures
NameTimeMethod
Aspartate Aminotransferase (AST) >1.5-2x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with AST (a test of liver function) values greater than 1.5 to 2 times the ULN

Disease Activity Score-C-Reactive Protein (DAS28-CRP) <2.6 at 3 Months3 months

Number of participants with DAS28-CRP (measuring RA symptoms including: tender joint count, swollen joint count, patient's assessment of disease activity, and CRP in patients with high CRP at baseline), of less than 2.6. The DAS runs from 0 to 10 - higher scores indicate worse symptoms. A score of less than 2.6 indicates remission of RA symptoms

Disease Activity Score-C-Reactive Protein (DAS28-CRP) <3.2 at 3 Months3 months

Number of participants with DAS28-CRP (measuring RA symptoms including: tender joint count, swollen joint count, patient's assessment of disease activity, and CRP in patients with high CRP at baseline), of less than 3.2. The DAS runs from 0 to 10 - higher scores indicate worse symptoms. A score of less than 3.2 indicates low disease activity.

Disease Activity Score-Erythrocyte Sedimentation Rate (DAS28-ESR) <2.6 at 3 Months3 months

Number of participants with DAS28-ESR (measuring RA symptoms including: tender joint count, swollen joint count, patient's assessment of disease activity, and ESR in patients with high ESR at baseline), of less than 2.6. The DAS runs from 0 to 10 - higher scores indicate worse symptoms. A score of less than 2.6 indicates remission of RA symptoms

Disease Activity Score-Erythrocyte Sedimentation Rate (DAS28-ESR) <3.2 at 3 Months3 months

Number of participants with DAS28-ESR (measuring RA symptoms including: tender joint count, swollen joint count, patient's assessment of disease activity, and ESR in patients with high ESR at baseline), of less than 3.2. The DAS runs from 0 to 10 - higher scores indicate worse symptoms. A score of less than 3.2 indicates low disease activity.

American College of Rheumatology 50 (ACR50) Response at 3 Months3 months

The number of participants with greater than or equal to 50% improvement in tender and swollen joint counts, AND in any 3 of the following: physician's assessment of disease activity, patient's assessment of disease activity, patient's assessment of pain, HAQ-DI; and CRP or ESR, whichever was elevated at baseline, after 3 months

American College of Rheumatology 70 (ACR70) Response at 3 Months3 months

The number of participants with greater than or equal to 70% improvement in tender and swollen joint counts, AND in any 3 of the following: physician's assessment of disease activity, patient's assessment of disease activity, patient's assessment of pain, HAQ-DI; and CRP or ESR, whichever was elevated at baseline, after 3 months

American College of Rheumatology Index of Improvement (ACRn) at 3 Months3 months

The index of improvement in RA, where 0 indicates no improvement and 100 indicates a 100% improvement across all signs and symptoms of RA after 3 months of treatment

American College of Rheumatology 20 (ACR20) Response at Week 11 week

The number of participants with greater than or equal to 20% improvement in tender and swollen joint counts, AND in any 3 of the following: physician's assessment of disease activity, patient's assessment of disease activity, patient's assessment of pain, HAQ-DI; and CRP or ESR, whichever was elevated at baseline, after 1 week.

American College of Rheumatology 20 (ACR20) Response at Week 22 weeks

The number of participants with greater than or equal to 20% improvement in tender and swollen joint counts, AND in any 3 of the following: physician's assessment of disease activity, patient's assessment of disease activity, patient's assessment of pain, HAQ-DI; and CRP or ESR, whichever was elevated at baseline, after 2 weeks

Rheumatoid Arthritis Magnetic Resonance Imaging Scoring (RAMRIS) Erosion Score at 3 MonthsBaseline to 3 months

Change from baseline in RAMRIS erosion score (a measure of bone erosion in the hands and wrists), calculated as the score at 3 months minus the score at baseline. The erosion score runs from 0 to 250 with lower values indicating a better clinical condition. A negative change indicates an improvement in symptoms.

Rheumatoid Arthritis Magnetic Resonance Imaging Scoring (RAMRIS) Osteitis Score at 3 MonthsBaseline to 3 months

Change from baseline in RAMRIS osteitis score (a measure of bone inflammation in the hands and wrists), calculated as the score at 3 months minus the score at baseline. The osteitis score runs from 0 to 75 with lower values indicating a better clinical condition. A negative change indicates an improvement in symptoms.

Rheumatoid Arthritis Magnetic Resonance Imaging Scoring (RAMRIS) Synovitis Score at 3 MonthsBaseline to 3 months

Change from baseline in RAMRIS synovitis score (a measure of inflammation in the joints of the hands and wrists), calculated as the score at 3 months minus the score at baseline. The synovitis score runs from 0 to 24 with lower values indicating a better clinical condition. A negative change indicates an improvement in symptoms.

Alanine Aminotransferase (ALT) >1.5x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with ALT (a test of liver function) values greater than 1.5 times the ULN

Alanine Aminotransferase (ALT) >1.5-2x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with ALT (a test of liver function) values greater than 1.5 to 2 times the ULN

Alanine Aminotransferase (ALT) >2-3x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with ALT (a test of liver function) values greater than 2 to 3 times the ULN

Alanine Aminotransferase (ALT) >3x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with ALT (a test of liver function) values greater than 3 times the ULN

Alanine Aminotransferase (ALT) >3-5x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with ALT (a test of liver function) values greater than 3 to 5 times the ULN

Alanine Aminotransferase (ALT) >5-10x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with ALT (a test of liver function) values greater than 5 to 10 times the ULN

Alanine Aminotransferase (ALT) >10x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with ALT (a test of liver function) values greater than 10 times the ULN

Aspartate Aminotransferase (AST) >1.5x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with AST (a test of liver function) values greater than 1.5 times the ULN

Aspartate Aminotransferase (AST) >2-3x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with AST (a test of liver function) values greater than 2 to 3 times the ULN

Aspartate Aminotransferase (AST) >3x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with AST (a test of liver function) values greater than 3 times the ULN

Aspartate Aminotransferase (AST) >3-5x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with AST (a test of liver function) values greater than 3 to 5 times the ULN

Aspartate Aminotransferase (AST) >5-10x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with AST (a test of liver function) values greater than 5 to 10 times the ULN

Aspartate Aminotransferase (AST) >10x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with AST (a test of liver function) values greater than 10 times the ULN

Bilirubin >1.5x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with bilirubin (a test of liver function) values greater than 1.5 times the ULN

Alkaline Phosphatase >1.5x Upper Limit of Normal (ULN) and >1.5x BaselineAny time between baseline and 3 months

The number of participants with alkaline phosphatase (a test of liver function) values greater than 1.5 times the ULN and greater than 1.5 times baseline

Bilirubin >2x Upper Limit of Normal (ULN)Any time between baseline and 3 months

The number of participants with bilirubin (a test of liver function) values greater than 2 times the ULN

Absolute Neutrophil Count (ANC) <1500/mm3Any time between baseline and 3 months

The number of participants with ANC values less than 1500/mm3

Trial Locations

Locations (43)

RASF-Clinical Research Center

🇺🇸

Boca Raton, Florida, United States

The Osteoporosis & Clinical Trials Center

🇺🇸

Hagerstown, Maryland, United States

Desert Medical Advances

🇺🇸

Palm Desert, California, United States

Department of Rheumatology

🇺🇸

Washington, District of Columbia, United States

Memorial Medical Group Clinical Research Inst

🇺🇸

South Bend, Indiana, United States

Arthritis & Rheumatic Disease Specialties

🇺🇸

Aventura, California, United States

Hopital Pellegrin

🇫🇷

Bordeaux Cedex, France

CHU Liege

🇧🇪

Liege, Belgium

Paddock Park Clinical Research

🇺🇸

Ocala, Florida, United States

San Diego Arthritis & Medical Clinic

🇺🇸

San Diego, California, United States

Rheumatology Associates, SC

🇺🇸

Chicago, Illinois, United States

Houston Institute for Clinical Research

🇺🇸

Houston, Texas, United States

Azienda Ospedaliera Santa Maria della Miseri

🇮🇹

Udine, Italy

Florida Medical Research Institute

🇺🇸

Gainsville, Florida, United States

Intermountain Orthopedics

🇺🇸

Boise, Idaho, United States

Lovelace Scientific Resources

🇺🇸

Sarasota, Florida, United States

Fiechtner Research, Inc.

🇺🇸

Lansing, Michigan, United States

North Shore Long Island Jewich Health System

🇺🇸

Lake Success, New York, United States

Andrew Porges, MD PC

🇺🇸

Roslyn, New York, United States

Rheumatology Associates

🇺🇸

Erie, Pennsylvania, United States

Clinical Research Division

🇺🇸

Mayfield Village, Ohio, United States

Rheumatology Associates of Long Island

🇺🇸

Smithtown, New York, United States

Clinical Research Center of Reading, LLP

🇺🇸

West Reading, Pennsylvania, United States

Rheumatic Disease Associates

🇺🇸

Willow Grove, Pennsylvania, United States

ZNA Middelheim

🇧🇪

Antwepen, Belgium

Arthritis Northwest, PLLC

🇺🇸

Spokane, Washington, United States

UZ Gent

🇧🇪

Gent, Belgium

Reumalab S.A.

🇨🇴

Medellin, Antioquia, Colombia

Reumatologos del Caribe

🇨🇴

Barranquilla, Atlantico, Colombia

CIREEM

🇨🇴

Bogota, Cundinamarca, Colombia

Dr. Renato Guzman

🇨🇴

Bogota, Cundinamarca, Colombia

Riesgo de Fractura S.A.

🇨🇴

Bogota, Cundinamarca, Colombia

Klinikum der J.W. Goethe Universitaet

🇩🇪

Frankfurt, Germany

ClinPharm International GmbH Leipzig

🇩🇪

Leipzig, Germany

Klinikum Eilbek

🇩🇪

Hamburg, Germany

Rheumazentrum am Universitatsklinikum Leipzig

🇩🇪

Leipzig, Germany

Reumatologia Azienda Ospedaliera Universitaria

🇮🇹

Siena, Italy

Universitatsklinikum Wurzburg

🇩🇪

Wurzburg, Germany

Instituto de Ginecologia y Reproduccion

🇵🇪

Lima, Peru

Center for Arthritis & Osteoperosis

🇺🇸

Elizabethtown, Kentucky, United States

Health Research of Oklahoma

🇺🇸

Oklahoma City, Oklahoma, United States

Westroads Medical Group

🇺🇸

Omaha, Nebraska, United States

Austin Rheumatology & Research

🇺🇸

Austin, Texas, United States

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