Safety, Tolerance, Pharmacokinetics and Activity of HE3286 in Patients With Rheumatoid Arthritis

Main Inclusion Criteria:

• Male or female patient 18-75 years of age
• Patient with stable or active disease on a stable dose of methotrexate for at least 30 days prior to Day 1
• Patient has normal thyroid stimulating hormone (TSH) levels with or without thyroid replacement therapy
• Patient is willing to abstain from consuming grapefruit containing products from 24 hours prior to dosing until the end of the study as it may affect the pharmacokinetic measurements
• Patient has not experienced renal or liver disease by history and/or based on laboratory results
• Patient has not experienced acute cardiac disease within 6 months prior to Screening
• Patient must provide voluntary, written, informed consent prior to screening evaluations and be able to follow verbal and written instructions.

Main Exclusion Criteria:

• Functional status class IV according to The American College of Rheumatology (ACR) criteria
• Patient who has a history of clinically significant cardiovascular disease (including coronary artery disease), clinically significant hepatic, respiratory or renal abnormalities, or clinically significant endocrine disorders (including diabetes)
• Patient with active Tuberculosis (TB) or evidence of latent TB without previous adequate therapy
• Systemic autoimmune disorder (including, but not limited to, systemic lupus erythematosus, inflammatory bowel disease, scleroderma, inflammatory myopathy, mixed connective tissue disease or any overlap syndrome)
• Inflammatory joint disease other than RA

• Patient who has received any of the following immunosuppressive drugs:

  • Etanercept within 1 month of Day 1;
  • Abatacept, adalimumab, infliximab, leflunomide, imuran, cyclosporin, anakinra, sulfasalazine, bextra, celebrex or gold within 2 months of Day 1 or for biological agents 6 half lives, whichever is greater;
  • Rituximab within 1 year of Day 1
• Patient that is bed or wheelchair bound
• Patients taking prednisone within 2 weeks prior to Screening
• Patient requiring or receiving any of the following within thirty (30) days prior to the screening visit: interleukins, steroids (i.e., anabolic steroids, glucocorticoids), hormone replacement therapy (except stable low-dose HRT for at least 6-months prior to screening), birth control pills, anti-cancer chemotherapeutic agents (except methotrexate), metabolic inhibitors (except methotrexate), concomitant medications that prolong the QT/QTc interval
• Patient who has any clinically significant abnormalities in laboratory results at Screening