Safety and Pharmacokinetics Study of HE3286 in Patients With Active, Mild-to-Moderate Ulcerative Colitis

Inclusion Criteria:

• 18-65 years of age
• Diagnosed (> 6 weeks) or recently relapsed active mild-to-moderate ulcerative colitis based on colonoscopy or flexible sigmoidoscopy
• Mayo Scoring System for Assessment of Ulcerative Colitis Activity score of 4-9
• Stable dose prior to screening of 6-mercaptopurine (50-150 mg/day 6-MP) [at least 2 months], Azathioprine (50-100 mg/day) [at least 2 months], and 5-ASA [at least 2 weeks]
• For females of reproductive potential, agree to avoid pregnancy during the study and for 3 months following study completion, have a negative serum pregnancy test (b-HCG) at screening and negative urine pregnancy test and use an acceptable method of birth control
• No history of narcotic and/or alcohol abuse within 2 years of screening and agrees to consume < 6 oz. of wine or equivalent per day
• No experienced renal or liver disease by history and/or based on laboratory results
• Must provide voluntary, written, informed consent prior to screening evaluations and be able to follow verbal and written instructions
• Must be able to swallow capsules

Exclusion Criteria:

• Primary sclerosing cholangitis
• Positive for C. difficile toxin in the stool
• Requires hospitalization for treatment of severe ulcerative colitis
• History of clinically significant cardiovascular disease (including coronary artery disease), clinically significant hepatic, respiratory or renal abnormalities, or clinically significant endocrine disorders (not including diabetes)
• Clinically significant abnormalities on laboratory results (renal insufficiency, liver function abnormalities, abnormal WBC or ANC)
• Any clinically significant unstable medical abnormality, chronic disease, or active, serious clinical infection or condition, other than ulcerative colitis
• Uncontrolled hypertension defined as systolic BP > 160 mmHg and/or diastolic BP > 100 mmHg on three or more assessment on more than one day(blood pressure must be stable for > 3 months prior to screening)
• Malignancy within the past 5 years, except for successfully treated basal cell carcinoma of the skin
• Requiring or receiving anti-TNF-a or other immune modulating drugs (other than 6-MP or azathioprine) within 8 weeks prior to screening
• Requiring or receiving any of the following within 4 weeks of the screening visit: interleukins, steroids (i.e., anabolic steroids, glucocorticoids), narcotics, anti-cancer chemotherapeutic agents, metabolic inhibitors or nutraceuticals with immune enhancement claims
• Requiring oral or intravenous cortisone
• Requiring corticosteroid enemas
• Acute illness within 10 days prior to Day 1 or taking antibiotics for UC (but not for a infectious disease) within 14 days of Day 1
• Any clinical condition or receiving therapy that, in the opinion of the Investigator, would make the patient unsuitable for study or unable to comply with the dosing requirements