Bucillamine for the Treatment of Acute Gout Flare in Subjects With Moderate to Severe Gout

To evaluate the safety and tolerability of two regimens of Bucillamine 100 mg (900 mg and
1,800 mg) over seven days of treatment compared with Colchicine 0.6 mg (1.8 mg) in the
treatment of patients with acute gout flare

Inclusion Criteria:

- Subjects must present with confirmed diagnosis of gout, meeting the American College
of Rheumatology (ACR) 1977 preliminary criteria for the classification of acute
arthritis of primary gout

- Subjects must have experienced at least one (1) acute gouty arthritic attack in the
12 months prior to randomization

- Presence of acute gout flare for no longer than 3 days at Visit 2

- Pain intensity at inclusion (Visit 2) of 7-10 on 11-point PI-NRS (defined as severe
gout flare for this study)

- All patients should not have contraindications for Colchicine use

- Subjects with a history of intolerance to NSAIDs (Checklists Checklist 1)

- Subjects with significant medical contraindication to NSAIDs (Checklist 2)

- Subjects with past failure of NSAIDs to control acute gouty arthritis attacks in the
previous 12 months (Checklist 3)

- Regarding significant medical contraindication to NSAIDs or past failure of NSAIDs to
control acute gouty arthritis attacks in the previous 12 months (i.e. refractoriness
to NSAIDs) the patient must meet one of below criteria:

1. At least one historical episode within the previous 12 months of being
refractory or intolerant to NSAIDs that makes the physician concerned to use
NSAIDs for a subsequent acute gout attack

2. The current (referring) physician judgment is that NSAIDs are not appropriate
for treating the patient's gouty arthritis flare which may be due to changes in
patient status such as worsening co-morbid conditions or co-medications (e.g.,
GI tract disease, renal insufficiency, hypertension, fluid retention, concurrent
use of diuretics and/or an angiotensin converting enzyme inhibitor or
angiotensin receptor blocker, especially in CKD)

- Subjects must be willing and able to give written informed consent. A HIPAA and/or
state privacy consent must also be signed

- Subjects must be able to swallow tablets

- Use of permitted concomitant medications must be unchanged in dose and or frequency,
30 days prior to screening

- Adequate organ function, evidenced by the following laboratory results within 90 days
prior to randomization (historical lab results are acceptable).

- Creatine clearance > 45 mL/min based on Cockroft-Gault glomerular filtration rate
(GFR) estimation

- For women of childbearing potential and men with partners of childbearing potential,
agreement to use a highly effective, non-hormonal form of conception.

Exclusion Criteria:

- Subjects with rheumatoid arthritis, psoriatic arthritis, evidence/suspicion of
infectious/septic arthritis, acute polyarticular gout (4 or more joints), with
arthritis due to any cause other than gout that may confound any study assessments
per Investigator discretion

- Subjects who have experienced >2 acute gouty arthritic attacks per month, or >12
attacks overall, in the 6 months prior to randomization

- Subjects with a history of myocardial infarction, unstable angina, cerebrovascular
events, or coronary artery bypass grafting within the previous 6 months prior to
screening

- Subjects with a Body Mass Index >45 kg/m2; calculated as body weight (kg)/height (m)2
at Screening Visit

- Subjects with acute or chronic infections including known HIV and/or Hepatitis B or C

- Uncontrolled hypertension (>160/90 mmHg seated) (if the first set of BP assessment
meets the definition of uncontrolled hypertension, a second set of BP assessments may
be performed after the patient has rested for at least 30 min. If the second set of
BP assessments does not meet the definition of uncontrolled hypertension the patient
will be eligible for participation)

- Subjects with proteinuria ≥1+ or ≥30 mg on dipstick urinalysis that is confirmed on
repeat assessment within 24 hours

- Subjects with significant heart failure and activity impairment (Class III-IV of the
New York Heart Association (NYHA)

- Subjects with any history of malignancy, 5 years prior to randomization

- Subjects with CKD NKF stages 3B -5 chronic renal dysfunction (eGFR <45 mL/min/1.73m2
acc. to Cockcroft Gault formula)

- Subjects with serious hepatic disorder (Child-Pugh scores B or C)

- Subjects who have not washed out of dopamine antagonists or depleting drugs excluding
anticholinergics and/or antihistamines with anticholinergic effects at least 14 days
prior to Day 1 (Visit 2)

- Subjects with a documented history of alcohol or substance abuse within the 12 months
prior to randomization(consumption of >21 units of alcohol per week is considered
alcohol abuse)

- Subjects with significant CNS effects including vertigo and dizziness