This crossover study investigates the safety, tolerability, pharmacokinetics (PK) ,pharmacodynamics (PD) effect of three dose levels of PB-201,and characterizes the PK profile of a prominent des-methyl metabolite of PB-201(WI-0800), following dosing of three dose levels of PB-201 in drug-naive Chinese adult subjects with Type 2 diabetes mellitus (T2DM) as monotherapy.

There were 7 days separating 4 treatment periods and at least 7-day washout (but not exceeding 14 days) between dosing in 4 periods with 3 dose levels of PB-201 and placebo. Three dose levels of PB-201 are: split dose regimen of 50 mg 30 minutes before morning meal plus 50 mg 30 minutes before lunch at approximately 3.5 hours after morning dose, and split dose regimen of 100 mg 30 minutes before morning meal plus 100 mg 30 minutes before lunch at approximately 3.5 hours after morning dose, and split dose regimen of 150 mg 30 minutes before morning meal plus 100 mg 30 minutes before lunch at approximately 3.5 hours after morning dose.

Inclusion Criteria:

1. Glycosylated hemoglobin (HbA1c) 7.5%-11% at screening, and 7.0%-10.0% pre-randomization
2. FPG 7.0 mmol/L-11.0mmol/L at screening and pre-randomization
3. Body mass index (BMI) 18.5 and-35.0 kg/m2 at screening
4. Antidiabetics-naive within 2 months before screening

Exclusion Criteria:

1. Diagnosis of type 1 diabetes mellitus or secondary forms of diabetes

2. History of febrile illness within 5 days prior to dosing

3. Medical history of myocardial infarction, angina/unstable angina, coronary revascularization, stroke or transient ischemic attack

4. Any medical history or current clinical evidence of congestive heart failure, New York Heart Association (NYHA) Functional Classification, Classes II-IV

5. Episode(s) of hypoglycemia adverse events (HAE) of 'severe' intensity prior to screening; either:

   1. >1 in the previous 3 months; or
   2. >2 in the previous 6 months