To date, seven completed Phase I studies have shown BRL 49653C to be safe and well tolerated. The levels of exposure to BRL 49653C have been shown to be similar in both the fed and fasted state, and pharmacokinetic analysis has shown no evidence of accumulation after 10 days once daily dosing of 1 to 5 mg in obese volunteers. A total of 140 volunteers received BRL 49653C ranging in doses of 0.2 to 20 mg (20 mg dose is approximately 4 to 5-fold higher than doses expected to be administered to NIDDM patients). Of these, 140 subjects, 91 received one or more single doses of BRL 49653C up to 20 mg. This includes 10 healthy elderly males (>= 65 years of age). Additionally, 49 obese subjects have received dosages of up to 5 mg/day for 10 consecutive days.