Increasing evidence supports the importance of postprandial glucose (PPG) in glycemic control with regard to the development of complications in patients with diabetes. PPG plays a critical role in determining overall glycemic control, particularly in patients who are close to their glycemic goals. Data also indicate that postprandial hyperglycemia may have a greater effect on the development of cardiovascular complications compared with elevated fasting plasma glucose. Several antidiabetic agents that specifically target PPG are currently available, including glinides, glucagon-like peptide-1 mimetics, dipeptidyl peptidase-4 inhibitors, and rapid-acting insulin analogs. A more intensive approach to managing PPG may improve the care of patients with diabetes and, ultimately, the outcome of these patients.