Background: Type-2 diabetes mellitus accounts for 80-90% of diabetic patients.
So far, the treatment of diabetes mainly aims at elevating insulin level and lowering glucose
level in the peripheral blood and mitigating insulin resistance. Physiologically, insulin secretion
from pancreatic β cells is delicately regulated. Thus, how insulin-related therapies could
titrate blood glucose appropriately and avoid the occurrence of hypoglycemia remains an important
issue for decades. Similar question is addressed on how to attenuate vascular complication
in diabetic subjects.
Methods: We overviewed the evolution of each class of anti-diabetic drugs that have been
used in clinical practice, focusing on their mechanisms, clinical results and cautions.
Results: Glucagon-like peptide-1 receptor agonists stimulate β cells for insulin secretion in
response to diet but not in fasting stage, which make them superior than conventional insulinsecretion
stimulators. DPP-4 inhibitors suppress glucagon-like peptide-1 degradation. Sodium/
glucose co-transporter 2 inhibitors enhance glucose clearance through urine excretion.
The appearance of these new drugs provides new information about glycemic control. We update
the clinical findings of Glucagon-like peptide-1 receptor agonists, DPP-4 inhibitors and
Sodium/glucose cotransporter 2 inhibitors in glycemic control and the risk or progression of
cardiovascular disease in diabetic patients. Stem cell therapy might be an alternative tool for
diabetic patients to improve β cell regeneration and peripheral ischemia. We summarize the
clinical results of mesenchymal stem cells transplanted into patients with diabetic limb and
Conclusion: A stepwise intensification of dual and triple therapy for individual diabetic patient
is required to achieve therapeutic target.