Gemigliptin: An emerging treatment option for Type 2 diabetes


It is a newer drug for the treatment of type 2 diabetes. It belongs to the class of medications known as dipeptidyl peptidase-4 (DPP-4) inhibitors and works by increasing the levels of the incretin hormones glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) in the body. Incretins help stimulate insulin secretion from the pancreas in a glucose-dependent manner and suppress glucagon secretion, both actions which help lower blood sugar levels.

How does it work?

It works by selectively inhibiting the DPP-4 enzyme. DPP-4 is responsible for the breakdown of the incretin hormones GLP-1 and GIP. By blocking the action of DPP-4, it allows GLP-1 and GIP levels to remain elevated for longer after eating. This helps promote insulin secretion from pancreatic beta cells when blood glucose levels rise after eating. At the same time, it also suppresses excess glucagon release from pancreatic alpha cells, which normally opposes the blood sugar lowering effect of insulin. Together, these actions of it help regulate post-meal blood sugar levels and aid in bringing hyperglycemia under control in patients with type 2 diabetes.

Clinical efficacy

Several clinical trials have evaluated the anti-hyperglycemic efficacy and safety profile of Gemigliptin:

– A 12-week study compared 50mg to placebo or sitagliptin 100mg in 471 patients with type 2 diabetes. It led to greater reductions in A1C levels (measure of average blood sugar levels over past 3 months) compared to placebo. Its effects were similar to sitagliptin.

– Another 24-week study randomized 675 patients to 50mg or glimepiride (a sulfonylurea drug) 1-4mg. Both treatments significantly lowered A1C, with demonstrating non-inferiority to glimepiride. It also reduced fasting plasma glucose levels better than glimepiride.

– A long-term 104-week study evaluated the durability of its glucose-lowering effects. It showed 50mg maintained reductions in A1C levels comparable to baseline even after 2 years of treatment with no significant safety issues reported.

– Combination studies showed 50mg added to metformin or glimepiride therapy provided additional A1C lowering beyond single drug therapies alone, with a safety profile similar to the individual components.

This clinical evidence supports gemigliptin’s effectiveness at improving glycemic control when used as monotherapy or in combination with other oral anti-diabetic drugs. Its effects appear durable over the long-term without high risks of hypoglycemia.

Safety and tolerability

Overall, gemigliptin has demonstrated a favorable safety and tolerability profile in clinical trials:

– Incidence of adverse effects with it has generally been low and comparable to placebo.

– No episodes of severe hypoglycemia have been reported with its monotherapy unlike some other anti-diabetic drugs. This lowers the risk of potentially dangerous hypoglycemic episodes in patients.

– Being weight neutral, it does not promote weight gain – a side effect seen commonly with many other diabetes medications like insulin secretagogues and insulin.

– Other side effects reported include headache, nasopharyngitis and urinary tract infection – all mild to moderate in severity.

– No drug interactions of clinical significance have been observed thus far withit. It can therefore be safely combined with many other commonly used medications.

Wider applications

Apart from its efficacy in lowering blood glucose levels, some additional benefits of its therapy are being evaluated:

– Studies suggest DPP-4 inhibition with gemigliptin may provide protective effects against diabetes complications by reducing cardiovascular risk factors, improving lipid profiles and showing anti-inflammatory activity.

– Preliminary research indicates it may aid weight loss, improve fatty liver disease and help control post-meal sugar spikes in diabetic patients – expanding its clinical applications.

– Ongoing investigations are also exploring gemigliptin’s potential role in reversing beta cell dysfunction and loss of insulin secretion over the long-term progression of diabetes.

Thus, it appears to be a promising oral anti-diabetic medication offering glycemic control with a favorable side effect profile. Its multiple extra-pancreatic effects may distinguish it from other drugs in its class with broader clinical benefits for managing diabetes and preventing its complications long-term.

Availability and conclusion

It has been approved for treatment of type 2 diabetes in several nations including South Korea, China and other Asian countries. In India, it is currently under review by drug regulators. If approved, it will provide clinicians an effective new option to optimize glycemic management, especially in patients where other oral drugs cannot be used or have failed. Its novel advantages related to safety, weight changes and beta cell preservation also position gemigliptin favourably as a treatment paradigm likely to increase medication adherence in diabetes care. Ongoing research continues to expand our understanding of all its therapeutic attributes.

1.  Source: Coherent Market Insights, Public sources, Desk research
2. We have leveraged AI tools to mine information and compile it