Great News for Diabetics! Novo Nordisk Oral Semaglutide Got FDA Approval!

New oral Nordic Semaglutide tablet (Rybelsus)^®) was officially approved by the FDA for use in combination with diet and exercise to improve glycemic control in adults with type 2 diabetes on September 20. The drug is the first oral glucagon-like peptide-1 (GLP-1) receptor agonist drug approved worldwide. The drug is taken orally once a day and its approved therapeutic doses are 7 mg and 14 mg, which will enter the market in the US in the fourth quarter.

Type 2 diabetes is the most common type of diabetes, and occurs when the pancreas does not produce enough insulin to keep blood sugar at a normal level. GLP-1 is a normal body hormone that slows down digestion and prevents the liver from producing too much sugar, and also helps the pancreas produce more insulin when needed, therefore, it has beneficial effects on many important organs including the pancreas, heart and liver. However, insufficient levels of GLP-1 are often found in patients with type 2 diabetes.

Semaglutide belongs to the GLP-1 receptor agonist family. The advantage of GLP-1 receptor agonists is that they can effectively control blood sugar, while significantly reducing the incidence of hypoglycemic events, and also have the benefits of significant weight loss and risk reduction of cardiovascular events. On December 5, 2017, with the approval of the FDA, the injection form of Semaglutide is officially marketed as a long-acting GLP-1 receptor agonist, which is administered once a week.

Objectively speaking, compared with short-acting injection-type hypoglycemic drugs, long-acting GLP-1 receptor agonists only need to be injected once a week, thus reducing patient's pain from injection and improving patient compliance. But the majority of diabetic patients are still eagerly looking forward to the emergence of oral dosage forms. However, since Semaglutide is a polypeptide drug, it is necessary to face the challenge of degradation of various peptidases in the intestine in order to achieve oral administration and intestinal absorption. The researchers created an oral formula by combining Semaglutide with a small molecule absorption enhancer, SNAC. The combination with SNAC allows Semaglutide to be absorbed in the stomach, and partial dissolution of SNAC can locally form a relatively high pH environment in the stomach, thereby increasing the solubility of Semaglutide and reducing the degradation of peptidases in the stomach.

The application for market entry and approval of oral Semaglutide were based on the results of 10 PIONEER clinical trials involving a total of 9543 adult patients with type 2 diabetes. A series of "head-to-head" clinical trials of the PIONEER project have confirmed that, Rybelsus® is more effective at lowering blood sugar levels than Sitagliptin and Empagliflozin. In addition, weight loss of up to 4.4 kg was achieved with Rybelsus® treatment.Throughout the PIONEER trials, Rybelsus® demonstrated properties such as safety and good tolerance. In the trails, the most common adverse event was mild to moderate nausea, but with prolonged treatment could be gradually reduced.

Novo Nordisk's Rybelsus® is currently being audited by other registered regulators. For example, the application of oral Semaglutide for treating type 2 diabetes was submitted to the European Medicines Agency (EMA) on April 26, 2019, and the application was submitted to the Japan’s Pharmaceuticals and Medical Devices Agency (PMDA)in July 2019. In addition, the NDA application of Rybelsus^®(oral Semaglutide) for reducing the risk of cardiovascular events in adultPatientswith type 2 diabetes, and the sNDA application of Ozempic^®(subcutaneous injection form of Semaglutide) for new indications, i.e. reducing the risk of cardiovascular events in adult patients with type 2 diabetes, were also submitted to the FDA on March 20, 2019. These two applications are expected to be approved on January 20, 2020.

According to EvaluatePharma, GLP-1 and SGLT-2 will account for half of the world's top 10 hypoglycemic drugs in 2024. As the world's first oral GLP-1 hypoglycemic drug, global sales of oral Semaglutide are expected to reach $3.23 billion at that time.

Oral Semaglutide only needs to be administered orally once a day, to get rid of the inconvenience and psychological torture caused by the injection. At the same time, it has better hypoglycemic and weight-reducing effects than traditional mainstream drugs, and also reduces the risk of cardiovascular events. Great news for diabetes!