The number of people with diabetes in my country ranks first in the world, and the launch of new oral drugs can greatly improve the quality of life of patients.
my country is the largest country with diabetes, and the number of sugar friends has exceeded 100 million. Although there are many hypoglycemic therapies, there is still a high proportion of type 2 diabetes patients who have not reached the target blood sugar level after oral hypoglycemic drugs, and more effective treatments are urgently needed.
A few days ago, Novo Nordisk announced that the European Commission has approved the marketing of oral semaglutide tablets (trade name Rybelsus) to improve the blood glucose levels of patients with type 2 diabetes with diet and exercise.
Semaglutide tablets are the first and currently only oral glucagon-like peptide 1 (GLP-1) receptor agonist. In September last year, semaglutide tablets have been approved by the US FDA, combined with diet control and exercise, to improve blood sugar control in adult patients with type 2 diabetes.
The approval is based on the efficacy and safety of oral semaglutide in 10 PIONEER clinical trials, which included a total of 9543 adults with type 2 diabetes.
The results showed that after 52 weeks of treatment, compared with sitagliptin (DPP-4 inhibitor), empagliflozin (SGLT2 inhibitor), and liraglutide (GLP-1 receptor agonist), taking Soma The glycosylated hemoglobin level (HbA1c) of patients with glutide tablets was significantly reduced, and the weight could be reduced by up to 4.3 kg.
Talk about GLP-1 receptor agonists
Semaglutide is an analog of the natural hormone GLP-1. GLP-1 is a polypeptide hormone secreted by intestinal cells. By binding to the GLP-1 receptor, it stimulates the secretion of insulin and inhibits the secretion of glucagon, thereby promoting glucose metabolism. At the same time, it can also delay gastric emptying and suppress appetite.
Natural GLP-1 is secreted after people have a meal, stimulated by glucose. In patients with type 2 diabetes, the secretion level of GLP-1 is significantly reduced, which is also one of the important reasons that lead to uncontrolled blood sugar in patients. Therefore, the development of GLP-1 analogs has always been an important research direction for the treatment of type 2 diabetes.
In 2017, the US FDA has approved Semaglutide injection (Semaglutide, trade name Ozempic) (0.5 mg or 1 mg) as an aid to diet adjustment and exercise to improve blood glucose levels in type 2 diabetes. In January this year, semaglutide injection Ozempic was again approved by the FDA to reduce the risk of major adverse cardiovascular events in adult patients with pre-existing cardiovascular disease, including myocardial infarction, stroke or death.
At present, the FDA has approved a total of 8 GLP-1 receptor agonist products on the market. Except for semaglutide tablets, the rest are injections.
The emergence of semaglutide tablets has broken the dilemma of daily or weekly GLP-1RA injections for patients with type 2 diabetes, and provided them with a less invasive and convenient treatment option for blood sugar control.
From injection to oral administration, it’s far more complicated than you think
From a convenient point of view, oral medication is the preferred method of medication for patients. However, oral drugs are usually small molecules and need to have a certain degree of hydrophobicity.
Generally speaking, the absorption of small molecule drugs is mainly carried out in the intestine. However, the absorption of peptide drugs in the intestinal tract will face great challenges, because a variety of peptidases in the intestine will degrade peptides before they are absorbed.
The uniqueness of oral semaglutide is that a small molecule absorption enhancer called SNAC is added to allow semaglutide to be directly absorbed in the stomach.
At the same time, the dissolution of SNAC in the stomach can locally increase the pH of the environment, increase the solubility of semaglutide, and prevent semaglutide from being degraded by peptidases in the stomach.
Although semaglutide tablets are oral dosage forms, their performance in controlling blood sugar and reducing patients’ weight is no less than that of semaglutide injections.
At present, semaglutide has been approved in the United States, Switzerland and the European Union as an aid to improve blood sugar levels in adults with type 2 diabetes.
From the approval of the first GLP-1RA drug to the approval of semaglutide tablets, GLP-1 receptor agonists have gone through several iterations.
It is hoped that the new therapy will be launched in China as soon as possible, and it will bring more convenient and effective choices for patients with type 2 diabetes.