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From Injections to Pills GLP 1 for Type 2 Diabetes .pdf

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From Injections to Pills: GLP-1 for Type 2
Diabetes is increasing at an alarming rate in the United States. According to
the CDC’s (Centers for Disease Control) National Diabetes Statistics
Report for 2020 cases of diabetes have risen to an estimated 34.2 million.
Although there are many anti-diabetic therapies, there is still a high proportion
of patients with type 2 diabetes who do not reach the target blood glucose level
after oral anti-diabetic drugs, and a more effective treatment plan is urgently
In September 2019, Novo Nordisk announced that the FDA approved the oral
Semaglutide tablets (trade name Rybelsus) to be marketed, combined with
diet and exercise to improve blood sugar levels in patients with type 2 diabetes.
Semaglutide tablets are the first and currently the only oral glucagon-like
peptide 1 (GLP-1) receptor agonist. The approval is based on the efficacy
and safety of oral semaglutide in 10 PIONEER clinical trials involving a total of
9543 adults with type 2 diabetes.

About GLP-1 Receptor Agonist
Semaglutide is an analogue of the natural hormone GLP-1. GLP-1, a peptide
hormone secreted by intestinal cells, stimulates the secretion of insulin and
inhibits the secretion of glucagon by binding to the GLP-1 receptor, thereby
promoting glucose metabolism. At the same time, it can also delay gastric
emptying and suppress appetite.
Natural GLP-1 is secreted by the stimulation of glucose after a meal. In



patients with type 2 diabetes, the level of GLP-1 secretion is significantly
reduced, which is also one of the important reasons for the uncontrolled blood
glucose of patients. Therefore, the development of GLP-1 analogues has been
an important research and development direction for the treatment of type 2
In 2017, the US FDA approved Semaglutide injection (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 of 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.
Currently, the FDA has approved a total of 6 GLP-1 receptor agonist
products for the market. Except for semaglutide tablets (Rybelsus), the
rest are injections.
Generic Name

Commercial Name
Byetta, Bydureon
Victoza, Saxenda

FDA Aprroval Year


Lyxumia in Europe, Adlyxin in the United States



Ozempic, Rybelsus


The emergence of semaglutide tablets has broken the dilemma that patients
with type 2 diabetes need to receive GLP-1RA injections daily or weekly,
providing them with a less invasive and convenient treatment option for
controlling blood sugar.

From Injections to Pills
From a convenient point of view, oral medication is the preferred method of
medication for patients. Oral drugs are usually small molecules and need to be



In general, the absorption of small molecule drugs mainly takes place in the
intestine. However, the absorption of peptide drugs in the intestinal tract will
face great challenges, because many peptidases present in the intestinal tract
will degrade the polypeptide before it is absorbed.
The uniqueness of oral semaglutide is that a small molecule absorption
enhancer called SNAC is added to allow semaglutide to be absorbed directly
in the stomach.
At the same time, SNAC dissolution 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.

Image Source: Dovepress, The mechanism of absorption of semaglutide and SNAC
coformulation tablet.

Although semaglutide tablets are oral, their performance in controlling blood
sugar and reducing patients' weight is no worse than that of somalutide
At present, semaglutide has been approved in the United States, Switzerland



and the European Union as an auxiliary means to improve blood sugar levels
in adults with type 2 diabetes.
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Product Name















Rybelsus® (oral semaglutide) approved for the treatment of adults with type 2
diabetes in the EU
Rybelsus® (semaglutide tablets), the first GLP-1 in a tablet approved in the US

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