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Following pioglitazone, the world ushered in the world's first non-TZD PPAR full agonist
.
On October 19th, according to the latest announcement on the official website of the National Medical Products Administration (NMPA), Microchip's Class 1 new drug, sitaglipta sodium (silapin), was officially approved.
The single drug is suitable for diet control and exercise to improve Blood glucose control in adults with type 2 diabetes
.
Screenshot from NMPA
Sitagliptin
Sitagliptin It is reported that this approval is based on the data of two confirmatory Phase 3 clinical trials published by Microchip Biosciences in ScienceBulletin
.
The results showed that compared with sitagliptin, after 24 weeks of treatment with sitagliptin, the absolute value of glycosylated hemoglobin (HbA1c) was reduced by 1.
In terms of safety, compared with the placebo and sitagliptin control groups, the two dose groups of sitagliptin are basically consistent in the overall incidence and severity of adverse events
.
In the two trials, a lower frequency of side effects related to PPARγ activation in the sitaglipta sodium treatment group, such as edema events and weight gain, was observed, but they were significantly lower than those reported by TZD drugs
Public information shows that Chiglitazar Sodium is a peroxisome proliferator activated receptor (PPAR) full agonist, which can simultaneously activate the three subtype receptors of PPARα, δ and γ, and induce downstream The expression of target genes related to insulin sensitivity, fatty acid oxidation, energy conversion and lipid transport, inhibits PPARγ receptor phosphorylation related to insulin resistance
.
And compared with the first-generation insulin sensitizers represented by thiazolidinedione (TZD), in the treatment of type 2 diabetes, sitaglipta sodium can not only control blood sugar, but also treat the patients’ common lipids.
Metabolic disorders and abnormal blood pressure, which are beneficial to the prevention and control of cardiovascular complications, are new and more comprehensive drug treatments for type 2 diabetes
.
It is worth mentioning that Merck’s sitagliptin phosphate tablets entered the country as early as 2009, and entered the national medical insurance catalog in 2017, and then quickly increased the volume by virtue of medical insurance advantages
.
According to relevant statistics, the sales of sitagliptin phosphate tablets in urban public hospitals and county-level public hospitals in 2020 will be 1.
NASH Potential New Drug
NASH Potential New Drug In addition to being used for type 2 diabetes, from the current clinical results, sitaglipta sodium can also significantly reduce aspartate aminotransferase and alanine aminotransferase, which is expected to become non-alcoholic steatohepatitis/non-alcoholic fatty liver disease (NASH/NAFLD).
) Potential new drugs for treatment
.
"Non-alcoholic fatty liver disease prevention guidelines" pointed out that NAFLD is the most common chronic liver disease in the world, and the incidence of cirrhosis in NASH patients within 10-15 years is as high as 15%-25%, and fatty liver cirrhosis occurs with primary HCC, The probability of liver failure and recurrence of transplanted liver is 30%-40%
.
Among them, non-alcoholic fatty liver disease (NAFLD) is a metabolic stress liver injury closely related to insulin resistance and genetic susceptibility, including non-alcoholic simple steatosis and non-alcoholic steatohepatitis (NASH) , Liver cirrhosis and hepatocellular carcinoma (HCC)
.
In addition, NAFLD patients are usually accompanied by type 2 diabetes, central obesity, hyperlipidemia, hypertension and so on
However, from the perspective of disease progression, NASH mainly occurs in four major stages: fatty liver (a large amount of fat accumulates in liver cells), immune inflammatory response, fibrosis, and cancer
.
Therefore, the current NASH drug development mainly includes targets that affect lipid metabolism, inflammation targets, fibrosis targets, weight loss and other targets
Even with many targets, as of now, only one new NASH drug from Saroglitazar has been approved for marketing in the world
.
It is reported that Saroglitazar is a dual agonist of PPARα and γ, while sitaglipta sodium, as a full PPAR agonist, has a prominent role in regulating glucose and lipid metabolism and a certain anti-inflammatory effect.
summary
summaryIn 2019, there were 116 million diabetic patients in China, of which about 90% were type 2 diabetes, and 56% were still undiagnosed.
In addition, according to EvaluatePharma's forecast, the global NASH drug market will reach US$40 billion in 2025.
Siglipta sodium, as the first non-TZD PPAR full agonist, is also expected to become the next blockbuster potential new drug in the field of NASH after winning type 2 diabetes
