Today, China’s National Food and Drug Administration (NMPA) recently announced that Microchip's Class 1 new drug sitaglipta sodium has been approved for marketing.
The single drug is suitable for diet control and exercise to improve blood sugar control in adult patients with type 2 diabetes
This is a new generation of insulin sensitizer candidate drugs independently designed, synthesized, screened and developed by Microchip.
It is also the second new drug approved by Microchip Biotech after Chidamine
Screenshot source: NMPA official website
Type 2 diabetes mellitus (T2DM) is a chronic metabolic disease.
The main manifestation of patients is resistance to insulin, which leads to the inability to fully exert the function of insulin
The existing type 2 diabetes treatment drug thiazolidinedione (TZD) is the first-generation insulin sensitizer.
Although the glucose metabolism is controlled after the medication, the patient's lipid metabolism and energy metabolism have also begun to be disordered
Therefore, this therapy has certain limitations in clinical application
According to microchip bios public information, sitaglipta sodium is a configuration-restricted peroxidase proliferator-activated receptor full agonist, which can moderately activate the three receptor subtypes of PPARα, γ and δ, and inhibit it more effectively CDK5 activated by obesity and inflammatory factors phosphorylates PPARγ, thereby selectively changing the expression of a series of genes related to insulin sensitization
According to the NMPA official website, as a new PPAR full agonist, sitaglipta sodium can not only control blood sugar in the treatment of type 2 diabetes, but also treat the lipid and energy metabolism disorders that are usually associated with patients, thereby benefiting the heart.
The prevention and control of vascular complications is expected to become a new and more comprehensive drug treatment for type 2 diabetes
In July 2021, Microchip issued a press release stating that the journal Science Bulletin published the results of two confirmatory phase 3 clinical trials, which is also the world's first phase 3 PPAR full agonist for the treatment of T2DM Clinical trial report
The two studies were led by two Chinese clinical experts, Professor Ji Linong and Professor Jia Weiping, and aimed to compare the two doses of sitaglipta sodium (32 mg and 48 mg) with a placebo or a control drug (sitagliptin 100 mg).
) Comprehensive efficacy and safety after 24 weeks of treatment
The combined results of two phase 3 trials showed that after 24 weeks of treatment with sitaglipta sodium, the absolute value of glycosylated hemoglobin (HbA1c) was reduced by 1.
32% to 1.
52% compared to before treatment, and both doses showed continuous and clinical significance The role of blood sugar control
The main efficacy endpoint of the trial showed superior efficacy compared with placebo and non-inferior efficacy compared with the control drug
While effectively controlling HbA1c, the two dose groups of sitaglipta sodium showed superiority in fasting blood glucose, insulin resistance index, 2-hour postprandial blood glucose, free fatty acids, triglycerides and a series of secondary efficacy endpoints.
Trends in the efficacy of control drugs
In terms of safety, compared with the placebo and the control group, the two dose groups of sitaglipta sodium 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
Regarding the two Phase 3 clinical results and their significance, Science Bulletin also published a review article by Professor DeFronzo, Director of the Diabetes Center of the University of Texas in the United States
He pointed out that sitaglipta sodium is different in chemical structure from TZD drugs.
In terms of function, it has a balanced agonistic activity on the three receptor subtypes of PPAR.
While effectively and continuously controlling blood sugar, it clearly shows it.
It can improve insulin resistance and reduce triglycerides and free fatty acids
Professor DeFronzo also commented that sitaglipta sodium significantly reduces aspartate aminotransferase and alanine aminotransferase, suggesting its potential in the treatment of non-alcoholic steatohepatitis/non-alcoholic fatty liver disease (NASH/NAFLD)
It is worth mentioning that the research and development of siglita sodium has lasted more than 16 years
The product was approved for drug clinical trials in China in June 2005
Since then, the product has officially entered the stage of clinical research
In September 2019, Microchip Technology submitted a new drug listing application for sitaglipta sodium and was accepted
This time the product was approved in China, and it has been more than 16 years since its first clinical approval
 The National Food and Drug Administration approved the listing of sitaglipta sodium tablets.
Retrieved Oct 19, 2021, from https:// Two phase III clinical results of Sigglita Sodium, a new diabetes drug developed by Microchip Biosciences, were published.
Retrieved Jul 28, 2021, from https://mp.
 China's original innovative drug sitaglipta sodium-improving insulin resistance and reversing abnormal glucose and lipids.
Retrieved Aug 15, 2021, from https://mp.