According to the "Chinese Guidelines for the Prevention and Treatment of Type 2 Diabetes (2020 Edition)," the incidence of type 2 diabetes in China has been steadily increasing in recent years. From 0.67% in 1980 to 11.2% in 2017, the incidence has increased several tens of times. Among them, type 2 diabetes (T2DM) accounts for over 90%, with a higher prevalence in males (12.1%) than in females (10.3%), and variations exist among different ethnic groups and regions. Although the prevalence of diabetes is high, the awareness rate is only 36.5%, the treatment rate is only 32.2%, and the control rate of treated patients is 49.2%. While there have been improvements, these rates still remain at very low levels.
Like all chronic diseases, the treatment of diabetes must consider patient compliance, especially when multiple drug therapies fail to meet standards. Studies have shown that the complexity of treatment regimens is one of the important factors affecting compliance. The more complex the treatment plan, the poorer the blood sugar control in diabetic patients, leading to more suffering, more complications, and a heavier disease burden.
In order to effectively address the low blood sugar control rate caused by poor compliance, China has taken the lead in introducing the independently developed first biweekly ultra-long-acting dipeptidyl peptidase-4 inhibitor (DPP-4i) - HSK7653. It is reported that DPP-4i has been widely used in the treatment of diabetes. By inhibiting DPP-4 activity, it reduces the inactivation of glucagon-like peptide-1 (GLP-1) and increases the level of GLP-1 in the blood within the physiological range. GLP-1 can stimulate pancreatic β cells to secrete insulin, inhibit pancreatic α cells from secreting glucagon, suppress the appetite center, delay gastric emptying, promote pancreatic β cell proliferation, and reduce blood sugar through various mechanisms.
Studies have shown that compared to traditional DPP-4i drugs, the mechanism of action, efficacy, and safety advantages of HSK7653 are more pronounced. Based on clinical research data before its market launch, HSK7653 has a half-life of over 100 hours, ensuring a long dosing interval of once every two weeks. It can achieve sustained DPP-4 inhibition, with a DPP-4 inhibition rate of over 80% on the 14th day, comparable to the efficacy of Japanese formulations. Additionally, HSK7653 has no impact on major CYP enzyme subtypes, can be used in combination therapy or to treat multiple comorbidities simultaneously, and does not increase drug exposure in patients with impaired liver or kidney function, eliminating the need to adjust the dosage.
Reportedly, this new drug was developed by Haisco Pharmaceutical Group. Researchers added a fluorine group to the structure of alogliptin, introducing a trifluoromethyl (CF3) group at the 6th position on the tetrahydrofuran ring at an unconventional chemical site, successfully developing HSK7653.
