Dipiaron
The modern approach to the treatment of diabetes requires simultaneous exposure to several mechanisms contributing to hyperglycemia.
New directions in the search for drugs for the treatment of diabetes mellitus (DM) are the search for ways to optimize carbohydrate metabolism, regulation of insulin signaling pathways, as well as effects on the physiological mechanisms of insulin secretion (the latter is currently the most promising area of research).
Dipiaron is an oral agonist of the GPR119 receptor. The GPR119 receptor is a new validated target for T2DM therapy, metabolic syndrome and obesity. Dipiaron influences on the secretion of glucagon-like peptide type 1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP).
Dipiaron could be highly effective in monotherapy and in combination with DPP-4 inhibitors. It has a more convenient route of administration than many synthetic GLP-1 agonists in the second line of T2DM therapy.
There are no analogues of the Dipiaron on the world market - this is an innovative development of Russian science. The drug was developed according to the Pharma-2020 program, by combining the efforts of leading physicians and pharmacologists of the Volgograd State Medical University in partnership with the ChemRar Group of Companies.
How does it work?
Stimulation of the secretion of endogenous GLP-1 and GIP on specialized cells of the gastrointestinal tract
Stimulation of incretin production triggers insulin production and helps lower glucose levels
Improvement of the preservation and regeneration of β-cells, increase in the number of insulin-positive β-endocrinocytes in the pancreatic islets in all parts of the gland
Incretin-regulating action
Insulin production
Influence on the pancreas
Reduction of food intake by slowing gastrointestinal motility and reducing appetite
Weight loss
Key advantages
Original mechanism of action
Stimulation of the GPR119 receptor only on K- and L-cells of the intestine, but not in the pancreas
Security
Potentially high safety profile, no risk of systemic side effects due to low systemic availability
Reducing the number of complications
A pronounced preventive effect of complications of the cardiovascular system is expected and, as a result, a decrease in the risk of disability
Preclinical studies
In vitro and in vivo preclinical studies of the efficacy and safety of the drug were performed. The results of preclinical trials have shown that Dipiaron:
- is non-toxic and has a high safety profile
- stimulates the secretion of GLP-1 and insulin, helps to reduce glucose levels
- stimulates an increase in the number and size of pancreatic islets
- shows endothelial and cerebroprotective action
- promotes weight loss, works equally effectively in both obese and non-obese animals
Clinical trials
Current work: manufacturing of clinical batches, complection of documents for phase I clinical trial approval.
Phase I clinical trial is conducted with the participation of healthy volunteers.
It is planned to determine the range of safe doses for subsequent studies of efficacy and safety in patients, as well as to preliminarily evaluate the effect of Dipiaron on biomarkers.
It is planned to determine the range of safe doses for subsequent studies of efficacy and safety in patients, as well as to preliminarily evaluate the effect of Dipiaron on biomarkers.
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