The first imitation drug of vildagliptin tablets will be listed in China soon.

Vildagliptin (Vildagliptine) is a model developed by NovartisDPP-4inhibitors, suitable for treatment2type diabetes, in2011Year8Month officially acquiredCFDAApproved for listing.

Vildagliptin unilateral2018YearH1Performance is6.5billion dollars,2017The annual global performance is12.33billion dollars,2016year11.93Billions of dollars. In our country,DPP-4The market for inhibitors is just starting, with sitagliptin, saxagliptin, vildagliptin, linagliptin and alogliptin entering2017The annual version of the national health insurance catalog, and limited to second-line drugs, is now also included in the provincial and municipal health insurance catalog.

 

glucagon-like peptide1(GLP-1)

glucagon-like peptide1(GLP-1) is by the small intestineLA peptide hormone secreted by cells that promotes the digestion of food.GLP-1It is secreted into the blood vessels, thereby exerting its physiological function. Research shows that,GLP-1Has a variety of physiological functions: ①To induce the transcription of pre-insulin gene and promote the biosynthesis and secretion of insulin;Promote the proliferation and differentiation of β-cells and inhibit the apoptosis of β-cells; ③Inhibit the secretion of glucagon; ④Delay gastric emptying, control appetite, and reduce food intake. from this,GLP-1For the treatment of diabetes, it is possible to control the deterioration of diabetes, and can reduce the risk of weight gain by controlling appetite, so as to make up for some shortcomings of existing anti-diabetic drugs, and has broad application prospects. However, this peptide in vivo will soon be dipeptidyl peptidase (DPP-IV) hydrolysis and inactivation (half-life only2 minleft and right),DPP-Therefore, Ⅳ inhibitors have become the research focus of new anti-diabetic drugs.

 

Drug Introduction

Chinese name: Vilgliptin

English name:Vildagliptine

Trade name: Jia Weile

Molecular formula:C₁₇H₂₅N₃O₂

Vidagliptin is a representative drug of dipeptidyl peptidase inhibitors, which is relatedDPP-IV Competitive binding to form a resurrection to inhibit its activity, thereby increasing the free plasmaGLP-1concentration, play a hypoglycemic effect, and in the control of blood sugar at the same time reverse the deterioration of islet function in patients with diabetes, showing a good prospect.

 

Domestic patent situation

Regarding the patent application of Novartis, the original research company, the vilgliptin compound was first filed on the date of application.1999 Year12Month9day of patent applicationCN1160330CThe application has been authorized to protect the Vilagliptin compound or its pharmaceutically acceptable salts and their use for inhibition.DPP-IV, diabetes, obesity, the patent expires.2019Year12Month9day.

Regarding the crystal form of vilxagliptin, two patent applications of the original research company.CN101238099AandCN101106977ANone of them are authorized, so the original research company does not have patent protection for the Vilagliptin crystal form at present.

With regard to the patent or patent application for the vildagliptin preparation, a number of patents of the original research company protect the preparation or composition of vildagliptin, such.CN101208085BA formulation containing vilxagliptin or a pharmaceutically acceptable salt thereof and hydroxypropyl methylcellulose, microcrystalline cellulose and magnesium stearate is protected;CN101618216BA pharmaceutical compressed tablet or a pharmaceutical direct compression tablet containing granules of vildagliptin or a pharmaceutically acceptable salt thereof is protected;CN101035522BA composition comprising vildagliptin or a pharmaceutically acceptable salt thereof and a glitazone drug and a metformin drug and a use of the composition are protected;CN101277688BProtected contains (1)1.5-20% of vildagliptin or a pharmaceutically acceptable salt thereof and (2)80-98.5% of a composition of metformin or a pharmaceutically acceptable salt thereof.

Patent or patent application for the use of vilxagliptin, the earliest patent of the original research company.CN1160330Cprotected vildagliptin for the treatmentDPP-IV, diabetes, obesity, and then the company applied for the application of vildagliptin to reduce hypoglycemic events and the application of regulating hyperlipidemia, and has been authorized, see patent.CN101267838BandCN100402026C.

Open No.	Patent Name	Application Date	Legal status
CN1160330C	N-Replace2-Cyanopyrrolidine compounds	1999-12-09	Authorization
CN101238099A	Salts of vildagliptin	2006-08-02	Withdrawal
CN101106977A	Formulation and method of direct compression	2006-01-17	Withdrawal
CN101208085B	1-[(3-hydroxyl-Adamantil-1-amino group)-acetyl]-Pyrrolidinyl-2(s)-modified-release formulations of nitriles	2006-06-08	Authorization
CN101618216B	Direct compression formulation and method	2005-01-17	Authorization
CN101035522B	DPP-IV agent,PPARCombination of an antidiabetic agent and metformin	2005-10-21	unpaid annual fee
CN101277688B	Formulation comprising metformin and vildagliptin	2006-09-25	Authorization
CN101267838B	DPP-IVUse of inhibitors to reduce hypoglycemic events	2006-09-18	Authorization
CN100402026C	Use of substituted cyanopyrrolidines and combined preparations containing them for the treatment of hyperlipidemia and related diseases	2003-06-02	unpaid annual fee

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Local pharmaceutical enterprises layout

According to statistics, Nanjing Youke Pharmaceutical, Qilu Pharmaceutical, Tide Pharmaceutical, Haosen Pharmaceutical, Sihuan Pharmaceutical and other companies.7 A domestic generic drug Vilagliptin tablets have entered the production application stage.