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药品详细

Vildagliptin(维格列汀)

化学结构式图
中文名
维格列汀
英文名
Vildagliptin
分子式
C17H25N3O2
化学名
(2S)-1-{2-[(3-hydroxyadamantan-1-yl)amino]acetyl}pyrrolidine-2-carbonitrile
分子量
Average: 303.3993
Monoisotopic: 303.194677059
CAS号
274901-16-5
ATC分类
A10B Oral Blood Glucose Lowering Drugs, Excl. Insulins
药物类型
small molecule
阶段
approved
商品名
Galvus;
同义名
EQUA;Galvus;Jalra;LAF 237;LAF237;NVP-LAF-237;NVP-LAF237;Xiliarx;
基本介绍

Vildagliptin, previously identified as LAF237, is a new oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucaon release by the alpha cells of the islets of Langerhans in the pancreas. It is currently in clinical trials in the U.S. and has been shown to reduce hyperglycemia in type 2 diabetes mellitus. While the drug is still not approved for use in the US, it was approved in Feb 2008 by European Medicines Agency for use within the EU and is listed on the Australian PBS with certain restrictions.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Balas B, Baig MR, Watson C, Dunning BE, Ligueros-Saylan M, Wang Y, He YL, Darland C, Holst JJ, Deacon CF, Cusi K, Mari A, Foley JE, DeFronzo RA: The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab. 2007 Apr;92(4):1249-55. Epub 2007 Jan 23. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Adamantanes
    Substructures
    • Hydroxy Compounds
    • Aliphatic and Aryl Amines
    • Amino Ketones
    • Nitriles and Derivatives
    • Pyrrolidines
    • Adamantanes
    • Cyanides
    • Alcohols and Polyols
    • Heterocyclic compounds
    • Carboxamides and Derivatives
    • Cyclooctane and Derivatives
    适应症
    Diabetes 糖尿病;
    药理
    Indication Used to reduce hyperglycemia in type 2 diabetes mellitus.
    Pharmacodynamics Vildagliptin belongs to a class of orally active antidiabetic drugs (DPP-IV inhibitors) that appear to have multiple functional benefits beyond simple blood-glucose control. One of these is a potential protective effect on pancreatic beta cells, which deteriorate in diabetes. Vildagliptin appears to be safe, very well tolerated, and efficacious. Following a meal, gut incretin hormones are released. The most important incretin hormones are GLP-1 and glucose-dependent insulinotropic polypeptide (GIP). These hormones, secreted in the human small intestine, are responsible for insulin release due to increased glucose levels. In contrast to agents that promote insulin secretion via glucose-independent mechanisms, GLP-1's dependence on glucose concentration is considered beneficial due to a lower risk of hypoglycemia. GLP-1 also inhibits glucagon secretion and increases beta cell mass by stimulating proliferation and neogenesis. However, the clinical utility of GLP-1 is limited by its short half-life (2 minutes). GLP-1 is rapidly degraded by the proteolytic enzyme DPP-IV. To enhance GLP-1 activity, inhibition of the DPP-IV enzyme is emerging as a novel therapeutic approach in the treatment of diabetes. Administration of vildagliptin enhances GLP-1's ability to produce insulin in response to elevated concentrations of blood glucose, inhibit the release of glucagon following meals, slow the rate of nutrient absorption into the bloodstream, slow the rate of gastric emptying, and reduce food intake.
    Mechanism of action Vildagliptin inhibits dipeptidyl peptidase-4 (DPP-4). This in turn inhibits the inactivation of GLP-1 by DPP-4, allowing GLP-1 to potentiate the secretion of insulin in the beta cells. Dipeptidyl peptidase-4's role in blood glucose regulation is thought to be through degradation of GIP and the degradation of GLP-1.
    Absorption Rapidly absorbed following oral administration with an oral bioavailability of greater than 90%.
    Volume of distribution Not Available
    Protein binding 9.3%
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life The elimination half-life is approximately 90 minutes.
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties Not Available
    Predicted Properties
    Property Value Source
    water solubility 1.75e+00 g/l ALOGPS
    logP 1.12 ALOGPS
    logP -0.22 ChemAxon
    logS -2.2 ALOGPS
    pKa (strongest acidic) 14.71 ChemAxon
    pKa (strongest basic) 9.03 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 76.36 ChemAxon
    rotatable bond count 3 ChemAxon
    refractivity 82 ChemAxon
    polarizability 33.17 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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