Tìm theo
Vildagliptin
Các tên gọi khác (10 ) :
  • EQUA
  • Galvus
  • Jalra
  • LAF 237
  • LAF-237
  • LAF237
  • NVP-LAF-237
  • NVP-LAF237
  • Vildagliptin
  • Xiliarx
dipeptidyl peptidase iv inhibitors, antidiabetic agents
Thuốc Gốc
Small Molecule
CAS: 274901-16-5
ATC: A10BH02
CTHH: C17H25N3O2
PTK: 303.3993
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H25N3O2
Phân tử khối
303.3993
Monoisotopic mass
303.194677059
InChI
InChI=1S/C17H25N3O2/c18-9-14-2-1-3-20(14)15(21)10-19-16-5-12-4-13(6-16)8-17(22,7-12)11-16/h12-14,19,22H,1-8,10-11H2/t12?,13?,14-,16?,17?/m0/s1
InChI Key
InChIKey=SYOKIDBDQMKNDQ-XWTIBIIYSA-N
IUPAC Name
(2S)-1-{2-[(3-hydroxyadamantan-1-yl)amino]acetyl}pyrrolidine-2-carbonitrile
Traditional IUPAC Name
vildagliptin
SMILES
OC12CC3CC(C1)CC(C3)(C2)NCC(=O)N1CCC[C@H]1C#N
Độ hòa tan
1.75e+00 g/l
logP
-0.22
logS
-2.2
pKa (strongest acidic)
14.71
pKa (Strongest Basic)
9.03
PSA
76.36 Å2
Refractivity
82 m3·mol-1
Polarizability
33.17 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. 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.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration with an oral bioavailability of greater than 90%.
▧ Protein binding :
9.3%
▧ Half Life :
The elimination half-life is approximately 90 minutes.
Chỉ Định : Used to reduce hyperglycemia in type 2 diabetes mellitus.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Galvus
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04876
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6918537
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=99443227
ChemSpider
http://www.chemspider.com/Chemical-Structure.5293734.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=11695
PharmGKB
http://www.pharmgkb.org/drug/PA165958346
Wikipedia
http://en.wikipedia.org/wiki/Vildagliptin
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