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Vildagliptin

Chemical compound From Wikipedia, the free encyclopedia

Vildagliptin

Vildagliptin, sold under the brand name Galvus among others, is an oral anti-hyperglycemic agent (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs.[1] Vildagliptin inhibits the inactivation of GLP-1[2][3] and GIP[3] by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucagon release by the alpha cells of the islets of Langerhans in the pancreas.

Quick Facts Clinical data, Trade names ...
Vildagliptin
Thumb
Thumb
Clinical data
Trade namesGalvus, others
Other namesLAF237
AHFS/Drugs.comUK Drug Information
Pregnancy
category
  • Not recommended
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • UK: POM (Prescription only)
  • EU: Rx-only[1]
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability85%
Protein binding9.3%
MetabolismMainly hydrolysis to inactive metabolite; CYP450 not appreciably involved
Elimination half-life2 to 3 hours
ExcretionKidney
Identifiers
  • (S)-1-[N-(3-Hydroxy-1-adamantyl)glycyl]pyrrolidine-2-carbonitrile
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.158.712
Chemical and physical data
FormulaC17H25N3O2
Molar mass303.406 g·mol−1
3D model (JSmol)
Solubility in waterFreely Soluble in water
  • N#C[C@H]4N(C(=O)CNC13CC2CC(C1)CC(O)(C2)C3)CCC4
  • 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 Y
  • Key:SYOKIDBDQMKNDQ-XWTIBIIYSA-N Y
 NY (what is this?)  (verify)
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The most common side effects include dizziness.[1]

It was approved by the European Medicines Agency (EMA) in 2007.[4] The European Medicines Agency has also approved a combination of vildagliptin and metformin, vildagliptin/metformin (Eucreas by Novartis) as an oral treatment for type-2 diabetes.[5]

Vildagliptin has been shown to reduce hyperglycemia in type 2 diabetes mellitus.[2]

Medical uses

Vildagliptin is indicated, as an adjunct to diet and exercise, to improve glycemic control in adults with type 2 diabetes as monotherapy in people in whom metformin is inappropriate due to contraindications or intolerance; and in combination with other medicinal products for the treatment of diabetes, including insulin, when these do not provide adequate glycemic control.[1]

Adverse effects

The most common side effects include dizziness.[1]

References

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