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Vildagliptin

Chemical compound

Summary

Chemical compound

FieldValue
Verifiedfieldschanged
Watchedfieldschanged
verifiedrevid470630169
imageVildagliptin.svg
image_classskin-invert-image
altSkeletal formula
image2Vildagliptin-3D-balls.png
image_class2bg-transparent
alt2Ball-and-stick model
tradenameGalvus, others
Drugs.com
DailyMedID
pregnancy_AU
pregnancy_categoryNot recommended
routes_of_administrationBy mouth
ATC_prefixA10
ATC_suffixBH02
ATC_supplemental, (with metformin)
legal_AU
legal_BR
legal_CA
legal_DE
legal_NZ
legal_UKPOM
legal_US
legal_EURx-only
legal_EU_comment
legal_UN
legal_statusRx-only
bioavailability85%
protein_bound9.3%
metabolismMainly hydrolysis to inactive metabolite; CYP450 not appreciably involved
elimination_half-life2 to 3 hours
excretionKidney
CAS_number_Ref
CAS_number274901-16-5
PubChem6918537
IUPHAR_ligand6310
DrugBank_Ref
DrugBankDB04876
ChemSpiderID_Ref
ChemSpiderID5293734
UNII_Ref
UNIII6B4B2U96P
KEGG_Ref
KEGGD07080
ChEMBL_Ref
ChEMBL142703
synonymsLAF237
IUPAC_name(S)-1-[N-(3-Hydroxy-1-adamantyl)glycyl]pyrrolidine-2-carbonitrile
C17H=25N=3O=2
SMILESN#C[C@H]4N(C(=O)CNC13CC2CC(C1)CC(O)(C2)C3)CCC4
StdInChI_Ref
StdInChI1S/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
StdInChIKey_Ref
StdInChIKeySYOKIDBDQMKNDQ-XWTIBIIYSA-N
solubilityFreely Soluble in water

| Drugs.com =

| elimination_half-life = 2 to 3 hours

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. Vildagliptin inhibits the inactivation of GLP-1 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.

The most common side effects include dizziness.

It was approved by the European Medicines Agency (EMA) in 2007. 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.

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

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.

Adverse effects

The most common side effects include dizziness.

References

References

  1. (26 September 2007). "Galvus EPAR".
  2. (June 1993). "Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum". European Journal of Biochemistry.
  3. (December 2008). "Vildagliptin: a new oral treatment for type 2 diabetes mellitus". Vascular Health and Risk Management.
  4. (February 25, 2008). "EU approves Novartis's Eucreas diabetes drug". Reuters.
  5. (May 2004). "Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes". The Journal of Clinical Endocrinology and Metabolism.
Wikipedia Source

This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page.

dipeptidyl-peptidase-4-inhibitors pyrrolidines nitriles drugs-developed-by-novartis carboxamides adamantanes tertiary-alcohols
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