Vildagliptin

Last updated

Vildagliptin
Vildagliptin.svg
Vildagliptin-3D-balls.png
Clinical data
Trade names Galvus, others
Other namesLAF237
AHFS/Drugs.com UK 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
Bioavailability 85%
Protein binding 9.3%
Metabolism Mainly hydrolysis to inactive metabolite; CYP450 not appreciably involved
Elimination half-life 2 to 3 hours
Excretion Kidney
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 InfoCard 100.158.712 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C17H25N3O2
Molar mass 303.406 g·mol−1
3D model (JSmol)
Solubility in water Freely 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 Yes check.svgY
  • Key:SYOKIDBDQMKNDQ-XWTIBIIYSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

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.

Contents

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

  1. 1 2 3 4 5 "Galvus EPAR". European Medicines Agency (EMA). 26 September 2007. Retrieved 20 February 2025. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  2. 1 2 Ahrén B, Landin-Olsson M, Jansson PA, Svensson M, Holmes D, Schweizer A (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. 89 (5): 2078–2084. doi: 10.1210/jc.2003-031907 . PMID   15126524.
  3. 1 2 Mentlein R, Gallwitz B, Schmidt WE (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. 214 (3): 829–835. doi: 10.1111/j.1432-1033.1993.tb17986.x . PMID   8100523.
  4. ↑ Mathieu C, Degrande E (December 2008). "Vildagliptin: a new oral treatment for type 2 diabetes mellitus". Vascular Health and Risk Management. 4 (6): 1349–1360. doi: 10.2147/vhrm.s3005 . PMC   2663430 . PMID   19337548.
  5. ↑ "EU approves Novartis's Eucreas diabetes drug". Reuters. 25 February 2008.
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