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.

Vildagliptin

Clinical data
Trade names	Galvus, others
Other names	LAF237
AHFS/Drugs.com	UK Drug Information
Pregnancy category	Not recommended
Routes of administration	By mouth
ATC code	A10BH02 (WHO) ,A10BD08 (WHO) (with metformin)
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
IUPAC name (S)-1-[N-(3-Hydroxy-1-adamantyl)glycyl]pyrrolidine-2-carbonitrile
CAS Number	274901-16-5 N
PubChem CID	6918537
IUPHAR/BPS	6310
DrugBank	DB04876 Y
ChemSpider	5293734 Y
UNII	I6B4B2U96P
KEGG	D07080 Y
ChEMBL	ChEMBL142703 Y
CompTox Dashboard (EPA)	DTXSID80881091
ECHA InfoCard	100.158.712
Chemical and physical data
Formula	C17H25N3O2
Molar mass	303.406 g·mol−1
3D model (JSmol)	Interactive image
Solubility in water	Freely Soluble in water
SMILES N#C[C@H]4N(C(=O)CNC13CC2CC(C1)CC(O)(C2)C3)CCC4
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 Y Key:SYOKIDBDQMKNDQ-XWTIBIIYSA-N Y
NY (what is this?)  (verify)

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]