Vildagliptin

Vildagliptin
Clinical data
Trade names	Galvus, Zavamet others
Other names	LAF237
AHFS/Drugs.com	UK Drug Information
License data	EU EMA: by INN;
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; 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 ;
PubChem CID	6918537;
IUPHAR/BPS	6310;
DrugBank	DB04876 ;
ChemSpider	5293734 ;
UNII	I6B4B2U96P;
KEGG	D07080 ;
ChEMBL	ChEMBL142703 ;
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 mg/mL (20 °C)
	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 ; Key:SYOKIDBDQMKNDQ-XWTIBIIYSA-N ;
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Vildagliptin, sold under the brand name Galvus and 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^[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.

It was approved by the EMA in 2007.^[4]

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

^ WHO International Working Group for Drug Statistics Methodology (August 27, 2008). "ATC/DDD Classification (FINAL): New ATC 5th level codes". WHO Collaborating Centre for Drug Statistics Methodology. Archived from the original on May 6, 2008. Retrieved September 5, 2008.
^ ^a ^b 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.
^ ^a ^b 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.
^ 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.

[1] WHO International Working Group for Drug Statistics Methodology (August 27, 2008). "ATC/DDD Classification (FINAL): New ATC 5th level codes". WHO Collaborating Centre for Drug Statistics Methodology. Archived from the original on May 6, 2008. Retrieved September 5, 2008.

[ahren-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.

[mentlein-3] 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.

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