Vildagliptin
{{drugbox
| IUPAC_name = (2S)-1-{2-[(3-hydroxy-1-adamantyl)amino]acetyl}
pyrrolidine-2-carbonitrile
| image = Vildagliptin.svg
| width = 140px
| CAS_number = 274901-16-5
| ATC_prefix = A10
| ATC_suffix = BH02
| PubChem = 6918537
| DrugBank =
| C = 17 |H = 25 |N = 3 |O = 2
| molecular_weight = 303.399 g/mol
| bioavailability = 85%
| protein_bound = 9.3%
| metabolism = Mainly hydrolysis to inactive metabolite; CYP450 not appreciably involved
| elimination_half-life = 2 to 3 hours
| excretion = Renal
| pregnancy_category = Not recommended
| legal_status =
| routes_of_administration = Oral
}}
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overview
Vildagliptin, previously identified as LAF237, is a new oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucaon release by the alpha cells of the islets of Langerhans in the pancreas.
It is currently in clinical trials and has been shown to reduce hyperglycemia in type 2 diabetes mellitus.[1]
Vildagliptin has been submitted to the U.S. Food and Drug Administration for approval, and will be marketed as Galvus by Novartis. The Food and Drug Administration demanded additional clinical data before it can approve vildagliptin including extra evidence that skin lesions and kidney impairment seen during an early study on animals have not occurred in human trials. Vildagliptin is currently approved for use in the European Union, although it is not yet marketed. The recent finding of liver toxicity problems among clinical trial patients[2] could delay the European debut of this drug.
Dipeptidyl peptidase-4's role in blood glucose regulation is thought to be through inactivation of GIP[3] and GLP-1.[1][3]
See also
- dipeptidyl peptidase-4 (CD26)
References
- ↑ 1.0 1.1 Ahren B, Landin-Olsson M, Jansson PA, Svensson M, Holmes D, Schweizer A. Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes. J Clin Endocrinol Metab. 2004 May;89(5):2078-84. PMID 15126524. Free Full Text.
- ↑ Novartis Diabetes Drug Delayed The Wall Street Journal Online, November 7, 2007.
- ↑ 3.0 3.1 Mentlein R, Gallwitz B, Schmidt WE. 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. Eur J Biochem. 1993 Jun 15;214(3):829-35. PMID 8100523.
External links
- Banting and Best Diabetes Centre at UT laf237 - Vildagliptin
- Banting and Best Diabetes Centre at UT dp_iv - About DPP-4
- The race to get DPP-4 inhibitors to market - Forbes.com
- Merck's March Madness - Forbes.com