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Vildagliptin
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| Systematic (IUPAC) name | |
| (2S)-1-{2-[(3-hydroxy-1-adamantyl)amino]acetyl} pyrrolidine-2-carbonitrile |
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| Identifiers | |
| CAS number | |
| ATC code | A10 A10 (with metformin)1 |
| PubChem | |
| Chemical data | |
| Formula | C17H25N3O2 |
| Mol. mass | 303.399 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 85% |
| Protein binding | 9.3% |
| Metabolism | Mainly hydrolysis to inactive metabolite; CYP450 not appreciably involved |
| Half life | 2 to 3 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
Not recommended |
| Legal status | |
| Routes | Oral |
Vildagliptin (previously identified as LAF237, trade name Galvus) 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-123 and GIP3 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 has been shown to reduce hyperglycemia in type 2 diabetes mellitus.2
Novartis has since withdrawn its intent to submit vildagliptin to the FDA, as of July 2008.4 The Food and Drug Administration had demanded additional clinical data before it could approve vildagliptin including extra evidence that skin lesions and kidney impairment seen during an early study on animals have not occurred in human trials.
While the drug is still not approved for use in the US, it has been approved by European Medicines Agency for use within the EU.5
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Combination with metformin
The EMEA has also approved a new oral treatment released by Novartis, called Eucreas, a combination of vildagliptin and metformin.6
See also
References
- ^ 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. Retrieved on 2008-09-05.
- ^ a b 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.
- ^ a b 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.
- ^ Focus on Health: Drug makers say FDA slows U.S. pipeline --- Emphasis on safety, side effects grows; swing of pendulum? By Avery Johnson and Ron Winslow 2180 words 2 July 2008 The Wall Street Journal Europe
- ^ EU approves Novartis diabetes drug Galvus.Reuters, February 01, 2008
- ^ EU approves Novartis's Eucreas diabetes drug. Reuters, February 25, 2008.
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
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