Vildagliptin

drugbox
IUPAC_name = (2"S")-1-{2- [(3-hydroxy-1-adamantyl)amino] acetyl}
pyrrolidine-2-carbonitrile

---

width = 140
CAS_number = 274901-16-5
ATC_prefix = A10
ATC_suffix = BH02
ATC_supplemental = ATC|A10|BD08 (with metformin) [cite web |url=http://www.whocc.no/atcddd/new_atc_ddd.html#ATCDDD_FINAL |title=ATC/DDD Classification (FINAL): New ATC 5th level codes |date=August 27, 2008 |author=WHO International Working Group for Drug Statistics Methodology |publisher=WHO Collaborating Centre for Drug Statistics Methodology |accessdate=2008-09-05]
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_UK = POM
legal_status =
routes_of_administration = 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-1 and GIPMentlein 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.] 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.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. [http://jcem.endojournals.org/cgi/content/full/89/5/2078 Free Full Text] .]

Novartis has since withdrawn its intent to submit vildagliptin to the FDA, as of July 2008. [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 words2 July 2008The Wall Street Journal Europe] 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.EU approves Novartis diabetes drug Galvus. [http://www.reuters.com/article/companyNews/idUSL0116387320080201 Reuters, February 01, 2008] ]

Combination with metformin

The EMEA has also approved a new oral treatment released by Novartis, called Eucreas, a combination of vildagliptin and metformin.EU approves Novartis's Eucreas diabetes drug. [http://www.reuters.com/article/companyNews/idUSZAT00747520080225 Reuters, February 25, 2008] .]

ee also

*dipeptidyl peptidase-4 (CD26)

References

External links

* - Vildagliptin
* - About DPP-4
* [http://www.forbes.com/2004/01/26/cx_mh_rl_diabetestearsheet_5.html The race to get DPP-4 inhibitors to market] - Forbes.com
* [http://www.forbes.com/finance/2007/03/02/merck-novartis-januvia-pf-ii-in_dk_0302soapbox_inl.html Merck's March Madness] - Forbes.com