Saxagliptin
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Saxagliptin
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| Systematic (IUPAC) name | |
| (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl) acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile |
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| Identifiers | |
| CAS number | ? |
| ATC code | ? |
| PubChem | 6451162 |
| Chemical data | |
| Formula | C18H25N3O2 |
| Mol. weight | 315.41 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Saxagliptin (rINN), previously identified as BMS-477118, is a new oral hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs.[1] It was developed by Bristol-Myers Squibb. The trade name under which saxagliptin will be marketed has not yet been released.
It is currently in clinical trials for the treatment of type 2 diabetes mellitus.[2]
Dipeptidyl peptidase-4's role in blood glucose regulation is thought to be through degradation of GIP[3] and the degradation of GLP-1.[3][4]
[edit] See also
[edit] References
- ^ Augeri D, Robl J, Betebenner D, Magnin D, Khanna A, Robertson J, Wang A, Simpkins L, Taunk P, Huang Q, Han S, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel G, Egan D, Marcinkeviciene J, Chang S, Biller S, Kirby M, Parker R, Hamann L (2005). "Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.". J Med Chem 48 (15): 5025-37. PMID 16033281.
- ^ ClinicalTrails.gov. Saxagliptin Treatment in Subjects With Type 2 Diabetes Who Are Not Controlled With Diet and Exercise. ClinicalTrials.gov Identifier: NCT00121641. Available at: http://www.clinicaltrials.gov/show/NCT00121641. Accessed on: October 19, 2006.
- ^ 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.
- ^ 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.
[edit] External links
- About DPP-4 - glucagon.com
- The race to get DPP-4 inhibitors to market - Forbes.com
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