Lixisenatide

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Lixisenatide
Clinical data
Trade names Lyxumia
Licence data EMA:Link
Legal status POM (UK)
Routes Subcutaneous
Identifiers
CAS number 827033-10-3
ATC code A10BX10
PubChem CID 16139342
ChemSpider 17295846
Chemical data
Formula C215H347N61O65S 
Mol. mass 4858.49 g/mol

Lixisenatide (intended trade name Lyxumia) is a once-daily injectable GLP-1 receptor agonist discovered by Zealand Pharma A/S o Denmark and licensed and developed by Sanofi.[1] As of September 2010 it is in clinical trials for diabetes.[2] Lixisenatide was accepted for review by the US FDA on February 19, 2013, and approved by the European Commission on February 1, 2013.[3] On September 12, 2013, Sanofi delayed the approval process in the US, citing internal data from a cardiovascular risk study. The drug will likely be resubmitted for approval in 2015.

GLP-1 is a naturally-occurring peptide that is released within minutes of eating a meal. It is known to suppress glucagon secretion from pancreatic alpha cells and stimulate insulin secretion by pancreatic beta cells. GLP-1 receptor agonists are in development as an add-on treatment for type 2 diabetes and their use is endorsed by the European Association for the Study of Diabetes, the American Diabetes Association, the American Association of Clinical Endocrinologists and the American College of Endocrinology.

The GetGoal phase III clinical program will provide data for lixisenatide in adults with type 2 diabetes treated with various oral anti-diabetic agents or insulin. With ten trials in the program, GetGoal started in May 2008 and has enrolled more than 4,300 patients. To date, GetGoal-X, GetGoal-L, GetGoal-L Asia, GetGoal-Mono, GetGoal-S and GetGoal-F1 have reported positive top-line results supporting efficacy and safety for lixisenatide.

Chemistry[edit]

Lixisenatixe has been described as "des-38-proline-exendin-4 (Heloderma suspectum)-(1–39)-peptidylpenta-L-lysyl-L-lysinamide", meaning it is derived from the first 39 amino acids in the sequence of the peptide exendin-4, found in the Gila monster (Heloderma suspectum), omitting proline at position 38 and adding six lysine residues. Its complete sequence is:[4]

H–HisGlyGlu–Gly–ThrPhe–Thr–SerAspLeu–Ser–LysGlnMet–Glu–Glu–Glu–AlaValArg–Leu–Phe–Ile–Glu–Trp–Leu–Lys–Asn–Gly–Gly–Pro–Ser–Ser–Gly–Ala–Pro–Pro–Ser–Lys–Lys–Lys–Lys–Lys–Lys–NH2

References[edit]

  1. ^ Christensen, M; Knop, FK; Holst, JJ; Vilsboll, T (2009). "Lixisenatide, a novel GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus". IDrugs : the investigational drugs journal 12 (8): 503–13. PMID 19629885. 
  2. ^ "Positive Phase III Data for Two Separate Type 2 Diabetes Therapies Reported at ESAD". Genetic Engineering & Biotechnology News. 20 September 2010. 
  3. ^ "Sanofi New Drug Application for Lixisenatide Accepted for Review by FDA". Drugs.com/PR Newsire. 19 February 2013. 
  4. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended INN: List 61". WHO Drug Information 23 (1): 66f. 2009.