Lixisenatide
| Clinical data | |
|---|---|
| Trade names | Lyxumia |
| Licence data | EMA:Link |
| Legal status |
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| Routes of administration | Subcutaneous injection |
| Identifiers | |
| CAS Number | 827033-10-3 |
| ATC code | A10BX10 |
| PubChem | CID 16139342 |
| IUPHAR/BPS | 7387 |
| ChemSpider | 17295846 |
| ChEBI | CHEBI:85662 |
| Chemical data | |
| Formula | C215H347N61O65S |
| Molar mass | 4858.49 g/mol |
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Lixisenatide (trade name Lyxumia) is a once-daily injectable GLP-1 receptor agonist for the treatment of diabetes, discovered by Zealand Pharma A/S of Denmark and licensed and developed by Sanofi.[1] Lixisenatide was accepted for review by the US FDA on February 19, 2013, and approved by the European Commission on February 1, 2013.[2] 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.
Mechanism of action
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 used 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.
Physical and chemical properties
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:[3]
- H–His–Gly–Glu–Gly–Thr–Phe–Thr–Ser–Asp–Leu–Ser–Lys–Gln–Met–Glu–Glu–Glu–Ala–Val–Arg–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
- ↑ 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.
- ↑ "Sanofi New Drug Application for Lixisenatide Accepted for Review by FDA". Drugs.com/PR Newsire. 19 February 2013.
- ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended INN: List 61" (PDF). WHO Drug Information 23 (1): 66f. 2009.
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