Lixisenatide — compound monograph
GLP-1 receptor agonist (exendin-based, short-acting). Approved. The Institute assesses 3 outcomes for this compound and grades the strongest at moderate certainty.
§1Identification and status
§1.1Nomenclature
- Preferred name
- Lixisenatide
- Compound class
- GLP-1 receptor agonist (exendin-based, short-acting)
- Assessment series
- Incretin receptor agonists
- Synonyms and codes
- AVE0010 · ZP10 · lixisenatide (INN) · Adlyxin (trade) · Lyxumia (trade)
- Route as evaluated
- Subcutaneous once daily before the first meal of the day
§1.2Chemistry
Chemical identifiers are reproduced where they are public. Where a structure has not been published the monograph records not disclosed rather than constructing one.[1]
- CAS registry number
- 320367-13-3
- Molecular formula
- C215H347N61O65S
- Average mass
- 4858.49
- Monoisotopic mass
- 4856.30
- ATC classification
- A10BJ03
§1.3Sequence and structural notes
A 44-residue exendin-4 derivative in which the C-terminal proline is deleted and six lysine residues are appended. The polylysine tail raises the isoelectric point and alters pharmacokinetics, producing a short-acting agent with a pronounced prandial profile.
§1.4Assessment status
The Institute assesses Lixisenatide across 3 indications and grades the strongest of them at moderate certainty. Holds a marketing authorisation for at least one indication in at least one jurisdiction.
Table 1. Assessed outcomes for Lixisenatide, ordered by certainty. Each row links to the per-indication evidence extract.
| Indication | Effect as recorded | Certainty | Trials |
|---|---|---|---|
| Atherosclerotic cardiovascular disease and cardiovascular risk reduction | MACE hazard ratio 1.02 — neutral | High | 1 |
| Type 2 diabetes mellitus | −0.7 to −0.9 % HbA1c at 24 weeks with pronounced postprandial glucose reduction | High | 3 |
| Obesity and overweight in adults | −1.8 to −2.7 kg | Moderate | 1 |
| Effects are reproduced as the contributing trials reported them. Where a confidence interval is held it appears on the per-indication extract rather than in this summary table. | |||
References cited on this page
References are numbered in order of first citation in this document. Each superscript in the text links to its entry below.
- International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use. ICH Q6B Specifications: Test Procedures and Acceptance Criteria for Biotechnological/Biological Products. ICH Harmonised Tripartite Guideline 1999;Step 4 version. identifier not held by the Institute
Identifiers are reproduced only where the Institute holds them. Where a digital object identifier or PubMed identifier is not shown, the Institute has recorded the journal and year and has not constructed an identifier.