Exenatide — compound monograph
GLP-1 receptor agonist (exendin-based, short- and extended-release). Approved. The Institute assesses 4 outcomes for this compound and grades the strongest at high certainty.
§1Identification and status
§1.1Nomenclature
- Preferred name
- Exenatide
- Compound class
- GLP-1 receptor agonist (exendin-based, short- and extended-release)
- Assessment series
- Incretin receptor agonists
- Synonyms and codes
- AC2993 · exendin-4 · synthetic exendin-4 · Byetta (trade) · Bydureon (trade)
- Route as evaluated
- Subcutaneous twice daily (immediate release) or once weekly (poly(lactide-co-glycolide) microsphere extended release)
§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
- 141758-74-9
- Molecular formula
- C184H282N50O60S
- Average mass
- 4186.57
- Monoisotopic mass
- 4184.63
- ATC classification
- A10BJ01
§1.3Sequence and structural notes
A 39-residue peptide identical to exendin-4, isolated originally from the venom of Heloderma suspectum. It shares 53 % identity with human GLP-1 and is naturally resistant to DPP-4 because of a glycine at position 2. The C-terminal Pro-Ser-rich tail contributes to receptor binding and to stability.
§1.4Assessment status
The Institute assesses Exenatide across 4 indications and grades the strongest of them at high certainty. Holds a marketing authorisation for at least one indication in at least one jurisdiction.
Table 1. Assessed outcomes for Exenatide, 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 0.91 — non-inferior to placebo but not superior | High | 1 |
| Type 2 diabetes mellitus | −0.8 to −1.9 % HbA1c depending on presentation and background therapy | High | 3 |
| Delayed gastric emptying and gastrointestinal motility effects | Marked acute delay in gastric emptying that shows partial tachyphylaxis with continued twice-daily dosing | Moderate | 1 |
| Obesity and overweight in adults | −2.3 to −3.6 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.