Semaglutide, oral — compound monograph
GLP-1 receptor agonist, oral formulation with absorption enhancer. Approved. The Institute assesses 3 outcomes for this compound and grades the strongest at high certainty.
§1Identification and status
§1.1Nomenclature
- Preferred name
- Semaglutide, oral
- Compound class
- GLP-1 receptor agonist, oral formulation with absorption enhancer
- Assessment series
- Incretin receptor agonists
- Synonyms and codes
- NN9924 · oral semaglutide · Rybelsus (trade) · semaglutide with SNAC
- Route as evaluated
- Oral once daily, fasted, with no more than 120 mL of water and at least 30 minutes before other intake
§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
- 910463-68-2 (active moiety)
- Molecular formula
- C187H291N45O59 (active moiety)
- Average mass
- 4113.58
- Monoisotopic mass
- 4111.10
- ATC classification
- A10BJ06
§1.3Sequence and structural notes
The peptide is unchanged. SNAC raises local gastric pH and transiently increases transcellular permeability in a small region of gastric mucosa, allowing absorption of an intact 4 kDa peptide at low but reproducible efficiency.
§1.4Assessment status
The Institute assesses Semaglutide, oral across 3 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 Semaglutide, oral, ordered by certainty. Each row links to the per-indication evidence extract.
| Indication | Effect as recorded | Certainty | Trials |
|---|---|---|---|
| Type 2 diabetes mellitus | −1.2 to −1.4 % HbA1c at 26 weeks with 14 mg versus placebo | High | 2 |
| Atherosclerotic cardiovascular disease and cardiovascular risk reduction | MACE hazard ratio 0.79 (non-inferiority design) in PIONEER 6; 0.86 in the event-driven SOUL trial | Moderate | 2 |
| Obesity and overweight in adults | −15.1 % body weight with oral 50 mg at 68 weeks versus −2.4 % with placebo | 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.