Semaglutide: difference between revisions
Diff·revision 13 → 14·23:35, 15 Nov 2024
Difference between revision 13 and revision 14 of Semaglutide. 23 lines changed; the page grew by 1,050 bytes.
| Revision 13 — 10:04, 30 Oct 2024 OrforglipronOona (talk) convert the substitution list to a table so the analogues line up 5,608 bytes +30 | Revision 14 — 23:35, 15 Nov 2024 ColdChainCleo (talk) expand §Chemistry and engineering 6,658 bytes +1,050 | ||
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| 12 | | Molecular formula = {{math|C_{187}H_{291}N_{45}O_{59}}} | 12 | | Molecular formula = {{math|C_{187}H_{291}N_{45}O_{59}}} |
| 13 | | Molar mass = 4,113.58 g·mol⁻¹ | 13 | | Molar mass = 4,113.58 g·mol⁻¹ |
| + | 14 | <!-- Pharmacokinetics --> | |
| + | 15 | | Half-life = ≈165 h (7 days) | |
| + | 16 | | Bioavailability, SC = ≈89% | |
| + | 17 | | Albumin binding = >99% | |
| + | 18 | | Time to steady state = 4–5 weeks | |
| 14 | }} | 19 | }} |
| 15 | {{hatnote|For the oral formulation and its absorption enhancer, see [[Oral semaglutide]]. For the drug class, see [[GLP-1 receptor agonist]].}} | 20 | {{hatnote|For the oral formulation and its absorption enhancer, see [[Oral semaglutide]]. For the drug class, see [[GLP-1 receptor agonist]].}} |
| ⋮ | ⋮ | ||
| 35 | The oral formulation is a different pharmacokinetic proposition entirely. Bioavailability is roughly 0.4–1%, achieved by co-formulation with the absorption enhancer sodium N-(8-(2-hydroxybenzoyl)amino)caprylate, and it is critically dependent on dosing in the fasting state with no more than 120 mL of water and a subsequent 30-minute fast. Deviation from those conditions changes exposure severalfold.{{r|knudsen2019}} | 40 | The oral formulation is a different pharmacokinetic proposition entirely. Bioavailability is roughly 0.4–1%, achieved by co-formulation with the absorption enhancer sodium N-(8-(2-hydroxybenzoyl)amino)caprylate, and it is critically dependent on dosing in the fasting state with no more than 120 mL of water and a subsequent 30-minute fast. Deviation from those conditions changes exposure severalfold.{{r|knudsen2019}} |
| 36 | 41 | ||
| + | 42 | == Clinical evidence == | |
| + | 43 | | Trial | Population | Dose | Primary result | | |
| + | 44 | |---|---|---|---| | |
| + | 45 | | SUSTAIN 6 | T2D, high CV risk | 0.5/1.0 mg weekly | MACE HR 0.74 (95% CI 0.58–0.95) | | |
| + | 46 | | STEP 1 | Obesity, no diabetes | 2.4 mg weekly | −14.9% vs −2.4% weight at 68 wk | | |
| + | 47 | | STEP 2 | Obesity with T2D | 2.4 mg weekly | −9.6% vs −3.4% weight at 68 wk | | |
| + | 48 | | SELECT | CVD, overweight, no T2D | 2.4 mg weekly | MACE HR 0.80 (95% CI 0.72–0.90) | | |
| + | 49 | | FLOW | T2D with CKD | 1.0 mg weekly | Kidney outcome HR 0.76 | | |
| + | 50 | ||
| + | 51 | The [[STEP trial programme|STEP]] programme established the obesity indication and the [[SUSTAIN trial programme|SUSTAIN]] programme the glycaemic one; [[SELECT trial|SELECT]] and [[FLOW trial|FLOW]] added the outcome indications.{{r|wilding2021,lincoff2023}} | |
| + | 52 | ||
| 37 | == References == | 53 | == References == |
| 38 | {{reflist}} | 54 | {{reflist}} |
| ⋮ | ⋮ | ||
| 41 | <ref name="wilding2021">Wilding JPH, Batterham RL, Calanna S, et al. "Once-weekly semaglutide in adults with overweight or obesity." ''New England Journal of Medicine'' 384(11):989–1002 (2021). DOI:10.1056/NEJMoa2032183. PMID 33567185.</ref> | 57 | <ref name="wilding2021">Wilding JPH, Batterham RL, Calanna S, et al. "Once-weekly semaglutide in adults with overweight or obesity." ''New England Journal of Medicine'' 384(11):989–1002 (2021). DOI:10.1056/NEJMoa2032183. PMID 33567185.</ref> |
| 42 | <ref name="lincoff2023">Lincoff AM, Brown-Frandsen K, Colhoun HM, et al. "Semaglutide and cardiovascular outcomes in obesity without diabetes." ''New England Journal of Medicine'' 389(24):2221–2232 (2023). PMID 37952131.</ref> | 58 | <ref name="lincoff2023">Lincoff AM, Brown-Frandsen K, Colhoun HM, et al. "Semaglutide and cardiovascular outcomes in obesity without diabetes." ''New England Journal of Medicine'' 389(24):2221–2232 (2023). PMID 37952131.</ref> |
| + | 59 | ||
| + | 60 | == See also == | |
| + | 61 | * [[GLP-1 receptor agonist]] | |
| + | 62 | * [[Tirzepatide]] | |
| + | 63 | * [[Liraglutide]] | |
| + | 64 | * [[Oral semaglutide]] | |
| + | 65 | * [[STEP trial programme]] | |
| 43 | 66 | ||
| 44 | {{DEFAULTSORT:Semaglutide}} | 67 | {{DEFAULTSORT:Semaglutide}} |