Table 2.
GLP-1-based therapeutic peptides.
| Peptide Name | AA Sequence | Development Stage | Reference | |
|---|---|---|---|---|
| GLP-1(1-37) | HDEFERHAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG | N/A | (60) | |
| GLP-1(1-36) | HDEFERHAEGTFTSDVSSYLEGQAAKEFIAWLVKGR | N/A | (60) | |
| GLP-1(7-36) | HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR | N/A | (60) | |
| N-acetyl GLP-1(7-36) | Ac-HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR | Preclinical | (61) | |
| Exendin-4 (Exenatide) | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS | Daily - Approved 2005, Weekly- Approved 2014 (d/c 2021), Phase II-AD/PD (AstraZeneca) | (62–63) | |
| Lixisenatide | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK | Approved 2016-T2DM, Phase II-AD/PD (Sanofi) | (64) | |
| Liraglutide | HAEGTFTSDVSSYLEGQAAK*(Glu-hexadecanoyl-Glu-OH)EFIAWLVRGRG | Approved 2010-T2DM, Approved 2019-Obesity, Phase II-AD/PD, CVD (Novo Nordisk) | (65, 66) | |
| Albiglutide | HGEGTFTSDVSSYLEGQAAKEFIAWLVKGR-{Human Albumin} | Approved 2014 (d/c 2017)-T2DM, Phase II-CVD (GlaxoSmithKline) | (67) | |
| Dulaglutide | HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGGGGGGSGGGGSGGGG{Human IgG4-Fc} | Approved 2014-T2DM, Phase II-CVD, Phase II-AD/PD (Eli Lilly) | (68) | |
| Semaglutide | HXEGTFTSDVSSYLEGQAAK*(Glu-mPEG-17-carboxyheptadecanoyl-Glu-OH)EFIAWLVRGRG | Approved 2017- T2DM, Filed 2021-Obesity, Phase II-CVD (Novo Nordisk) | (69, 70) | |
| Oral Semaglutide (Rybelsus) | HXEGTFTSDVSSYLEGQAAK*(Glu-mPEG-17-carboxyheptadecanoyl-Glu-OH)EFIAWLVRGRG/SNAC | Approved 2020-T2DM (Novo Nordisk) | (71–72) | |
| D-Ala8GLP-1(Lys37) - pentasaccharide | H(DA)EGTFTSDVSSYLEGQAAKEFIAWLVKGRK*(Pentasaccharide) | Preclinical | (73, 74) | |
| [Gln28]exenatide | HGEGTFTSDLSKQMEEEAVRLFIEWLKQGGPSSGAPPPS | Preclinical | (75) | |
| (Val8)GLP-1(GluPAL) | HVEGTFTSDVSSYLEGQAAKEFIAWLVK*(-Glu-PAL)GR | Preclinical | (76) | |
Amino acid sequences are provided in their single-letter abbreviation format. Modifications from native sequences are highlighted by red lettering. Current development stages, associated condition and holding companies (in brackets) are provided (where available) for each. FDA approval dates, and discontinuation date if applicable, are also provided where appropriate. “SNAC” represents formulation with sodium N-[8-(2-hydroxybenzoyl) amino caprylate, an absorption aid. “Ac” represents an N-terminal acetylation, “hexadecanoyl-Glu” and “carboxyheptadecanoyl-Glu” represent fatty acid attachments. “mPEG” indicates mini-polyethylene glycol addition. “PAL” indicates the addition of a palmitic acid chain. A “D” prefix before a residue indicates inclusion of the enantiomer for the naturally-occurring L form of the residue.