Table 1. Stable GLP-1 Receptor Agonists.
| manufacturer/developer | dosage | plasma half-life | status | ref | |
|---|---|---|---|---|---|
| Peptide GLP-1R Agonists | |||||
| exenatide (1) | AstraZeneca | 5–10 μg b.i.d. sc | 2.4 h | approved in U.S. (2005) | (24) |
| liraglutide (2) | Novo Nordisk | 1.2–1.8 mg once daily sc | 11–15 h | approved in U.S. (2009) | (25) |
| taspoglutide (3) | Ipsen/Roche | 165 h | (49) | ||
| lixisenatide (4) | Sanofi-Aventis | 20 μg once daily | 2.7–4.3 h | approved in European Union, Mexico, Australia, and Japan | (94) |
| semaglutide (5) | Novo Nordisk | 160 h | phase 3 | (97) | |
| constrained GLP-1 analogs (6) | Ahn et al. | (73) | |||
| fluorinated GLP-1 analogs (7) | Kumar et al. | (41) | |||
| bile acid conjugated exendin-4 analogs (8) | Lee et al. | (99) | |||
| truncated GLP-1R agonists (9) | Mapelli et al. (Bristol-Myers Squibb) | (55) | |||
| β3-peptide analog (10) | Schepartz et al. | (100) | |||
| Protein GLP-1R Agonists | |||||
| albiglutide (11) | GlaxoSmithKline | 30 mg/week | 6–8 days | approved in Europe (2013) and U.S. (2014) | (97, 101) |
| CJC-1134-PC (12) | ConjuChem | 8 days | phase 2 | (102) | |
| dulaglutide | Eli Lilly | once weekly | 90 h | phase 3 | (103) |
| langlenatide | Hanmi | once weekly | 180 h | phase 2 | (104) |
| VRS-859 | Diartis | once monthly | 139 h | phase 1 | (105) |