Table 1.
Peptide | Clinical Status |
Sequence | Ref. |
---|---|---|---|
GLP-1 (7–36) | HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG-NH2 | [Lopez et al. 1983] | |
Exendin-4 | Approved | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 | [Eng et al. 1992] |
Liraglutide (Victoz, Saxenda) | Approved | HAEGTFTSDVSSYLEGQAA-(K-P1)-EFIAWLVRGRG | [Bayes et al. 2003; Ostawal et al. 2016] |
Exenatide (Byetta, Bydureon) | Approved | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 | [Gedulin et al. 2003] |
CJC-1131 | Preclinical (No longer in development) | HaEGTFTSDVSSYLEGQAAKEFIAWLVKGR-P2 | [Kim et al. 2003] |
Albiglutide (Eperzan, Tanzeum) | Approved | HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRHGEGTFTSDVSSYLEGQAAKEFIAWLVKGR-Albumin | [Stewart et al. 2008] |
Taspoglutide | Failed Phase III (Hypersensitivity) | H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVK-Aib-R-NH2 | [Sebokova et al. 2010] |
CJC-1134 | Canceled Phase II (Competition) | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPP-P3 | [Baggio et al. 2008] |
Lixisenatide | Approved | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK-NH2 | [Christensen et al. 2009] |
Exenatide-XTEN | Phase I | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-XTEN | [Schellenberger et al. 2009] |
Efpeglenatide (LAPS CA Exendin-4, LAPS Exendin-4, HM11260C) | Phase II | 4-imidazoacetyl-GEGTFTSDLSKQMEEEAVRLFIEWL-(K-PEG-Fc)-NGGPSSGAPPPS-NH2 | [Choi et al. 2014] |
Dulaglutide (Trulicity) | Approved | HGEGTFTSDVSSYLEEQAAKEFIAWLVKGG-Fc-Fc-GGKVLWAIFEKAAQEELYSSVDSTFTGEGH | [Jimenez-Solem et al. 2010] |
Semaglutide (NN9924/OG217SC) | Phase III | H-Aib-EGTFTSDVSSYLEGQAA-(K-P4)-EFIAWLVRGRG-NH2 | [Lund et al. 2011] |
Amphiphile Mimetic | Preclinical | HSEGTFTSDGEEEAAVV-(K-P5)-NH2 | [Khan et al. 2012] |
Coumaglutide (13c) | Preclinical | HGEGTFTSDV-(C-P6)-SYLEGQAAKEFIAWLVKGR-NH2 | [Sun et al. 2015b] |
I-3 | Preclinical | HGEGTFTSDLS-(C-P7)-QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 | [Sun et al. 2016] |
Text that is bolded indicates modification from the native GLP-1 (7-36 amide) sequence. See Fig. 2 for the chemical structures represented by pendant groups P1-7.