TABLE 1.
Agent | Recommended dose and schedule | Amino acid sequence of GLP-1 component | Homology to naturally occurring GLP-1 |
---|---|---|---|
Naturally occurring human GLP-1(5) | N/A | His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-Gly | N/A |
Albiglutide (6) | 30 mg QW | His-Gly-Glu-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg | 97%; modified GLP-1 dimer fused in series to human albumin. Amino acid substitution at position 8 (glycine to alanine), dimer. |
Dulaglutide (7,8) | 0.75 − 1.5 mg QW | His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Glu-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Gly-Gly | 90%; synthetic human GLP-1 dimer (8-glycine,22-glutamic acid,36-glycine) fusion protein with peptide (synthetic 16-amino acid linker) fusion protein with immunoglobulin G4 (synthetic human Fc fragment). |
Exenatide (9,10) | 10 μg BID, ER formulation: 2 mg QW | His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2 | 53%; synthetic version of exendin-4. |
Liraglutide (5,11) | 1.2 or 1.8 mg QD | His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly | 97%; glutamic acid and 16-C free fatty acid addition at position 26. Amino acid substitution at position 34 (lysine to arginine). |
Lixisenatide* (12) | 20 μg QD | His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-Lys-Lys-Lys-Lys-Lys-Lys-NH2 | Homology not published but, based on amino acid sequence, likely to be <50%. Synthetic version of exendin-4. |
Licensed in Europe. Not approved in the United States.
QW, once weekly; QD, once daily; BID, twice daily; ER, extended release.