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Table 1 Characteristics of GLP-1RAs

From: GLP-1RAs in type 2 diabetes: mechanisms that underlie cardiovascular effects and overview of cardiovascular outcome data

Drug Structure/homology To Human GLP-1 DPP-4 cleavage Half-life Recommendations in renal impairment Antibodies
Exenatide [39, 43,44,45] Substitution of alanine in position 2 by glycine
53% homology
Resistant 2–4 h (12 h for sustained release exenatide) Not recommended in patients with GFR < 30 mL/min
Sustained release exenatide is only licensed in mild-to-moderate renal impairment (GFR > 50 mL/min)
Anti-drug antibodies were more common, and titres were higher with exenatide once weekly than with exenatide twice daily
Lixisenatide [35, 46,47,48,49,50] Exendin-4 elongated with a residue of 6 lysines attached to the C-terminus
50% homology
Resistant 2–3 h Not recommended in patients with a GFR < 30 mL/min 56–60% of patients developed anti-drug antibodies, with no apparent effect on efficacy or safety
Liraglutide [51,52,53,54,55,56] One amino acid substitution (Lys34Arg) with the addition of a C-16 acyl group (palmitoyl) attached to Lys26 via a glutamate linker
97% homology
Resistant 10–12 h No restrictions or dose adjustments required Low incidence of anti-drug antibodies
Albiglutide [57,58,59] Composed of a GLP-1 (7–36) dimer fused to recombinant human albumin
95% homology
Resistant 5 days No restrictions or dose adjustments required Low incidence of anti-drug antibodies
Dulaglutide [42, 60, 61, 72] Two DPP-4 resistant GLP-1 molecules covalently bound to a modified immunoglobulin 4 Fc fragment
90% homology
Resistant 5 days No restrictions or dose adjustments required Low incidence of anti-drug antibodies
Taspoglutide [6466] Alpha-aminoisobutyric acid substitution at positions 8 and 35 of the human GLP-1(7–36)NH2 that enhances enzymatic stability and potency
93% homology
Resistant 165 h Renal impairment alters the pharmacokinetics of taspoglutide. The degree of renal impairment was associated with an increased exposure to taspoglutide and an increased risk of gastrointestinal adverse events Incidence of anti-drug antibodies as high as 49%
Semaglutide [5871, 73] Acyl group with a steric diacid at Lys26 and a large synthetic spacer and modified by the presence of a alpha-aminobutyric acid in position 8
94% homology
Resistant 1 week No restrictions or dose adjustments required for patients with renal impairment Low incidence of anti-drug antibodies
  1. Arg, arginine; DPP-4, dipeptidyl peptidase 4; GFR, glomerular filtration rate; GLP-1, glucagon-like peptide-1; Lys, lysine