Table 1.
Characteristics of GLP-1 receptor agonists
| Generic | Commercial | Backbone | Dosage | Administration | Half-life | Renal dose adjustment | Route of elimination |
|---|---|---|---|---|---|---|---|
| Short-acting compound | |||||||
| Exenatide | Byetta | Exendin-4 | 5 μg, 10 μg | Twice daily, SC | ~2.4 hr | Not recommended for patients with CrCl < 30 mL/min; caution needed for patients with CrCl 30–50 mL/min | Glomerular filtration followed by proteolysis; eliminated in the urine |
| Lixisenatide | Lyxumia | Exendin-4 | 10 μg, 20 μg | Once daily, SC | ~3 hr | Not recommended for patients with CrCl < 30 mL/min | Glomerular filtration and proteolysis; excreted in the urine |
| Long-acting compound | |||||||
| Liraglutide | Victoza | Human GLP-1 | 0.6–1.8 mg | Once daily, SC | ~13 hr | No dosage adjustment required; not recommended for patients with CrCl < 15 mL/min | Proteolysis; excreted via urine and feces |
| Liraglutide | Saxenda | Human GLP-1 | 0.6–3 mg | Once daily, SC | ~13 hr | No dosage adjustment required; not recommended for patients with CrCl < 15 mL/min | Proteolysis; excreted via urine and feces |
| Exenatide ER | Bydureon | Exendin-4 | 2 mg | Once weekly, SC | ~1 wk | Not recommended for patients with an eGFR < 45 mL/min/1.73 m2 or ESRD | Glomerular filtration followed by proteolysis; eliminated in the urine |
| Dulaglutide | Trulicity | Human GLP-1 | 0.75 mg, 1.5 mg | Once weekly, SC | ~5 day | No dosage adjustment required; not recommended for patients with CrCl < 15 mL/min | Proteolytic degradation |
| Semaglutide | Ozempic | Human GLP-1 | 0.5 mg, 1.0 mg | Once weekly, SC | ~1 wk | No dosage adjustment required; not recommended for patients with CrCl < 15 mL/min | Proteolysis; excreted via urine and feces |
| Albiglutidea | Tanzeum | Human GLP-1 | 30 mg, 50 mg | Once weekly, SC | ~5 day | No dosage adjustment required; not recommended for patients with CrCl < 15 mL/min | Not available |
| Oral agent | |||||||
| Semaglutide | Rybelsus | Human GLP-1 | 3 mg, 7 mg, 14 mg | Once daily, oral | ~1 wk | No dosage adjustment required | Proteolysis; excreted via urine and feces |
| Fixed-dose combination | |||||||
| Lixisenatide + glargine | Soliqua | Exendin-4 | 20 μg/iGlar 40 IU, 20 μg/iGlar 60 IU | Once daily, SC | ~3 hr | Closely monitor patients with CrCl 15–30 mL/min; not recommended for patients with CrCl < 15 mL/min | Glomerular filtration and proteolysis; excreted in the urine |
| Liraglutide + degludec | Xultophy | Human GLP-1 | 1.8 mg/iDeg 50 IU | Once daily, SC | ~13 hr | Not studied in severe renal impairment; liraglutide is not recommended for patients with CrCl < 15 mL/min | Proteolysis; excreted via urine and feces |
CrCl, creatinine clearance; eGFR, estimated glomerular filtration rate; ER, extended-release; ESRD, end-stage renal disease; GLP-1, glucagon-like peptide-1; iDeg, insulin degludec; iGlar, insulin glargine; SC, subcutaneous.
a
Marketing was discontinued in 2018.