Table 2.
GLP‐1 RA agent | Based on |
Molecular formula Molecular weight (kilodaltons) |
SC dosing | T max | t 1/2 | Homology to native GLP‐1 (%) | Presence of antibodies to agent/GLP‐1 (%) | Renal dosing | Elimination | CL (L/h) | ||
---|---|---|---|---|---|---|---|---|---|---|---|---|
Timing | Initial dose | Regular dose | ||||||||||
Exenatide BID b , 29 | Exendin‐4 11 , 97 |
C184H282N50O60S 4.2 |
BID within 1 h before morning and evening meals (approx. 6 h or more apart) | 5 mcg BID | 5 or 10 mcg BID | 2.1 h | 2.4 h | 53 98 | 38 | Creatinine CL < 30 mL/min not recommended | Renal/proteolysis | 9.1 |
Lixisenatide c , 30 | Exendin‐4 11 , 97 |
C215H347N61O65S 4.9 |
QD within 1 h before the first meal of the day | 10 mcg | 20 mcg | 1‐3.5 h | 3 h | 50 11 , 97 , 98 | 70 | eGFR < 15 mL/min/1.73 m2 not recommended | Renal/proteolysis | 35 |
Liraglutide d 27 | Modified human GLP‐1 |
C172H265N43O51 3.8 |
QD at any time of day, with or without food | 0.6 mg | 1.2 or 1.8 mg | 8‐12 h | 13 h | 97 | 8.6 | No dose adjustment | No specific organ | 1.2 |
Exenatide ER e 19 | Exendin‐4 |
C184H282N50O60S 4.2 |
QW at any time of day, with or without food | 2.0 mg | 2.0 mg | Peaks around 2 and 6‐7 weeks | 5 days | 53 98 | Not explicitly stated in the PI | eGFR < 30 mL/min/1.73 m2 not recommended | Renal/proteolysis | 9.1 |
Dulaglutide f 21 | Modified human GLP‐1 |
Not explicitly stated in the PI 63 |
QW at any time of day, with or without food | 0.75 mg | 0.75 or 1.5 mg | 24‐72 h (median, 48 h) | 5 days | 90 | 1.6 | No dose adjustment | Endogenous metabolism | 0.111 (0.75 mg) and 0.107 (1.5 mg) |
Semaglutide g 20 | Modified human GLP‐1 |
C187H291N45O59 4.1 |
QW at any time of day, with or without food | 0.25 mg | 0.5 or 1.0 mg | 1‐3 days | 7 days | 94 | 1 | No dose adjustment | Urine and faeces | 0.05 |
Long‐acting GLP‐1 RAs indicated as bold text.
Abbreviations: BID, twice‐daily; CL, clearance; eGFR, estimated glomerular filtration rate; ER, extended‐release; GLP‐1 RA, glucagon‐like peptide‐1 receptor agonist; GLP‐1, glucagon‐like peptide‐1; mcg, micrograms; mg, milligrams; PI, prescribing information; QD, once‐daily; QW, once‐weekly; SC, subcutaneous; t 1/2, elimination half‐life; 5 T max, time to maximum plasma concentration.
Albiglutide is not included in this table, as it was withdrawn from the market in summer 2018.
Byetta®; Amylin Pharmaceuticals; approved in 2005.
Adlyxin®; Sanofi‐Aventis; approved in 2016. Lixisenatide is also available in combination with insulin glargine under the name Soliqua®/Suliqua®.
Victoza®; Novo Nordisk; approved in 2010. Liraglutide is also available in combination with insulin degludec under the name Xultophy®.
Bydureon®; AstraZeneca; approved in 2012.
Trulicity®; Eli Lilly and Company; approved in 2014.
Ozempic®; Novo Nordisk; approved in 2017.