Table 2.
Summary of the pharmacokinetic properties of GLP1 and GLP1-ELP fusions
| Construct | t1/2,elim# (h) |
t1/2,biol# (h) |
tmax (h) |
Cmax (nM) |
Delivery Duration (d) |
AUC (nM×h) |
CL (mL/h) |
Bioavailability (%) |
|---|---|---|---|---|---|---|---|---|
| GLP1 | 0.08 (0.06 to 0.12) | 4.7 (3.4 to 7.0) | 0.75 | 484 ± 26% | < 1 | 4,418 ± 618% | 2.88 ± 0.48 | 98.1 ± 22.8 |
| GLP1-ELPsol | 5.7 (3.8 to 11.4) | 16.9 (14.5 to 20.3) | 6 | 2,123 ± 49 | 3 | 56,451 ± 1,782 | 0.23 ± 0.01 | 38.6 ± 0.8 |
| GLP1-ELPopt | 6.9 (5.3 to 9.8) | 45.2 (33.7 to 68.3) | 6 | 295 ± 13 | 10 | 29,872 ± 1,069 | 0.42 ± 0.10 | 33.4 ± 21.0 |
Values reported are the mean with 95% CI range in parentheses.
Cmax and AUC for GLP1 are lower than the values for GLP1-ELP because of the lower treatment dose used for free peptide (50 nmol/kg) versus GLP1-ELP fusion (700 nmol/kg).