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. Author manuscript; available in PMC: 2014 Mar 1.
Published in final edited form as: Pharm Res. 2012 Nov 15;30(3):751–760. doi: 10.1007/s11095-012-0917-z

Table III.

Final Pharmacokinetic Model-Estimated Parameters

Parameter (units) Description Estimate (CV%)
Vc(L·kg−1) a Central volume of distribution 1.4×10−1 (7)
kel(min−1· kg−1)a Elimination rate constant for free exenatide 3.2×10−2 (8)
kpt (min−1) Distribution rate constant 2.6 × 10−2 (15)
ktp (min−1) Distribution rate constant 2.7 × 10−2 (8)
kdeg (min−1) Degradation rate constant for free receptor 1.55 × 100 (18)
kint (min−1) Rate constant of internalization for
  exendine-4-receptor complex
2.3 × 10−3 (41)
kon(pM−1 ·min−1) Second-order association rate constant 1.7×10−5 (8)
Koff_mouse (min−1) First-order dissociation rate constant 2.3 × 10−4 (52)
Koff_rat (min−1) 5.2 × 10−5 (46)
Koff_monkey (min−1) 1.5×10−3 (58)
Rtot_0mouse (pM) Receptor concentration at baseline 1.0× 103 (N/A)b
Rtot_0rat (pM) 5.2 × 103 (N/A)b
Rtot_0monkey (pM) 5.2 × 102 (N/A)b
Vmax_mouse (pmol·min−1) Maximum absorption rate 8.3 × 101 (45)
Vmax_rat (pmol·min−1) 2.4 × 102 (19)
Vmax_monkey (pmol·min−1) 5.8 × 102 (62)
Km_mouse (pmol)
Km_rat (pmol)
Amount of exenatide when absorption
rate is half maximal
9.1 × 102 (61)
3.4 × 104 (24)
Km_monkey (pmol) 1.8 × 104 (74)
a

Value represents an allometric coefficient scaled to body weight

b

Not applicable; fixed value