TABLE 2.

Parameters of efalizumab PBPK models.

Parameter	Rabbit	NHP	Human	Source	Description
KD,FcRn [μM]	6.51	0.49	0.63	Human: Niederalt et al., 2018 NHP and rabbit: estimated	Equilibrium dissociation constant of efalizumab binding to FcRn
CD11a reference concentration [μM]	—	0.12 a	0.12 a	Estimated	Concentration in organ with maximal expression (=gonads)
kint,T [h−1]	—	0.005 a	0.005 a	Estimated	Internalization rate constant of CD11a
kint,C [h−1]	—	0.05 a	0.05 a	Estimated	Internalization rate constant of the efalizumab-CD11a-complex
KD [nM]	—	0.99 b	0.77 b	Bauer et al., 1999	Equilibrium dissociation constant of efalizumab binding to CD11a
koff [h−1]	—	0.33 a	0.33 a	Estimated	Dissociation rate constant of the efalizumab-CD11a-complex
MW [kDa]	149	149	149	Boehncke, 2007	Molecular weight
Rhyd [nm]	3.51	3.51	3.51	Calculated	Hydrodynamic radius
kass [µM−1 · min−1]	0.87	0.87	0.87	PK-Sim default	Association rate constant of efalizumab binding to FcRn

^a Same value assumed for NHP, and human.

^b In-vitro measurement.