1. The effect of a change in the expression level of the receptor and the binding affinity on the subcutaneous bioavailability of mAbs.
The effect of a change in the expression level of the receptor and the binding affinity on the subcutaneous bioavailability of mAbs. Simulation was performed using the model developed for rituximab injected subcutaneously at the back of rats (Kagan et al., 2012); the model schematic is shown in Fig. 5A. Reported values of KD and Rtot were changed 10-fold from the reported values, and all the other parameters were kept constant. The column in the middle (relative values of 1 for KD and Rtot) represent (A) the experimentally obtained bioavailability of 69% for 1 mg/kg and (B) 18% for 40 mg/kg dose.
Leonid Kagan Drug Metab Dispos 2014;42:
Copyright © 2014 by The American Society for Pharmacology and Experimental Therapeutics