Conformational implications of inverse pH-dependence of antibody aggregation

BIOT 427

Natalie Perico, Judith Purtell, Thomas Dillon, and Margaret Speed Ricci. Pharmaceutics Department, Amgen Inc, One Amgen Center Drive, Thousand Oaks, CA 91320
Antibody formulation development relies on accelerated stability data at elevated temperatures to optimize formulation parameters. However, the pH- and temperature-dependence of aggregation is complicated for antibody formulations. An inverse pH-dependence for aggregation between normal storage conditions (4C and 29°C) and accelerated conditions (37°C) was discovered for multiple IgG molecules. The nonlinear Arrhenius plots may suggest a conformational perturbation resulting in a different mechanism of self-association at higher temperature. However, biophysical characterization studies demonstrated no thermal unfolding at or below 37°C. Examination of the temperature-dependence of clipping suggested that clipping leading to aggregation was responsible for the increased higher order aggregates at low pH at elevated temperatures. Conformational differences in the hinge region due to disulfide connectivity resulted in differences in clipping and aggregation properties. These results have implications on the mechanisms of antibody aggregation and on the validity of using accelerated data to predict shelf-life.