Effect of residual moisture content on the stability of dried Apo2L/TRAIL crystals

BIOT 139

Heather Flores, hae@gene.com1, Ana Sofia Ressurreiçao2, Boyan Zhang3, Bruce Kabakoff1, Zahra Shahrokh4, and Mary E. M. Cromwell1. (1) Early Stage Pharmaceutical Development, Genentech Inc, 1 DNA Way, South San Francisco, CA 94080, (2) Portugal, (3) Early Stage Analytical Development, Genentech Inc, 1 DNA way MS 62, South San Francisco, CA 94080, (4) Transkaryotics Therapies, MA
Reducing the moisture content of crystalline Apo2L/TRAIL, a non-covalent homotrimer, below 5% may decrease the stability of the protein, a result significantly different than observed for proteins lyophilized in a glassy state. The primary degradation product at low moisture content is one that does not occur in solution or in non-crystalline lyophilized formulations. A concurrent increase in hexamer content by native SEC and non-reducible dimer under denaturing conditions suggests that the degradation product is a non-disulfide, covalent bond between monomers in adjacent trimers. This is further supported by the apparent ratio of one covalent dimer to four monomers in purified hexamer. Increasing the residual moisture can decrease the formation rate of this covalent hexamer but increase the rate of intramolecular disulfide bonds within the trimer. Further investigation into the degradation mechanisms of Apo2L/TRAIL crystals is ongoing.