Immunoconjugate formulations

摘要

The present invention provides an immunoconjugate formulation that is substantially free of particles, the immunoconjugate formulation comprising: an immunoconjugate and one or more excipients selected from the group consisting of: sucrose, polysorbate 20, polysorbate 80, cyclodextrin, dextrose, glycerol, polyethylene glycol, mannitol, sodium chloride, and an amino acid, wherein the formulation is a buffered aqueous solution having a pH of 4.5 to 7.6. The present invention also provides an immunoconjugate formulation that is substantially free of aggregates, the immunoconjugate formulation comprising: an immunoconjugate and one or more excipients selected from the group consisting of histidine, sucrose, glycine and sodium chloride, wherein the formulation is a buffered aqueous solution having a pH of 4.5 to 7.6. The present invention further provides an immunoconjugate formulation that is substantially free of both particles and aggregates.

主权项

1. An immunoconjugate liquid formulation comprising:
(i) an immunoconjugate, which is an antibody comprising one or more covalently linked hydrophobic cytotoxic drugs, (ii) 5-20 mM histidine, (iii) 100-300 mM glycine, (iv) 0.1-12% sucrose, and (v) 0.5-2% beta-cyclodextrin, wherein the pH of the formulation is 4.5 to 7.6.