Bevacizumab formulations with lower aggregation propensity, comprising corticosteroid anti-inflammatory drugs

摘要

The present invention is directed to combination formulations of monoclonal antibodies with anti-inflammatory agents, related methods and uses thereof.

主权项

1. A stable antibody formulation said formulation comprising an aqueous carrier, bevacizumab and a corticosteroid anti-inflammatory drug selected from dexamethasone, dexamethasone sodium phosphate, a dexamethasone derivative, betamethasone, betamethasone sodium phosphate, or a pharmaceutically acceptable salt thereof, wherein corticosteroid anti-inflammatory drug to bevacizumab-molar ratio ranges from is 1.53:1 to 153:1 and the dexamethasone derivative is of Formula (I): wherein R1 is selected from H, halogen, —OH, —O4PHNa2, —O—C(O)—R9; R2 is selected from H, OH, —O—C(O)—R10; R3 is selected from H or —CH3; R4 is selected from H, and halogen; R5 is selected from H, OH and carbonyl; R6 and R7 are H or form together a double bond; R8 is selected from optionally substituted C1-C6 alkyl and optionally substituted acetyl; R9 and R10 are independently selected from optionally substituted C1-C6 alkyl and optionally substituted C3-C8-cycloalkyl; R11 is selected from H or optionally substituted C1-C6 alkyl.