Govindan, Serengulam V.,Gale, Jonathan B.,Holman, Nicholas J.,Goldenberg, David M.
申请号:
AU2016285853
公开号:
AU2016285853A1
申请日:
2016.06.29
申请国别(地区):
AU
年份:
2017
代理人:
摘要:
The present invention concerns improved methods and compositions for preparing SN-38 conjugates of proteins or peptides, preferably immunoconjugates of antibodies or antigen-binding antibody fragments. More preferably, the SN-38 is attached to the antibody or antibody fragment using a CL2A linker, with 1-12, more preferably 6-8, alternatively 1-5 SN-38 moieties per antibody or antibody fragment. Most preferably, the immunoconjugate is prepared in large scale batches, with various modifications to the reaction scheme disclosed herein to optimize yield and recovery in large scale. Other embodiments concern optimized dosages and/or schedules of administration of immunoconjugate to maximize efficacy for disease treatment and minimize side effects of administration.