FIELD: biotechnology; medicine.
SUBSTANCE: group of inventions refers to pyrrolobenzodiazepine antibody-drug conjugates and use thereof. Disclosed is a conjugate of formula I:
,
where L is an antibody or its antigen-binding fragment to a tumor-associated antigen, DL is a link of formula II:
,
where either R10 and R11 form a double nitrogen-carbon bond between the nitrogen and carbon atoms with which they are bonded, or R11 is OH and R10 is:
,
p = 1–20.
EFFECT: said conjugates can be used for treating a proliferative disease; conjugates are well tolerated in toxicity studies in various animal species, which provides a high therapeutic index of such conjugates.
20 cl, 4 dwg, 4 tbl, 8 ex
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Authors
Dates
2021-03-03—Published
2017-02-10—Filed