UNIVERSITE DE STRASBOURG;CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
发明人:
Alain WAGNER,Sergii KOLODYCH,Oleksandr KONIEV
申请号：
US16614041
公开号：
US20200069815A1
申请日:
2018.05.15
申请国别(地区):
US
年份:
2020
代理人:
摘要：
This invention pertains to protein-drug conjugates that may be used in the treatment of cancers and to pharmaceutical compositions containing the same. The protein-drug conjugate has the following formula (I), wherein: L is a cysteine-containing protein residue linked through one or more of the cysteine groups of the protein, R1 is selected from the group consisting of arylene, arylene-heteroarylene, heteroarylene-arylene and heteroarylene, n is an integer from 0 to 5, p and q are independently 0 or 1, R2, R3 and Z are spacers, u is 0 or 1 and T is a cleavable unit sensitive to hydrolases, k is 1 or 2 and D is a cytotoxic drug residue selected from dolastatin residues, which may be identical to or different from each other when k is 2, m is the mean payload-to-protein ratio (PPR) of the conjugate, which ranges from 0.1 to 16.
