| 摘要 |
<P>PROBLEM TO BE SOLVED: To provide an improved conjugation process that would result in significantly lower levels of a low conjugate fraction (LCF) and have acceptable levels of aggregation, without significantly altering the physical properties of the conjugate, since the LCF competes with a calicheamicin-carrier conjugate for the target cell and potentially reduces efficacy of a cytotoxic drug. <P>SOLUTION: A method for preparing a monomeric cytotoxic drug-carrier conjugate is provided, with a drug loading significantly higher than in previously reported procedures and with decreased aggregation and an LCF. The present invention also provides a cytotoxic drug derivative-antibody conjugate, a composition comprising the conjugate and use of the conjugate, a monomeric calicheamicin derivative-anti-CD22 antibody conjugate, a composition comprising the conjugate, and use of the conjugate. <P>COPYRIGHT: (C)2012,JPO&INPIT |
