1246815-54-2Relevant articles and documents
Synthesis, characterization and targeting chemotherapy for ovarian cancer of trastuzumab-SN-38 conjugates
Yao, Yuqin,Yu, Lin,Su, Xiaolan,Wang, Yuxi,Li, Wenting,Wu, Yangpin,Cheng, Xiangzheng,Zhang, Hang,Wei, Xian,Chen, Hao,Zhang, Rundong,Gou, Lantu,Chen, Xiaoxin,Xie, Yongmei,Zhang, Bo,Zhang, Yonghui,Yang, Jinliang,Wei, Yuquan
, p. 5 - 17 (2015)
Antibody-drug conjugates (ADCs), combining monoclonal antibody with high cytotoxicity chemotherapeutic drug (warhead), have been successfully applied for clinical cancer therapy. Linker technology to select and design linker connecting warhead with antibo
IRINOTECAN IMMUNOASSAY
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Page/Page column 26; 29, (2011/06/26)
Novel conjugates of the pharmaceutically active metabolite of irinotecan and novel immunogens derived from this pharmaceutically active metabolite and monoclonal antibodies generated by these immunogens which are useful in immunoassays for the quantificat
A versatile prodrug approach for liposomal core-loading of water-insoluble camptothecin anticancer drugs
Liu, Xinli,Lynn, Bert C.,Zhang, Junhong,Song, Lin,Bom, David,Du, Wu,Curran, Dennis P.,Burke, Thomas G.
, p. 7650 - 7651 (2007/10/03)
We describe a versatile prodrug strategy for loading the liposomal lumen with water-insoluble camptothecins. The procedure involves conversion of an active camptothecin analogue to a 20-OR ω-aminoalkanoanic ester prodrug in which R = CO[CH2]nNH2 and n = 1-3. The basic amino group of the prodrug serves three roles. First, at pH ranges of 3-5, the amine enhances aqueous solubility. Second, it enhances responsiveness to a transmembrane ammonium sulfate gradient across the liposomal bilayer, thereby facilitating active loading of the agent into the liposomal aqueous core. Third, at a physiological pH of 7 or above (the pH to be encountered following drug release at the tumor site), the nucleophilicity of the amine manifests itself and cyclization to the C-21 carbonyl carbon occurs. This cyclization triggers a rapid and convenient nonenzymatic decomposition process that releases active camptothecin. Accordingly, this novel liposomal approach offers a potential system for tumor-targeting prodrugs of many water-insoluble camptothecins, including the highly lipophilic and clinically attractive analogues SN-38, 9-nitrocamptothecin and DB-67. The rate of formation of the active agent at the tumor site can be controlled through the selection of n (the length of the alkyl spacer group). Copyright
