CL2A-SN-38

CL2A-SN38 is a SN38 derivative with a Mal-PEG attached peptide linker, it can easily react with antibody to form an antibody-drug conjugate (ADC). SN-38 is a potent DNA Topoisomerase I inhibitor. CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A linker is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.

CL2A-SN-38 is a agent-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody agent conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A-SN-38 uses hydrolyzable linker to deliver active agents within tumor cells and in the tumor microenvironment, resulting in bystander effects[1].

Camptothecins

[1] Cardillo TM, et al. Humanized anti-Trop-2 IgG-SN-38 conjugate for effective treatment of diverse epithelial cancers: preclinical studies in human cancer xenograft models and monkeys. Clin Cancer Res. 2011 May 15;17(10):3157-69. DOI:10.1158/1078-0432.CCR-10-2939
[2] Thomas M Cardillo, et al. Humanized anti-Trop-2 IgG-SN-38 conjugate for effective treatment of diverse epithelial cancers: preclinical studies in human cancer xenograft models and monkeys. Clin Cancer Res. 2011 May 15;17(10):3157-69. DOI:10.1158/1078-0432.CCR-10-2939