7-Aminomethyl-10-methyl-11-fluoro camptothecin

7-Aminomethyl-10-methyl-11-fluoro Camptothecin is a semi-synthetic derivative of camptothecin and a potent ADC cytotoxin used as an ADC payload in antibody-drug conjugates. Its primary mechanism involves inhibition of topoisomerase I, leading to the stabilization of the DNA–enzyme complex, accumulation of single-strand DNA breaks, and induction of apoptosis in rapidly dividing tumor cells. The chemical modifications at the 7, 10, and 11 positions enhance solubility and facilitate conjugation to antibodies via various linker chemistries.

Within antibody-drug conjugates, 7-Aminomethyl-10-methyl-11-fluoro Camptothecin is conjugated to monoclonal antibodies through cleavable or non-cleavable linkers to achieve controlled intracellular release. The ADC maintains stability in systemic circulation, while enzymatic cleavage inside target cells releases the active payload. This targeted delivery ensures selective topoisomerase I inhibition in tumor cells, minimizing systemic exposure and supporting precise cytotoxic activity in tumor-targeted therapy.

Applications of 7-Aminomethyl-10-methyl-11-fluoro Camptothecin include its use in ADCs directed against solid tumors and hematologic malignancies. Its chemical structure is compatible with diverse linker systems, allowing optimization of conjugation efficiency, intracellular release kinetics, and pharmacokinetics. The payload demonstrates defined cytotoxicity in topoisomerase I-expressing cells and is incorporated into ADCs to deliver mechanistically controlled DNA-damaging effects for targeted antitumor activity.