CALICHEAMICIN-ANTIBODY-DRUG CONJUGATES AND METHODS OF USE

摘要

The invention relates generally to a calicheamicin molecule activated with a leaving group. The invention further relates generally to an antibody-drug conjugate comprising an antibody directly conjugated by a disulfide to one or more calicheamicin molecules.

主权项

1. A drug intermediate composition of Formula I or Formula II: wherein R is selected from H, —C(O)R1, —C(O)NR1R2, —S(O)2R1, and —S(O)2NR2R1; R1 and R2 are independently selected from C1-C6 alkyl and C6-C20 aryl; R3 is selected from NO2, Cl, F, CN, CO2H, and Br; and q is 0, 1, or 2.