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Calicheamicin is an enediyne antibiotic used as an antibody-drug conjugate payload: it binds the minor groove of DNA and cuts both strands at picomolar concentrations, about a thousand times more cytotoxic than conventional chemotherapy. That is why it is only given attached to an antibody (Mylotarg, Besponsa), and why liver toxicity, including veno-occlusive disease, is its defining risk.
Calicheamicin binds the minor groove and, once its enediyne core rearranges, cuts both strands of DNA. It is released by an acid-cleavable hydrazone linker in the lysosome. Gemtuzumab ozogamicin (CD33, acute myeloid leukaemia) and inotuzumab ozogamicin (CD22, acute lymphoblastic leukaemia) carry it. Hepatotoxicity, including veno-occlusive disease especially around stem-cell transplant, is the characteristic risk.
Ball-and-stick model from PubChem 2D record (no 3D conformer available). PubChem record
Showing the molecule this term concerns: Gemtuzumab ozogamicin.
Shares Gemtuzumab ozogamicin, Antibody-drug conjugate (ADC).