3-Acetyl-3-amino-5,12-dihydroxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-1-yl 2-deoxypentopyranoside--hydrogen chloride (1/1)

Beschreibungsmall and small-cell lung cancers. Amrubicin, a completely synthetic anthracycline derivative, mediates its growth inhibitory action via topoisomerase II inhibition. It is activated in viva by the formation of its 13-OH metabolite, amrubicinol, via reaction with carbonyl reductase. In contrast to doxorubicin and daunorubicin whose metabolites are inactive in the blood, amrubicinol is 10-100 fold more cytotoxic than amrubicin. In phase II clinical trials, amrubicin showed antitumor activity against non-small-cell lung cancers (response rate exceeding 20%) and against untreated extensive stage small-cell-lung cancers (response rate 78.8%). Amrubicin demonstrated a smaller distribution-volume, a shorter half-life in mice and also less chronic cardiotoxicity in preclinical studies compared to doxorubicin. Amrubicin was generally well tolerated with major adverse events being anaemia, leucopenia, thrombocytopenia and neutropenia.