[Survey of anthracyclines derivatives in haematology (author's transl)].
Anthracyclines, such as daunorubicin (DNR), rubidazone (RBD) and adriamycin (ADR) are intercalating drugs used in cancer chemotherapy. They inhibit synthesis of DNA and RNA, break DNA and inhibit mitochondrial oxidative chain. Their antitumoral experimental activities depend upon type of drug, tumor and route of administration. After i.v. administration, the drug is present in all tissues except central nervous system. Its disappearance from the plasma is biphasic with a long terminal half life, justifying intermittent chemotherapy. Anthracyclines metabolism occurs mainly in liver micrososomes, and 90% metabolites are excreted in the bile. The main toxicity is cardiac, as a congestive heart failure which appears when a cumulated drug dose is overcome. In man only, a few derivatives have been studied, compounds with activity and no cardiotoxicity are still in research. Action of malignancies depends on type of derivative. We use DNR since 1967, it is a remarkable active drug in induction treatment of AML, it is the only active drug on acute promyelocytic leukemia, and it increases number of remissions in all of adult patients and severe forms of children ALL. Adriamycin (ADR) is active on solid tumors (osteosarcoma, breast and thyroid cancers) and lymphomas. With rubidazone (RBD) we obtain 2/3 of remissions in acute monoblastic leukemia, and it is easier to use than DNR and equally active on AML. RBD is also active on severe cases of lymphomas (lymphosarcomas and Hodgkin's disease). A new compound DEA 14 DNR seems interesting: experimental antitumor activity is high (compared to DNR, RBD and ADR) and it appears to possess activity on solid tumors in man.
D000328:Adult; D000818:Animals; D000873:Anthracenes / Q000009:adverse effects / Q000378:metabolism / Q000627:therapeutic use; D000903:Antibiotics, Antineoplastic / Q000009:adverse effects / Q000378:metabolism / Q000627:therapeutic use*; D001711:Biotransformation; D002648:Child; D003630:Daunorubicin / Q000031:analogs & derivatives / Q000032:analysis / Q000627:therapeutic use; D004317:Doxorubicin / Q000627:therapeutic use; D006321:Heart / Q000187:drug effects; D006801:Humans; D007938:Leukemia / Q000188:drug therapy*; D008099:Liver / Q000378:metabolism
D000873:Anthracenes; D000903:Antibiotics, Antineoplastic; D004317:Doxorubicin; D003630:Daunorubicin
Les dérivés des anthracyclines en hématologie.