The anthracyclines: will we ever find a better doxorubicin?

作者: Raymond B. Weiss

DOI: 10.5555/URI:PII:009377549290036Z

关键词: IdarubicinDexrazoxaneEpirubicinDaunorubicinCardiotoxicityAnthracyclineEndocrinologyMedicineDoxorubicinPharmacologyChemotherapyInternal medicine

摘要: The anthracyclines are the class of antitumor drugs with widest spectrum activity in human cancers, and only a few cancers (eg, colon cancer) unresponsive to them. first two were developed 1960s. Doxorubicin (DOX) differs from daunorubicin (DNR) by single hydroxyl group. This fact has spurred researchers worldwide find analogs DOX that have less acute toxicity, cause cardiomyopathy, can be administered orally, and/or different, or greater, efficacy. Five DOX/DNR marketed other countries, one (idarubicin) is available United States. None these stronger efficacy than original anthracyclines, but there some differences toxicity. Methods been fashioned keep peak plasma level muted minimize cardiotoxicity, apparently effective method so far (prolonged drug infusion) cumbersome. bisoxopiperazine (especially dexrazoxane) provides protection against anthracycline-induced cardiomyopathy much promise for helping mitigate this major obstacle prolonged use anthracyclines. being evaluated 1990s selected their ability overcome multidrug resistance cancer cells. Thirty years after discovery anticancer anthracycline, means reducing anthracycline toxicity devised. Current studies evaluating increased doses epirubicin improve cytotoxicity, while limiting at present still reigns as having most proven cancerocidal effect.

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