期刊
EXPERT OPINION ON INVESTIGATIONAL DRUGS
卷 16, 期 6, 页码 855-866出版社
TAYLOR & FRANCIS LTD
DOI: 10.1517/13543784.16.6.855
关键词
(6-maleimidocaproyl)hydrazone derivative of doxorubicin; anthracyclines; anticancer prodrugs; cancer chemotherapy; DOXO-EMCH; doxorubicin; drug targeting
The (6-maleimidocaproyl)hydrazone derivative of doxorubicin (DOXO-EMCH) is an albumin-binding prodrug of doxorubicin with acid-sensitive properties that demonstrates superior antitumor efficacy in murine tumor models and a favorable toxicity profile in mice, rats and dogs, including significantly reduced cardiotoxicity. After intravenous administration, DOXO-EMCH binds rapidly to the Cys-34 position of circulating albumin and accumulates in solid tumors due to passive targeting. In a clinical Phase I study, the dose of doxorubicin could be increased by a factor of 4.5-340 mg/m(2) when 75 mg/m(2) of free doxorubicin is considered to be the dose that can be administered as a single agent concomitant with the typical spectrum of side effects (i.e., myelotoxicity and mucositis). DOXO-EMCH was able to induce tumor regressions in anthracycline-sensitive tumors (i.e., breast cancer, small cell lung cancer and sarcoma). Phase II studies will be initiated at the beginning of 2007.
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