Shenkenberg T D, Von Hoff D D
Ann Intern Med. 1986 Jul;105(1):67-81. doi: 10.7326/0003-4819-105-1-67.
Clinical studies using mitoxantrone, an anthraquinone, were begun in the United States in 1979. Subsequent phase II and III trials have shown that mitoxantrone has significant clinical activity in patients with breast cancer, acute leukemia, and lymphoma. The drug has antiviral, antibacterial, antiprotozoal, immunomodulating, and antineoplastic properties and is mutagenic in some animal systems. Its mechanism of action seems to involve both DNA intercalation and nonintercalative electrostatic interactions. The dose-limiting toxicity is myelosuppression when the drug is given on a single-dose, every-3-week schedule and mucositis when it is given daily for 5 days. Other toxicities include gastrointestinal and cardiac effects, the gastrointestinal toxicity being less severe and less frequent than that with the anthracycline anticancer drugs. Because of its low incidence of serious toxicities and effectiveness in treating certain solid tumors and leukemias, mitoxantrone is a promising new agent in the treatment of cancer.
1979年，美国开始了使用蒽醌类药物米托蒽醌的临床研究。随后的II期和III期试验表明，米托蒽醌在乳腺癌、急性白血病和淋巴瘤患者中具有显著的临床活性。该药物具有抗病毒、抗菌、抗原虫、免疫调节和抗肿瘤特性，并且在某些动物系统中具有致突变性。其作用机制似乎涉及DNA嵌入和非嵌入性静电相互作用。当按照每3周单剂量给药方案使用该药物时，剂量限制性毒性为骨髓抑制；当每日给药5天时，剂量限制性毒性为粘膜炎。其他毒性包括胃肠道和心脏影响，胃肠道毒性比蒽环类抗癌药物较轻且发生率较低。由于其严重毒性发生率低且在治疗某些实体瘤和白血病方面有效，米托蒽醌是一种有前景的新型抗癌药物。
