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[蛋白酶体抑制剂]

[Proteasome inhibitors].

作者信息

Hatake Kiyohiko, Mishima Yuko, Terui Yasuhito

机构信息

Department of Chemotherapy, Japanese Foundation for Cancer Research Hospital, 1-37-1 Kami-ikebukuro, Toshima-ku, Tokyo 170-8455, Japan.

出版信息

Gan To Kagaku Ryoho. 2004 Jul;31(7):999-1002.

Abstract

Bortezomib, one of the proteasome inhibitors, has been approved in the United States for multiple myeloma as a second-line chemotherapy. In Japan, bortezomib has been used for for phase I clinical trials for multiple myeloma. As the action mechanism, it has been proposed that bortezomib inhibits NF-kappaB via IkappaB alpha. It also demonstrated positive results for non-Hodgkin's lymphoma and non-small cell lung cancer, but not for colorectal cancer or chronic lymphocytic leukemia. The mechanism of drug resistance has been well analized. Bortezomib is very effective but still induces adverse effects including hypotension especially when there is an overdose. Medical oncologists or hematology/oncologists must exert due caution.

摘要

硼替佐米,一种蛋白酶体抑制剂,在美国已被批准作为二线化疗药物用于治疗多发性骨髓瘤。在日本,硼替佐米已被用于多发性骨髓瘤的I期临床试验。就其作用机制而言,有人提出硼替佐米通过IkappaBα抑制核因子κB。它对非霍奇金淋巴瘤和非小细胞肺癌也显示出阳性结果,但对结直肠癌或慢性淋巴细胞白血病无效。耐药机制已得到充分分析。硼替佐米非常有效,但仍会引发不良反应,包括低血压,尤其是在用药过量时。医学肿瘤学家或血液学/肿瘤学家必须格外谨慎。

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