摘要
Rigosertib是一种非ATP竞争性多激酶抑制剂,具有显著的抗有丝分裂和抗癌活性,可诱导多种肿瘤细胞增殖停滞和凋亡,对正常细胞增殖的影响很小。Rigosertib已作为高危骨髓增生异常综合征患者的治疗药物应用于Ⅲ期临床试验。本文就Rigosertib的分子作用机制、体内外抗肿瘤活性以及临床试验等方面的研究进展做简要综述。
As a non-ATP competitive multi-kinase inhibitor with marked anti-mitotic and anti-cancer activity,rigosertib has been found to induce the proliferative arrest and apoptosis of many kinds of tumor cells with little affect on normal cells. Rigosertib is currently under phase Ⅲ clinical trials as a therapy for high-risk myelodysplastic syndrome(MDS). In this paper, recent advances in the molecular mechanism, antitumor activity in vitro and in vivo and clinical trials of rigosertib were comprehensively reviewed.
引文
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