Ibrutinib and novel BTK inhibitors in clinical development.
Ibrutinib and novel BTK inhibitors in clinical development.
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ibrutinib和临床发育中的新型BTK抑制剂。
DOI：
10.1186/1756-8722-6-59
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发表时间：
2013-08-19
影响因子：
28.5
通讯作者：
Liu D
中科院分区：
文献类型：
--
作者：
Akinleye A;Chen Y;Mukhi N;Song Y;Liu D
靶向失调通路（RAS/RAF/MEK、PI 3 K/AKT/mTOR、JAK/STAT）的小分子抑制剂显著改善了癌症患者的临床结局。近年来，B细胞抗原受体（BCR）信号通路中的关键末端激酶布鲁顿酪氨酸激酶（BTK）已成为人类恶性肿瘤和自身免疫性疾病治疗干预的一个有吸引力的靶点。伊布替尼是一种新型的首次用于人体的BTK抑制剂，已在早期临床试验中证明了临床有效性和耐受性，并已进入III期试验。然而，需要进行额外的研究以确定最佳给药方案以及最有可能从BTK抑制中获益的患者。本文综述了伊鲁替尼和其他新型BTK抑制剂（GDC-0834、CGI-560、CGI-1746、HM-71224、CC-292和ONO-4059、CNX-774、LFM-A13）在治疗B细胞恶性肿瘤和自身免疫性疾病中的临床前和临床开发。
Small molecule inhibitors targeting dysregulated pathways (RAS/RAF/MEK, PI3K/AKT/mTOR, JAK/STAT) have significantly improved clinical outcomes in cancer patients. Recently Bruton’s tyrosine kinase (BTK), a crucial terminal kinase enzyme in the B-cell antigen receptor (BCR) signaling pathway, has emerged as an attractive target for therapeutic intervention in human malignancies and autoimmune disorders. Ibrutinib, a novel first-in-human BTK-inhibitor, has demonstrated clinical effectiveness and tolerability in early clinical trials and has progressed into phase III trials. However, additional research is necessary to identify the optimal dosing schedule, as well as patients most likely to benefit from BTK inhibition. This review summarizes preclinical and clinical development of ibrutinib and other novel BTK inhibitors (GDC-0834, CGI-560, CGI-1746, HM-71224, CC-292, and ONO-4059, CNX-774, LFM-A13) in the treatment of B-cell malignancies and autoimmune disorders.
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影响因子：
28.5
作者：
Akinleye A;Furqan M;Mukhi N;Ravella P;Liu D
通讯作者：
Liu D
影响因子：
20.3
作者：
Colombat, P;Salles, G;Solal-Céligny, P
通讯作者：
Solal-Céligny, P
影响因子：
2.6
作者：
Goodman, PA;Wood, CM;Uckun, FM
通讯作者：
Uckun, FM
影响因子：
12.8
作者：
Bam, Rakesh;Ling, Wen;Khan, Sharmin;Pennisi, Angela;Venkateshaiah, Sathisha Upparahalli;Li, Xin;van Rhee, Frits;Usmani, Saad;Barlogie, Bart;Shaughnessy, John;Epstein, Joshua;Yaccoby, Shmuel
通讯作者：
Yaccoby, Shmuel
影响因子：
20.3
作者：
Herman, Sarah E. M.;Gordon, Amber L.;Byrd, John C.
通讯作者：
Byrd, John C.