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用布鲁顿酪氨酸激酶（BTK）抑制剂靶向实体瘤

Targeting Solid Tumors With BTK Inhibitors.

作者信息

Uckun Fatih M, Venkatachalam Taracad

机构信息

Immuno-Oncology Program, Ares Pharmaceuticals, LLC, St. Paul, MN, United States.

出版信息

Front Cell Dev Biol. 2021 Apr 14;9:650414. doi: 10.3389/fcell.2021.650414. eCollection 2021.

DOI:10.3389/fcell.2021.650414
PMID:33937249
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8079762/
Abstract

The repurposing of FDA-approved Bruton's tyrosine kinase (BTK) inhibitors as therapeutic agents for solid tumors may offer renewed hope for chemotherapy-resistant cancer patients. Here we review the emerging evidence regarding the clinical potential of BTK inhibitors in solid tumor therapy. The use of BTK inhibitors may through lead optimization and translational research lead to the development of new and effective combination regimens for metastatic and/or therapy-refractory solid tumor patients.

摘要

将美国食品药品监督管理局（FDA）批准的布鲁顿酪氨酸激酶（BTK）抑制剂重新用作实体瘤治疗药物，可能为化疗耐药的癌症患者带来新的希望。在此，我们综述了有关BTK抑制剂在实体瘤治疗中临床潜力的新证据。BTK抑制剂的应用可能通过先导化合物优化和转化研究，为转移性和/或治疗难治性实体瘤患者开发新的有效联合治疗方案。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0605/8079762/510b40b1926c/fcell-09-650414-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0605/8079762/3c350aaba6db/fcell-09-650414-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0605/8079762/510b40b1926c/fcell-09-650414-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0605/8079762/3c350aaba6db/fcell-09-650414-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0605/8079762/510b40b1926c/fcell-09-650414-g002.jpg

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Inhibitors targeting Bruton's tyrosine kinase in cancers: drug development advances.针对癌症中布鲁顿酪氨酸激酶的抑制剂：药物研发进展。
Leukemia. 2021 Feb;35(2):312-332. doi: 10.1038/s41375-020-01072-6. Epub 2020 Oct 29.
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Inhibition of Bruton's Tyrosine Kinase Suppresses Cancer Stemness and Promotes Carboplatin-induced Cytotoxicity Against Bladder Cancer Cells.抑制布鲁顿酪氨酸激酶可抑制膀胱癌干细胞特性并增强卡铂的细胞毒性作用。
Anticancer Res. 2020 Nov;40(11):6093-6099. doi: 10.21873/anticanres.14630.
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A randomized phase 2 trial of pembrolizumab versus pembrolizumab and acalabrutinib in patients with platinum-resistant metastatic urothelial cancer.
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Development of a prognostic gene signature and exploration of P4HA1 in the modulation of cuproptosis in colorectal cancer.结直肠癌预后基因特征的开发及P4HA1在铜死亡调节中的探索
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