BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies
Abstract Bruton’s tyrosine kinase (BTK) is an essential component of multiple signaling pathways that regulate B cell and myeloid cell proliferation, survival, and functions, making it a promising therapeutic target for various B cell malignancies and inflammatory diseases. Five small molecule inhib...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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BMC
2022-10-01
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| Series: | Journal of Hematology & Oncology |
| Subjects: | |
| Online Access: | https://doi.org/10.1186/s13045-022-01353-w |
| _version_ | 1811201420501712896 |
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| author | Aqu Alu Hong Lei Xuejiao Han Yuquan Wei Xiawei Wei |
| author_facet | Aqu Alu Hong Lei Xuejiao Han Yuquan Wei Xiawei Wei |
| author_sort | Aqu Alu |
| collection | DOAJ |
| description | Abstract Bruton’s tyrosine kinase (BTK) is an essential component of multiple signaling pathways that regulate B cell and myeloid cell proliferation, survival, and functions, making it a promising therapeutic target for various B cell malignancies and inflammatory diseases. Five small molecule inhibitors have shown remarkable efficacy and have been approved to treat different types of hematological cancers, including ibrutinib, acalabrutinib, zanubrutinib, tirabrutinib, and orelabrutinib. The first-in-class agent, ibrutinib, has created a new era of chemotherapy-free treatment of B cell malignancies. Ibrutinib is so popular and became the fourth top-selling cancer drug worldwide in 2021. To reduce the off-target effects and overcome the acquired resistance of ibrutinib, significant efforts have been made in developing highly selective second- and third-generation BTK inhibitors and various combination approaches. Over the past few years, BTK inhibitors have also been repurposed for the treatment of inflammatory diseases. Promising data have been obtained from preclinical and early-phase clinical studies. In this review, we summarized current progress in applying BTK inhibitors in the treatment of hematological malignancies and inflammatory disorders, highlighting available results from clinical studies. |
| first_indexed | 2024-04-12T02:20:15Z |
| format | Article |
| id | doaj.art-9f3f7e5e4d0b46e99d1320a251a620d9 |
| institution | Directory Open Access Journal |
| issn | 1756-8722 |
| language | English |
| last_indexed | 2024-04-12T02:20:15Z |
| publishDate | 2022-10-01 |
| publisher | BMC |
| record_format | Article |
| series | Journal of Hematology & Oncology |
| spelling | doaj.art-9f3f7e5e4d0b46e99d1320a251a620d92022-12-22T03:52:08ZengBMCJournal of Hematology & Oncology1756-87222022-10-0115113510.1186/s13045-022-01353-wBTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studiesAqu Alu0Hong Lei1Xuejiao Han2Yuquan Wei3Xiawei Wei4Laboratory of Aging Research and Cancer Drug Target, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan UniversityLaboratory of Aging Research and Cancer Drug Target, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan UniversityLaboratory of Aging Research and Cancer Drug Target, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan UniversityLaboratory of Aging Research and Cancer Drug Target, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan UniversityLaboratory of Aging Research and Cancer Drug Target, State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan UniversityAbstract Bruton’s tyrosine kinase (BTK) is an essential component of multiple signaling pathways that regulate B cell and myeloid cell proliferation, survival, and functions, making it a promising therapeutic target for various B cell malignancies and inflammatory diseases. Five small molecule inhibitors have shown remarkable efficacy and have been approved to treat different types of hematological cancers, including ibrutinib, acalabrutinib, zanubrutinib, tirabrutinib, and orelabrutinib. The first-in-class agent, ibrutinib, has created a new era of chemotherapy-free treatment of B cell malignancies. Ibrutinib is so popular and became the fourth top-selling cancer drug worldwide in 2021. To reduce the off-target effects and overcome the acquired resistance of ibrutinib, significant efforts have been made in developing highly selective second- and third-generation BTK inhibitors and various combination approaches. Over the past few years, BTK inhibitors have also been repurposed for the treatment of inflammatory diseases. Promising data have been obtained from preclinical and early-phase clinical studies. In this review, we summarized current progress in applying BTK inhibitors in the treatment of hematological malignancies and inflammatory disorders, highlighting available results from clinical studies.https://doi.org/10.1186/s13045-022-01353-wBTKInhibitorsHematological malignanciesInflammatory diseasesSignaling pathwaysClinical trials |
| spellingShingle | Aqu Alu Hong Lei Xuejiao Han Yuquan Wei Xiawei Wei BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies Journal of Hematology & Oncology BTK Inhibitors Hematological malignancies Inflammatory diseases Signaling pathways Clinical trials |
| title | BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies |
| title_full | BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies |
| title_fullStr | BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies |
| title_full_unstemmed | BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies |
| title_short | BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies |
| title_sort | btk inhibitors in the treatment of hematological malignancies and inflammatory diseases mechanisms and clinical studies |
| topic | BTK Inhibitors Hematological malignancies Inflammatory diseases Signaling pathways Clinical trials |
| url | https://doi.org/10.1186/s13045-022-01353-w |
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