Ponatinib and other CML Tyrosine Kinase Inhibitors in Thrombosis
Abl1 kinase has important biological roles. The Bcr-Abl1 fusion protein creates undesired kinase activity and is pathogenic in 95% of chronic myeloid leukemia (CML) and 30% of acute lymphoblastic leukemia (ALL) patients. Targeted therapies to these diseases are tyrosine kinase inhibitors. The extent...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-09-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/21/18/6556 |
| _version_ | 1797554379106025472 |
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| author | Peng Zeng Alvin Schmaier |
| author_facet | Peng Zeng Alvin Schmaier |
| author_sort | Peng Zeng |
| collection | DOAJ |
| description | Abl1 kinase has important biological roles. The Bcr-Abl1 fusion protein creates undesired kinase activity and is pathogenic in 95% of chronic myeloid leukemia (CML) and 30% of acute lymphoblastic leukemia (ALL) patients. Targeted therapies to these diseases are tyrosine kinase inhibitors. The extent of a tyrosine kinase inhibitor’s targets determines the degree of biologic effects of the agent that may influence the well-being of the patient. This fact is especially true with tyrosine kinase inhibitor effects on the cardiovascular system. Thirty-one percent of ponatinib-treated patients, the tyrosine kinase inhibitor with the broadest inhibitory spectrum, have thrombosis associated with its use. Recent experimental investigations have indicated the mechanisms of ponatinib-associated thrombosis. Further, an antidote to ponatinib is in development by re-purposing an FDA-approved medication. |
| first_indexed | 2024-03-10T16:30:12Z |
| format | Article |
| id | doaj.art-efe9bf2b5af84961852e5419228e0293 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-10T16:30:12Z |
| publishDate | 2020-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-efe9bf2b5af84961852e5419228e02932023-11-20T12:55:49ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672020-09-012118655610.3390/ijms21186556Ponatinib and other CML Tyrosine Kinase Inhibitors in ThrombosisPeng Zeng0Alvin Schmaier1Department of Pharmacology, Case Western Reserve University, Cleveland, OH 44106, USADepartments of Medicine and Pathology, Case Western Reserve University and University Hospitals Cleveland Medical Center, Cleveland, OH 44106, USAAbl1 kinase has important biological roles. The Bcr-Abl1 fusion protein creates undesired kinase activity and is pathogenic in 95% of chronic myeloid leukemia (CML) and 30% of acute lymphoblastic leukemia (ALL) patients. Targeted therapies to these diseases are tyrosine kinase inhibitors. The extent of a tyrosine kinase inhibitor’s targets determines the degree of biologic effects of the agent that may influence the well-being of the patient. This fact is especially true with tyrosine kinase inhibitor effects on the cardiovascular system. Thirty-one percent of ponatinib-treated patients, the tyrosine kinase inhibitor with the broadest inhibitory spectrum, have thrombosis associated with its use. Recent experimental investigations have indicated the mechanisms of ponatinib-associated thrombosis. Further, an antidote to ponatinib is in development by re-purposing an FDA-approved medication.https://www.mdpi.com/1422-0067/21/18/6556ponatinibtyrosine kinase inhibitorsAbl1 kinaseBcr-Abl1chronic myelogenous leukemiathrombosis |
| spellingShingle | Peng Zeng Alvin Schmaier Ponatinib and other CML Tyrosine Kinase Inhibitors in Thrombosis International Journal of Molecular Sciences ponatinib tyrosine kinase inhibitors Abl1 kinase Bcr-Abl1 chronic myelogenous leukemia thrombosis |
| title | Ponatinib and other CML Tyrosine Kinase Inhibitors in Thrombosis |
| title_full | Ponatinib and other CML Tyrosine Kinase Inhibitors in Thrombosis |
| title_fullStr | Ponatinib and other CML Tyrosine Kinase Inhibitors in Thrombosis |
| title_full_unstemmed | Ponatinib and other CML Tyrosine Kinase Inhibitors in Thrombosis |
| title_short | Ponatinib and other CML Tyrosine Kinase Inhibitors in Thrombosis |
| title_sort | ponatinib and other cml tyrosine kinase inhibitors in thrombosis |
| topic | ponatinib tyrosine kinase inhibitors Abl1 kinase Bcr-Abl1 chronic myelogenous leukemia thrombosis |
| url | https://www.mdpi.com/1422-0067/21/18/6556 |
| work_keys_str_mv | AT pengzeng ponatinibandothercmltyrosinekinaseinhibitorsinthrombosis AT alvinschmaier ponatinibandothercmltyrosinekinaseinhibitorsinthrombosis |