Bosutinib in the management of chronic myelogenous leukemia
Gunhild Keller-von Amsberg, Philippe SchafhausenDepartment of Hematology and Oncology and, Stem Cell Transplantation and Pulmonology Division, Oncological Center, University Hospital Hamburg-Eppendorf, Hamburg, GermanyAbstract: Bosutinib (SKI-606) is an orally available, once-daily dual Src and Abl...
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Dove Medical Press
2013
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oai:doaj.org-article:cbaf3b78e7884248a6a18fa561a9eb412021-12-02T08:54:28ZBosutinib in the management of chronic myelogenous leukemia1177-54751177-5491https://doaj.org/article/cbaf3b78e7884248a6a18fa561a9eb412013-05-01T00:00:00Zhttp://www.dovepress.com/bosutinib-in-the-management-of-chronic-myelogenous-leukemia-a12959https://doaj.org/toc/1177-5475https://doaj.org/toc/1177-5491Gunhild Keller-von Amsberg, Philippe SchafhausenDepartment of Hematology and Oncology and, Stem Cell Transplantation and Pulmonology Division, Oncological Center, University Hospital Hamburg-Eppendorf, Hamburg, GermanyAbstract: Bosutinib (SKI-606) is an orally available, once-daily dual Src and Abl kinase inhibitor, approved by the US Food and Drug Administration for the treatment of adults with chronic, accelerated, or blast-phase Philadelphia chromosome-positive chronic myelogenous leukemia who are intolerant of or resistant to first- or second-generation tyrosine kinase inhibitors. Bosutinib effectively overcomes the majority of imatinib-resistance-conferring BCR-ABL mutations except V299L and T315I. In the Bosutinib Efficacy and Safety in chronic myeloid LeukemiA (BELA) trial, bosutinib attained a faster and deeper molecular response than imatinib in newly diagnosed chronic-phase chronic myelogenous leukemia patients. Treatment-emergent adverse events are usually very manageable. Low grade, mostly self-limiting diarrhea represents the most frequently observed toxicity of bosutinib. Anti-diarrheal drugs, antiemetic agents, and/or fluid replacement should be used to treat these patients. The improved hematological toxicity of bosutinib compared with other tyrosine kinase inhibitors has been ascribed to its minimal activity against platelet-derived growth factor receptor and KIT. In this review, we give an overview on the profile of bosutinib, the clinical potential and treatment-emergent adverse events.Keywords: CML, BCR-ABL, SRC/ABL kinase inhibitor, resistance-conferring mutationKeller-von Amsberg GSchafhausen PDove Medical PressarticleMedicine (General)R5-920ENBiologics: Targets & Therapy, Vol 2013, Iss default, Pp 115-122 (2013) |
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Medicine (General) R5-920 Keller-von Amsberg G Schafhausen P Bosutinib in the management of chronic myelogenous leukemia |
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Gunhild Keller-von Amsberg, Philippe SchafhausenDepartment of Hematology and Oncology and, Stem Cell Transplantation and Pulmonology Division, Oncological Center, University Hospital Hamburg-Eppendorf, Hamburg, GermanyAbstract: Bosutinib (SKI-606) is an orally available, once-daily dual Src and Abl kinase inhibitor, approved by the US Food and Drug Administration for the treatment of adults with chronic, accelerated, or blast-phase Philadelphia chromosome-positive chronic myelogenous leukemia who are intolerant of or resistant to first- or second-generation tyrosine kinase inhibitors. Bosutinib effectively overcomes the majority of imatinib-resistance-conferring BCR-ABL mutations except V299L and T315I. In the Bosutinib Efficacy and Safety in chronic myeloid LeukemiA (BELA) trial, bosutinib attained a faster and deeper molecular response than imatinib in newly diagnosed chronic-phase chronic myelogenous leukemia patients. Treatment-emergent adverse events are usually very manageable. Low grade, mostly self-limiting diarrhea represents the most frequently observed toxicity of bosutinib. Anti-diarrheal drugs, antiemetic agents, and/or fluid replacement should be used to treat these patients. The improved hematological toxicity of bosutinib compared with other tyrosine kinase inhibitors has been ascribed to its minimal activity against platelet-derived growth factor receptor and KIT. In this review, we give an overview on the profile of bosutinib, the clinical potential and treatment-emergent adverse events.Keywords: CML, BCR-ABL, SRC/ABL kinase inhibitor, resistance-conferring mutation |
format |
article |
author |
Keller-von Amsberg G Schafhausen P |
author_facet |
Keller-von Amsberg G Schafhausen P |
author_sort |
Keller-von Amsberg G |
title |
Bosutinib in the management of chronic myelogenous leukemia |
title_short |
Bosutinib in the management of chronic myelogenous leukemia |
title_full |
Bosutinib in the management of chronic myelogenous leukemia |
title_fullStr |
Bosutinib in the management of chronic myelogenous leukemia |
title_full_unstemmed |
Bosutinib in the management of chronic myelogenous leukemia |
title_sort |
bosutinib in the management of chronic myelogenous leukemia |
publisher |
Dove Medical Press |
publishDate |
2013 |
url |
https://doaj.org/article/cbaf3b78e7884248a6a18fa561a9eb41 |
work_keys_str_mv |
AT kellervonamsbergg bosutinibinthemanagementofchronicmyelogenousleukemia AT schafhausenp bosutinibinthemanagementofchronicmyelogenousleukemia |
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1718398332531900416 |