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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Autores principales: Keller-von Amsberg G, Schafhausen P
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Publicado: Dove Medical Press 2013
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spelling 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)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Keller-von Amsberg G
Schafhausen P
Bosutinib in the management of chronic myelogenous leukemia
description 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
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