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Bosutinib: a dual SRC/ABL kinase inhibitor for the treatment of chronic myeloid leukemia

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Bosutinib: a dual SRC/ABL kinase inhibitor for the treatment of chronic myeloid leukemia. / Keller, Gunhild; Schafhausen, Philippe; Brummendorf, Tim H.

In: EXPERT REV HEMATOL, Vol. 2, No. 5, 01.10.2009, p. 489-97.

Research output: SCORING: Contribution to journal › SCORING: Journal article › Research › peer-review

Harvard

Keller, G, Schafhausen, P & Brummendorf, TH 2009, 'Bosutinib: a dual SRC/ABL kinase inhibitor for the treatment of chronic myeloid leukemia', EXPERT REV HEMATOL, vol. 2, no. 5, pp. 489-97. https://doi.org/10.1586/ehm.09.42

APA

Keller, G., Schafhausen, P., & Brummendorf, T. H. (2009). Bosutinib: a dual SRC/ABL kinase inhibitor for the treatment of chronic myeloid leukemia. EXPERT REV HEMATOL, 2(5), 489-97. https://doi.org/10.1586/ehm.09.42

Vancouver

Keller G, Schafhausen P, Brummendorf TH. Bosutinib: a dual SRC/ABL kinase inhibitor for the treatment of chronic myeloid leukemia. EXPERT REV HEMATOL. 2009 Oct 1;2(5):489-97. https://doi.org/10.1586/ehm.09.42

Bibtex

@article{8761585e117f48cbb5b48e35e0fa9492,
title = "Bosutinib: a dual SRC/ABL kinase inhibitor for the treatment of chronic myeloid leukemia",
abstract = "The tyrosine kinase inhibitor imatinib mesylate (IM) set new standards in the treatment of chronic myeloid leukemia (CML). However, emergence of resistance to IM became a major therapeutic challenge. Bosutinib (SKI-606), a 7-alkoxy-3-quinolinecarbonitrile, functions as a dual inhibitor of SRC and ABL kinases, and preclinical studies demonstrated a high antiproliferative activity in human and murine CML cell lines. In ongoing Phase I/II clinical trials, bosutinib yielded promising results revealing high clinical efficacy, good tolerability and reduced toxicity in IM-resistant or -intolerant CML patients. In this article, we provide an overview on the mechanism of action, and the preclinical and currently available clinical data for bosutinib. Owing to its favorable toxicity profile and its high antileukemic activity, bosutinib is a promising novel treatment option for patients with CML. A recently initiated, randomized open-label Phase III clinical study will clarify its role in first-line therapy of Philadelphia chromosome-positive chronic-phase CML.",
keywords = "Aniline Compounds, Animals, Antineoplastic Agents, Clinical Trials as Topic, Drug Evaluation, Preclinical, Fusion Proteins, bcr-abl, Humans, Leukemia, Myelogenous, Chronic, BCR-ABL Positive, Nitriles, Protein Kinase Inhibitors, Proto-Oncogene Proteins c-abl, Quinolines, src-Family Kinases",
author = "Gunhild Keller and Philippe Schafhausen and Brummendorf, {Tim H}",
year = "2009",
month = oct,
day = "1",
doi = "10.1586/ehm.09.42",
language = "English",
volume = "2",
pages = "489--97",
journal = "EXPERT REV HEMATOL",
issn = "1747-4086",
publisher = "Expert Reviews Ltd.",
number = "5",

}

RIS

TY - JOUR

T1 - Bosutinib: a dual SRC/ABL kinase inhibitor for the treatment of chronic myeloid leukemia

AU - Keller, Gunhild

AU - Schafhausen, Philippe

AU - Brummendorf, Tim H

PY - 2009/10/1

Y1 - 2009/10/1

N2 - The tyrosine kinase inhibitor imatinib mesylate (IM) set new standards in the treatment of chronic myeloid leukemia (CML). However, emergence of resistance to IM became a major therapeutic challenge. Bosutinib (SKI-606), a 7-alkoxy-3-quinolinecarbonitrile, functions as a dual inhibitor of SRC and ABL kinases, and preclinical studies demonstrated a high antiproliferative activity in human and murine CML cell lines. In ongoing Phase I/II clinical trials, bosutinib yielded promising results revealing high clinical efficacy, good tolerability and reduced toxicity in IM-resistant or -intolerant CML patients. In this article, we provide an overview on the mechanism of action, and the preclinical and currently available clinical data for bosutinib. Owing to its favorable toxicity profile and its high antileukemic activity, bosutinib is a promising novel treatment option for patients with CML. A recently initiated, randomized open-label Phase III clinical study will clarify its role in first-line therapy of Philadelphia chromosome-positive chronic-phase CML.

AB - The tyrosine kinase inhibitor imatinib mesylate (IM) set new standards in the treatment of chronic myeloid leukemia (CML). However, emergence of resistance to IM became a major therapeutic challenge. Bosutinib (SKI-606), a 7-alkoxy-3-quinolinecarbonitrile, functions as a dual inhibitor of SRC and ABL kinases, and preclinical studies demonstrated a high antiproliferative activity in human and murine CML cell lines. In ongoing Phase I/II clinical trials, bosutinib yielded promising results revealing high clinical efficacy, good tolerability and reduced toxicity in IM-resistant or -intolerant CML patients. In this article, we provide an overview on the mechanism of action, and the preclinical and currently available clinical data for bosutinib. Owing to its favorable toxicity profile and its high antileukemic activity, bosutinib is a promising novel treatment option for patients with CML. A recently initiated, randomized open-label Phase III clinical study will clarify its role in first-line therapy of Philadelphia chromosome-positive chronic-phase CML.

KW - Aniline Compounds

KW - Animals

KW - Antineoplastic Agents

KW - Clinical Trials as Topic

KW - Drug Evaluation, Preclinical

KW - Fusion Proteins, bcr-abl

KW - Humans

KW - Leukemia, Myelogenous, Chronic, BCR-ABL Positive

KW - Nitriles

KW - Protein Kinase Inhibitors

KW - Proto-Oncogene Proteins c-abl

KW - Quinolines

KW - src-Family Kinases

U2 - 10.1586/ehm.09.42

DO - 10.1586/ehm.09.42

M3 - SCORING: Journal article

C2 - 21083014

VL - 2

SP - 489

EP - 497

JO - EXPERT REV HEMATOL

JF - EXPERT REV HEMATOL

SN - 1747-4086

IS - 5

ER -