Novel aspects of therapy with the dual Src and Abl kinase inhibitor bosutinib in chronic myeloid leukemia.
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Novel aspects of therapy with the dual Src and Abl kinase inhibitor bosutinib in chronic myeloid leukemia. / von Amsberg, Gunhild; Brümmendorf, Tim.
In: EXPERT REV ANTICANC, Vol. 12, No. 9, 9, 2012, p. 1121-1127.Research output: SCORING: Contribution to journal › SCORING: Journal article › Research › peer-review
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TY - JOUR
T1 - Novel aspects of therapy with the dual Src and Abl kinase inhibitor bosutinib in chronic myeloid leukemia.
AU - von Amsberg, Gunhild
AU - Brümmendorf, Tim
PY - 2012
Y1 - 2012
N2 - The dual Src/Abl kinase inhibitor bosutinib (SKI-606) targets the tyrosine kinase brc-abl, the key enzyme in the development of chronic myeloid leukemia (CML). In clinical trials, bosutinib yielded promising results with regard to efficacy, tolerability and toxicity in first-, second- and third-line therapy of CML patients. Remarkably, bosutinib is able to overcome most imatinib-resistant BCR-ABL1-1 mutations except V299L and T315I. Mostly, low-to-moderate grade gastrointestinal toxicitis are the most common treatment-emergent adverse events observed under bosutinib. Unlike other tyrosine kinase inhibitors approved for CML treatment to date, bosutinib shows only minimal inhibitory activity against c-KIT and the PDGF receptor. This may be causative for its favorable hematologic toxicity profile. In this review, the authors give an overview on the mechanism of action and currently available preclinical and clinical data for bosutinib in CML.
AB - The dual Src/Abl kinase inhibitor bosutinib (SKI-606) targets the tyrosine kinase brc-abl, the key enzyme in the development of chronic myeloid leukemia (CML). In clinical trials, bosutinib yielded promising results with regard to efficacy, tolerability and toxicity in first-, second- and third-line therapy of CML patients. Remarkably, bosutinib is able to overcome most imatinib-resistant BCR-ABL1-1 mutations except V299L and T315I. Mostly, low-to-moderate grade gastrointestinal toxicitis are the most common treatment-emergent adverse events observed under bosutinib. Unlike other tyrosine kinase inhibitors approved for CML treatment to date, bosutinib shows only minimal inhibitory activity against c-KIT and the PDGF receptor. This may be causative for its favorable hematologic toxicity profile. In this review, the authors give an overview on the mechanism of action and currently available preclinical and clinical data for bosutinib in CML.
KW - Humans
KW - Randomized Controlled Trials as Topic
KW - Treatment Outcome
KW - Disease-Free Survival
KW - Mutation
KW - Drug Resistance, Neoplasm
KW - Biological Availability
KW - Therapeutic Equivalency
KW - Aniline Compounds/administration & dosage/adverse effects/pharmacokinetics
KW - Fusion Proteins, bcr-abl/antagonists & inhibitors/genetics
KW - Gastrointestinal Diseases/chemically induced
KW - Leukemia, Myelogenous, Chronic, BCR-ABL Positive/drug therapy/genetics
KW - Nitriles/administration & dosage/adverse effects/pharmacokinetics
KW - Pharmacovigilance
KW - Piperazines/administration & dosage/adverse effects/pharmacokinetics
KW - Protein Kinase Inhibitors/administration & dosage/adverse effects/pharmacokinetics
KW - Pyrimidines/administration & dosage/adverse effects/pharmacokinetics
KW - Quinolines/administration & dosage/adverse effects/pharmacokinetics
KW - Humans
KW - Randomized Controlled Trials as Topic
KW - Treatment Outcome
KW - Disease-Free Survival
KW - Mutation
KW - Drug Resistance, Neoplasm
KW - Biological Availability
KW - Therapeutic Equivalency
KW - Aniline Compounds/administration & dosage/adverse effects/pharmacokinetics
KW - Fusion Proteins, bcr-abl/antagonists & inhibitors/genetics
KW - Gastrointestinal Diseases/chemically induced
KW - Leukemia, Myelogenous, Chronic, BCR-ABL Positive/drug therapy/genetics
KW - Nitriles/administration & dosage/adverse effects/pharmacokinetics
KW - Pharmacovigilance
KW - Piperazines/administration & dosage/adverse effects/pharmacokinetics
KW - Protein Kinase Inhibitors/administration & dosage/adverse effects/pharmacokinetics
KW - Pyrimidines/administration & dosage/adverse effects/pharmacokinetics
KW - Quinolines/administration & dosage/adverse effects/pharmacokinetics
M3 - SCORING: Journal article
VL - 12
SP - 1121
EP - 1127
JO - EXPERT REV ANTICANC
JF - EXPERT REV ANTICANC
SN - 1473-7140
IS - 9
M1 - 9
ER -
