The deregulated tyrosine kinase activity of the BCR-ABL fusion protein is the cause of malignant transformation in almost all cases of chronic myelogenous leukaemia (CML), making BCR-ABL an ideal target for pharmacological inhibition. Signal transduction inhibitor (STI571) (formerly CGP57 148B), is an ABL specific, tyrosine kinase inhibitor. In preclinical studies, it has been shown to selectively kill BCR-ABL expressing cells, both in-vitro and in vivo. The results of clinical studies to date are highly encouraging and STI571 promises to be an important addition to the therapy of CML.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1046/j.1365-2796.2001.00823.x | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Body mass index affects imatinib exposure: Real-world evidence from TDM with adaptive dosing.
Fundam Clin Pharmacol
February 2025
PRISM Biogénopôle La Timone University Hospital of Marseille, APHM, Marseille, France.
Background: Imatinib is the treatment of elderly or frail patients with chronic myeloid leukemia (CML). Trough levels of around 1000 ng/ml are considered as the target exposure.
Objectives: We searched for baseline parameters associated with imatinib pharmacokinetics, and studied the clinical impact of subsequent adaptive dosing.
[Efficacy and Safety of Flumatinib and Imatinib as First-line Treatments for Newly-diagnosed Chronic Myeloid Leukemia in Chronic Phase: A Real-world Study].
Zhongguo Shi Yan Xue Ye Xue Za Zhi
December 2024
Department of Hematology, The Affiliated Hospital of North Sichuan Medical College, Nanchong 637000, Sichuan Province, China.
Objective: To compare the efficacy and safety of flumatinib (FM) and imatinib (IM) as first-line treatment in newly-diagnosed patients with chronic myeloid leukemia in chronic phase (CML-CP) in real world.
Methods: A total of 84 newly-diagnosed CP-CML patients in our center from December 2019 to December 2022 were retrospectively analyzed. Among them, 32 cases received FM as first-line treatment, and 52 cases received IM.
Chronic myelogenous leukemia coexpressing V-e16a2, V-e13a2, e13a2, and e14a2 fusion transcripts: a case report and review of the literature.
Front Oncol
December 2024
Institute of Hematology, The Second Hospital of Shanxi Medical University, Taiyuan, China.
The coexistence of three or more transcripts in one patient with chronic myeloid leukemia (CML) is rarely reported. Thus, the disease progression and drug response are still unknown. This case report aimed to explore the drug response of CML with variant transcripts and to enrich the clinical treatment of rare types of CML.
View Article and Find Full Text PDFIdentification of novel BCR::ABL1 kinase domain mutation in patients with chronic myeloid leukaemia and imatinib resistance.
Malays J Pathol
December 2024
National Institutes of Health, Institute for Medical Research, Cancer Research Centre, Haematology Unit, 40170 Shah Alam, Selangor, Malaysia.
Introduction: The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs imatinib mesylate (IM) binding capacity, thus contributing to IM resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML) patients. Our study aims to determine the frequency of BCR::ABL1 KD mutations in CML patients with IM resistance.
View Article and Find Full Text PDFInfluence of CYP2C8*3 and ABCG2 C421A genetic polymorphisms on trough concentration and molecular response of imatinib in Egyptian patients with chronic myeloid leukemia.
Cancer Chemother Pharmacol
December 2024
Department of Medical Pharmacology, Faculty of Medicine, Assiut University, Assiut, 71515, Egypt.
Purpose: The treatment landscape for chronic myeloid leukemia (CML) has been revolutionized by the introduction of imatinib, a tyrosine kinase inhibitor, which has transformed the disease from a fatal condition into a manageable chronic illness for a substantial number of patients. Despite this, some individuals do not respond adequately to the treatment, and others may experience disease progression even with continued therapy. This study examined how CYP2C8*3 (G416A; rs11572080) and ABCG2 C421A (rs2231142) single nucleotide polymorphisms (SNPs) affect the plasma trough concentration and therapeutic response of imatinib in Egyptian CML patients.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!