Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations. SRC-family protein-tyrosine kinases interact with variety of cell-surface receptors and participate in intracellular signal transduction pathways; tumorigenic forms can occur through altered regulation or expression of the endogenous protein and by way of virally-encoded kinase genes.
The risk of major arterial adverse events in chronic myeloid leukaemia patients may significantly differ between tyrosine kinase inhibitors, suggests a meta-analysis published in Leukemia & Lymphoma.
The risk and impact of cardiovascular adverse events in long-term users of tyrosine kinase inhibitors for chronic myeloid leukaemia is highlighted in a review published in the Journal of Clinical Oncology.
Avillion LLP, a co-developer of late-stage pharmaceutical assets, announces the completion of enrolment in a global Phase III clinical trial called "BFORE," which is designed to assess the effectiveness and safety of BOSULIF (bosutinib) as a first-line treatment for patients with chronic phase Philadelphia chromosome positive (Ph+) chronic myelogenous leukemia (CML).
Researchers have discovered how a common mutation in a high-risk leukemia subtype drives the cancer's aggressiveness and have identified drugs that may work with existing precision medicines to improve survival. St. Jude Children's Research Hospital scientists led the study, which was published online today in the journal Cancer Cell.
Allogeneic haematopoietic stem cell transplantation can be considered for chronic- and accelerated-phase chronic myeloid leukaemia patients with prior exposure to second-generation tyrosine kinase inhibitors, say Polish researchers.
Allogeneic haematopoietic stem cell transplantation can be considered for chronic- and accelerated-phase chronic myeloid leukaemia patients with prior exposure to second-generation tyrosine kinase inhibitors, say Polish researchers.
Chronic myeloid leukaemia patients with rare BCR-ABL fusions may be missed by quantitative polymerase chain reaction, research suggests.
Clinicians testing the drug dasatinib, approved for several blood cancers, had hoped it would slow the aggressive growth of the deadly brain cancer glioblastoma; however, clinical trials to date have not found any benefit. Researchers at Mayo Clinic, who conducted one of those clinical trials, believe they know why dasatinib failed — and what to do about it.
The likelihood of complications associated with tyrosine kinase inhibitor therapy in patients with chronic myeloid leukaemia may be reduced by considering patient factors and differences in the toxicity profiles of the different drug options, a review suggests.
Treatment with a second-generation tyrosine kinase inhibitor prevents progression to blast crisis in chronic myeloid leukaemia patients with high levels of cancerous inhibitor of PP2A, research suggests.
A review of the European LeukemiaNet guidelines on the care of patients with chronic myeloid leukaemia highlights the need for research into the timing and use of second-line and third-line tyrosine kinase inhibitors.
A Spanish study suggests that bosutinib can help improve or maintain response in patients with chronic myeloid leukaemia after treatment failure of three previous tyrosine kinase inhibitors.
A research team from The Scripps Research Institute, Mayo Clinic and other institutions has identified a new class of drugs that in animal models dramatically slows the aging process—alleviating symptoms of frailty, improving cardiac function and extending a healthy lifespan.
Phase I/II clinical trial data support the use of bosutinib as second- or third-line tyrosine kinase inhibitor therapy in Japanese patients with Philadelphia chromosome-positive chronic myeloid leukaemia.
Timing may be decisive when it comes to overcoming cancer's ability to evade treatment. By hitting breast cancer cells with a targeted therapeutic immediately after chemotherapy, researchers from Brigham and Women's Hospital (BWH) were able to target cancer cells during a transitional stage when they were most vulnerable, killing cells and shrinking tumors in the lab and in pre-clinical models.
PF-114, a selective tyrosine kinase inhibitor, is active against native and mutated forms of the BCR–ABL oncogene in Philadelphia chromosome-positive leukaemias, according to preclinical cellular and in vivo results published in Leukemia.
Patients with chronic myelogenous leukaemia resistant or intolerant to at least one second-generation tyrosine kinase inhibitor have a higher probability of achieving a response to the third-generation TKI ponatinib than to a further second-generation TKI, research indicates.
The uncontrolled growth of cancer cells arises from their ability to hijack the cell’s normal growth program and checkpoints. Usually after therapy, a second cancer-signaling pathway will open after the primary one shuts down — creating an ingenious escape route for the cancer cell to survive. The answer, say Case Western Reserve researchers, is to anticipate and block that back-up track by prescribing two drugs from the start.
ARIAD Pharmaceuticals, Inc. today announced that the Committee for Medicinal Products for Human Use of the European Medicines Agency has adopted its final opinion on Iclusig (ponatinib) following the recommendations made by the Pharmacovigilance Risk Assessment Committee earlier this month.
A leukemia drug called dasatinib shows promise for treating skin, breast and several other cancers, according to researchers at Loyola University Chicago Stritch School of Medicine.