The high remission rates observed in patients with chronic myelogenous leukemia who receive Imatinib mesylate (Gleevec) indicate that targeted therapy for hematological malignancies is achievable. At the same time, progress in cellular biology over the past decade has resulted in a better understanding of the process of malignant transformation, a better classification of subtypes of each disea...

Imatinib (Gleevec) (formerly STI571) has demonstrated high levels of efficacy in chronic myelogenous leukemia (CML) and gastrointestinal stromal tumors (GIST) and has been used in more than 12,000 patients participating in clinical trials. Experience from clinical trials with imatinib has largely demonstrated the drug to be well tolerated in humans. Common side effects, usually manageable, incl...

Signal transduction therapy for cancer targets specific molecular elements that are essential for survival of the tumor. Gleevec has a profound effect on early phase chronic myeloid leukemia because it inhibits the major driving factor of the tumor, BCR-ABL. Almost all other cancers depend on several factors, and blocking a single signal transduction factor is largely ineffective. Effective sig...

Tyrosine kinase inhibitors are a new class of anticancer drugs, that are capable of directly interacting with the catalytic site of the target enzyme and thereby inhibiting catalysis. Therapeutically useful tyrosine kinase inhibitors are not specific for a single tyrosine kinase, but rather they are selective against a limited number of tyrosine kinases. The success of imatinib-mesylate (Gleeve...

New and innovative cancer treatments are appearing at an astonishing rate. Although the array of new approaches seems breathtaking, most can be grouped into a few categories based on underlying purpose. For example, with our greater understanding of the genetic defects that predispose to malignant cell growth has come the idea of therapeutic agents targeted to a single mutant protein. This appr...

Molecularly targeted therapy is a hot topic in oncology, and the development of imatinib mesylate (Gleevec) for gastrointestinal stromal tumors (GISTs) is one of our best examples of the successful translation of basic science research into effective treatment of malignancy. Dr. Eisenberg has thoroughly researched the impetus for the use of imatinib in GISTs and has methodically reviewed the re...

The palladium-catalyzed defluorinative coupling of 1-aryl-2,2-difluoroalkenes with boronic acids is described. Broad functional-group tolerance arises from a redox-neutral process by a palladium(II) active species which is proposed to undergo a β-fluoride elimination to afford the products. The monofluorostilbene products were formed with excellent diastereoselectivity (≥50:1) in all cases, and...

The lessons learned from the specifically ”targeted” treatment of patients with chronic myeloid leukemia (CML) using imatinib (Gleevec) are now being applied with sometimes dramatic success in a variety of other tumors in which critical driving mutations have been identified, including some, such as malignant melanoma and lung cancer, that are notoriously resistant to other treatments. Sadly, b...

although chronic myelogenous leukemia in pregnancy is rare, its management and treatment is more difficult and complicated. treatment of patients with chronic myelogenous leukemia includes bone marrow transplantation, however in less than 30% of patients the donor’s organ would be accepted. to this end, cytotoxic therapy is considered as an alternative therapeutic option. this option provides s...