Once-Daily Dasatinib for Treatment of Patients with Chronic Myeloid Leukemia

Abstract

Dasatinib 100 mg once daily has a more favorable risk to benefit assessment compared with the previous 70 mg twice-daily regimen and is now the recommended schedule for patients with CP CML.

Activity of the multikinase inhibitor dasatinib against ovarian cancer cells

“…However, toxicity issues have hampered the clinical development of this compound in epithelial malignancies. Nevertheless, a phase III dose-optimisation study has recently been carried out to compare the aforementioned regimen with others, including dasatinib 100 mg once daily, in patients with CML (Tyler, 2009). The results of this study showed that there was no significant difference in efficacy between these two regimens.…”

“…The safety profile was improved in the 100-mg once-daily dasatinib arm with significantly reduced frequencies of grade 3 -4 thrombocytopenia and all-grade pleural effusions. The number of patients who had to discontinue, reduce, or interrupt their dosage was also less among patients taking dasatinib 100 mg once daily (Tyler, 2009).…”

Use and costs of oral anticancer agents in the Netherlands in the period 2000–2008

“…It is also given for the treatment of gastrointestinal stromal tumours (GIST) . Dasatinib and nilotinib have been developed to treat imatinib‐resistant, progressive CML or can be given to patients that do not tolerate imatinib . Because in most CML patients imatinib response can be sustained over a long period, the incidence and the prevalence of the latter drugs are low.…”

Synthesis and Cytotoxicity of Novel 2-Amino-5-Thiazolecarboxamide Derivatives

“…The reaction mixture was stirred at reflux for 6 h. The reaction mixture was condensed, and water (10 mL) was added, extracted with ethyl acetate, washed with saturated NaHCO 3 Scheme 2 Synthetic routes for compounds 8 and 9. Table 1 The cytotoxicity data of 2-amino-5-thiazolecarboxamide derivatives 7a-g, 8 and water. The solvent was removed and purified by flash column chromatography (dichloromethane/methanol=20:1, v/v) to give the compounds 7a-g as white solids.…”

“…7 Among these, Dasatinib is a novel multi-targeted kinase inhibitor recently approved in several countries for the treatment of chronic myelogenous leukaemia (CML) as well as Philadelphia chromosome-positive acute lymphocytic leukaemia. 8,9 Dasatinib exhibits greater potency than imatinib mesylate and inhibits the majority of kinase mutations in imatinib-resistant CML. Unlike imatinib, which binds to the inactive conformation of Bcr-Abl, dasatinib binds to the active form of the enzyme.…”