Latest research on Dasatinib

Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML). The main targets of Dasatinib, are BCRABL, SRC, Ephrins and GFR.

Dasatinib dosage

The 1 mg/kg dose of Dasatinib was chosen on the basis of pilot studies and studies in experimental endotoxin-induced acute lung injury conducted in our lab. [source, 2016]
In dose response studies, HT29-BSRwt cells were treated with increasing concentrations of two inhibitors under clinical investigation (Dasatinib or saracatinib) for 2h following which bioluminescence activity in cells was monitored with IVIS spectrum system. [source, 2016]
Luciferase activity increased in a dose-dependent manner for both inhibitors, but saracatinib induced a greater increase in complemented Firefly luciferase activity than Dasatinib. [source, 2016]
Dasatinib also caused a significant dose dependent increase in phosphorylation of FAK at the auto-phosphorylation site Y397 in non-metastatic 769-P and 786-O cells (Fig. 3a–c). [source, 2016]
Dasatinib showed a significant dose dependent response on apoptosis, proliferation and motility in early non-metastatic 769-P and 786-O ccRCC cell lines (Fig. 4). [source, 2016]
Though bone marrow examination indicated that the patient was still in the chronic phase, considering the patient’s condition of disease, Dasatinib was used, and the dosage of Dasatinib was 100 mg daily. [source, 2015]
After taking Dasatinib, severe myelosuppression occurred in this patient, especially the platelet count, so we adjusted the dosage of Dasatinib considering both the disease and the patient’s count of platelet (Figure 1). [source, 2015]
During WST cell viability assays, tumor cells were treated after adhesion with sorafenib (0–8 uM), Dasatinib (0–1000 nM), canertinib (0–10 uM) or crizotinib (0–12 uM) for 48h, in which the doses were based on literature. [source, 2015]
Finally, Dasatinib treatment not only reduced ECM deposition but also improved ventricular function and geometry during PO, indicating that this drug used at appropriate lower doses may offer therapeutic benefits to patients with chronic PO. [source, 2015]
In CML patients, Dasatinib is given at a dose of 100–140 mg/day and is reported to exert a low level of cardiotoxicity [27, 28]. [source, 2015]