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.

Latest findings

Dasatinib (DAS; Bristol-Myers Squibb, New York, NY, USA), which has been widely studied for the treatment of cancer [4,5], is a second-generation oral multitarget inhibitor of several TYROSINE kinases, including Abl and Bcr-Abl family members, Src and Btk family members, c-Kit, PDGFR, and Eph receptors [6,7]. [source, 2016]
We hypothesized that Dasatinib would attenuate pulmonary fibrosis, ameliorate inflammatory responses, and improve lung function in experimental acute silicosis. [source, 2016]
For this purpose, we investigated the potential efficacy and mechanisms of Dasatinib in the treatment of silica-induced lung fibrosis. [source, 2016]
Fourteen days after administration of silica or saline, animals were further randomized to receive Dimethyl sulfoxide (DMSO 1% in saline solution, 100 μL, oral gavage) or Dasatinib (DAS 1 mg/kg body weight in DMSO 1%, 100 μL, oral gavage) during 14 days (Fig 1). [source, 2016]
Supernatant was then removed; cells were washed with 1× PBS, and then incubated with Dasatinib (100 ng/mL medium) or regular medium for 24 hours. [source, 2016]
Dasatinib minimized the expression of both cytokines (45.7% and 47.9%, respectively) (Fig 3). [source, 2016]
Dasatinib did not reduce the number of macrophages either in lung parenchyma or in granuloma (Fig 4, Table D in S1 File). [source, 2016]
However, Dasatinib increased the number of M2 macrophages in lung parenchyma (712.3%) and granuloma (336.5%) in animals with acute silicosis (Fig 6, Table F in S1 File). [source, 2016]
Dasatinib led to reductions in collagen fiber deposition and TGF-β (Fig 7, Table G in S1 File). [source, 2016]
In the model of acute silicosis used herein, Dasatinib improved lung mechanics and led to a reduction of fraction area of granuloma, neutrophils in lung tissue and granuloma, M1 macrophages in lung parenchyma and granuloma, fraction area of collapsed alveoli, collagen fiber content in lung parenchyma, protein levels of IL-1β, TNF-α, and TGF-β, and increased M2 macrophages in lung parenchyma and granuloma. [source, 2016]