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 interactions

In particular, the ABL kinase domain mutation T315I is resistant to Imatinib and second-generation ABL TKIs (e.g., nilotinib, Dasatinib, and Bosutinib). [source, 2015]
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]
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]
Thus, Dasatinib, an ATP-competitive protein TYROSINE kinase inhibitor, when used at therapeutic concentrations, inhibits the activity of Abl, Bcr-Abl, Src-family kinases and several additional kinases, including Src and Btk family members, c-Kit, PDGFR, and Eph receptors [27]. [source, 2016]
Therefore, Dasatinib might disrupt this pathway signaling, as NF-kB activation is Src TYROSINE kinase-dependent in macrophages [22]. [source, 2016]
Dasatinib, a second-generation TYROSINE kinase inhibitor, was chosen for our study because it is safe, presents potent antifibrotic effects, and has a lower cost [8]. [source, 2016]
These orphan drugs are Imiglucerase, sapropterin dihydrochloride, recombinant coagulation Factor VIII, coagulation factor VIIa, human coagulation Factor VIII, human prothrombin complex concentrate, bosentan, Iloprost, ambrisentan, recombinant human Growth hormone, Busulfan, teniposide, Mitoxantrone, Imatinib, Dasatinib, nilotinib, meisoindigo, Arsenious Acid, homoharringtonine, rituximab, sorafenib, Danazol, Riluzole and poractant alfa. [source, 2016]
Four approved drugs including ambrisentan, Somatropin, Dasatinib and meisoindigo were not available in the hospitals surveyed. [source, 2016]
Erlotinib, afatinib, and Dasatinib were purchased as 10 mM stocks dissolved in DMSO (Selleckchem). [source, 2016]
The combined treatment with Dasatinib (5 μM) and Doxorubicin (25 nM) significantly decreased cell viability of hMSC-TERT20-CE8 compared to treatment with Doxorubicin alone: 0.50 (95% CI: 0.48; 0.52) versus 0.78 (95% CI: 0.69; 0.90), respectively, p = 0.002. [source, 2016]