NCIt definition : The hydrochloride salt form of dordaviprone, a water soluble, orally bioavailable
inhibitor of the serine/threonine protein kinase Akt (protein kinase B) and extracellular
signal-regulated kinase (ERK), with potential antineoplastic activity. Upon administration,
dordaviprone binds to and inhibits the activity of Akt and ERK, which may result in
inhibition of the phosphatidylinositol 3-kinase (PI3K)/Akt signal transduction pathway
as well as the mitogen-activated protein kinase (MAPK)/ERK-mediated pathway. This
may lead to the induction of tumor cell apoptosis mediated by tumor necrosis factor
(TNF)-related apoptosis-inducing ligand (TRAIL)/TRAIL death receptor type 5 (DR5)
signaling in AKT/ERK-overexpressing tumor cells. The PI3K/Akt signaling pathway and
MAPK/ERK pathway are upregulated in a variety of tumor cell types and play a key role
in tumor cell proliferation, differentiation and survival by inhibiting apoptosis.
In addition, dordaviprone is able to cross the blood-brain barrier.;
Semantic type(s)