Preferred Label : Avutometinib and Defactinib;
NCIt synonyms : Avutometinib and Defactinib Co-packaged Formulation; Avutometinib and Defactinib Co-pack; Avutometinib/Defactinib; Avmapki Plus Fakzynja;
NCIt definition : An orally bioavailable co-packaged formulation composed of avutometinib, an inhibitor
of the serine/threonine protein kinases Raf and mitogen-activated protein kinase kinase
(MAP2K, MAPK/ERK kinase, or MEK), and defactinib, a focal adhesion kinase (FAK) inhibitor,
with antineoplastic and antiangiogenic activities. Upon oral administration of avutometinib
and defactinib, avutometinib specifically targets, binds to and inhibits the kinase
activities of Raf and MEK, resulting in the inhibition of Raf/MEK-mediated signal
transduction pathways. This results in the inhibition of Raf/MEK-dependent tumor cell
proliferation and survival. Defactinib targets, binds to and inhibits FAK, which may
prevent the integrin-mediated activation of several downstream signal transduction
pathways, including those involving RAS/MEK/extracellular signal-regulated kinase
(ERK) and PI3K/Akt, thereby inhibiting tumor cell migration, proliferation, survival,
and tumor angiogenesis. The RAS/RAF/MEK/ERK signaling pathway is often dysregulated
in human cancers and plays a key role in tumor cell proliferation, differentiation
and survival. The tyrosine kinase FAK, a signal transducer for integrins, is normally
activated by binding to integrins in the extracellular matrix (ECM) but may be upregulated
and constitutively activated in various tumor cell types.;
Drug name : Avmapki Fakzynja;
Origin ID : C217093;
has_target
- is_component_of_chemotherapy_regimen
