Preferred Label : Lomonitinib;
NCIt definition : An orally bioavailable inhibitor of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1;
FLK2) mutations and interleukin-1 receptor-associated kinase 4 (IRAK4), with potential
antineoplastic activity. Upon oral administration, lomonitinib targets, binds to and
inhibits the activity of FLT3 mutations, including the FLT3-ITD-F691L gatekeeper mutation,
while sparing the wild-type form of FLT3. This inhibits the proliferation of FLT3
mutant-expressing cancer cells. In addition, lomonitinib targets, binds to, and inhibits
the kinase activity of IRAK4. This inhibits IRAK4-mediated signaling and may reduce
adaptive resistance to FLT3 inhibition as toll-like receptor (TLR) activation plays
an important role in resistance to FLT3 inhibition. FLT3, a class III receptor tyrosine
kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute
myeloid leukemias. IRAK4, a serine/threonine-protein kinase, plays a key role in both
the TLR and IL-1R signaling pathways.;
UNII : U4DPU7W7QU;
CAS number : 2923221-56-9;
Molecule name : ZE46-0134; ZE46 0134;
Origin ID : C215087;
concept_is_in_subset
- has_target
