Preferred Label : EGFR/HER2 Mutant-selective Inhibitor BH-30643;
NCIt synonyms : Mutant-selective EGFR/HER2 Inhibitor BH-30643; EGFR/HER2 Inhibitor BH-30643; Mutant-selective OMNI-EGFR (TM) Inhibitor BH-30643;
NCIt definition : An orally bioavailable, mutant-selective, reversible macrocyclic inhibitor of human
epidermal growth factor receptor (EGFR) and epidermal growth factor receptor 2 (HER2),
with potential antineoplastic activity. Upon oral administration, EGFR/HER2 mutant-selective
inhibitor BH-30643 targets, reversibly binds to, and inhibits the activity of EGFR
with selective mutations, including, but not limited to, classical mutations, exon
20 insertion (Ex20ins) activating mutations as well as various resistance mutations,
such as ex19del/T790M, ex19del/C797S, ex19del/T790M/C797S, L858R/T790M, L858R/C797S,
and L858R/T790M/C797S. In addition, BH-30643 reversibly binds to and inhibits HER2
mutations, including ex20ins mutations. This prevents EGFR- and HER2-mediated signaling
and may result in the inhibition of tumor growth in certain mutant EGFR/HER2-expressing
tumors. EGFR and HER2, receptor tyrosine kinases mutated or overexpressed in many
tumor cell types, play major roles in tumor cell proliferation and tumor vascularization.
By largely sparing wild-type (WT) EGFR, BH-30643 may decrease the risk of EGFR-related
toxicities. Since BH-30643 concurrently targets activating mutations in EGFR and HER2,
it reduces the chances of resistance.;
Molecule name : BH 30643; BH-30643;
Origin ID : C215012;
concept_is_in_subset
- has_target
