drug_type
RELEVANT_DRUG
intervention_type
Small molecule TKI
drug_description
Oral HER2-selective tyrosine kinase inhibitor that blocks HER2 phosphorylation and downstream PI3K/AKT and RAS/RAF/MEK/ERK signaling; designed to spare EGFR.
nci_thesaurus_concept_id
C192219
nci_thesaurus_preferred_term
HER2 Inhibitor ELVN-002
nci_thesaurus_definition
An orally bioavailable, irreversible inhibitor of the receptor tyrosine kinase human epidermal growth factor receptor 2 (HER2; ErbB2; HER-2), with potential antineoplastic activity. Upon oral administration, HER2 inhibitor ELVN-002 selectively binds to and inhibits the activity of HER2 and various HER2 mutants, including Exon 20 insertion mutations (E20IMs), while not inhibiting wild-type (WT) EGFR. This prevents HER2-mediated signaling and may lead to cell death in HER2-expressing tumor cells. HER2, a receptor tyrosine kinase often overexpressed and mutated in a variety of tumor cell types, plays an important role in tumor cell proliferation and tumor vascularization. By sparing WT EGFR, ELVN-002 mostly avoids EGFR-related toxicities.
drug_category
SMALL MOLECULE DRUG
drug_class
Inhibitor
drug_delivery_route
Oral
drug_mechanism_of_action
Oral, irreversible HER2-selective tyrosine kinase inhibitor that binds and inhibits HER2 and HER2 mutants (including exon 20 insertions), blocking HER2 phosphorylation and downstream PI3K/AKT and RAS/RAF/MEK/ERK signaling, while sparing wild‑type EGFR; this suppresses proliferation and can induce death in HER2-expressing tumor cells.
drug_name
ELVN-002
nct_id_drug_ref
NCT06328738