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Association details:
Biomarker:HER-2 V777L
Cancer:Gastric Cancer
Drug:Tukysa (tucatinib) (HER2 inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: D – Preclinical
Title:

Abstract 4222: Tucatinib, a selective small molecule HER2 inibitor, is active in HER2 mutant driven tumors

Published date:
05/15/2020
Excerpt:
Tucatinib also potently inhibited the phosphorylation of HER2 in a V777L mutant MCF-10A cell line, and in a colorectal PDX model containing a V777L mutation, tucatinib alone or in combination with trastuzumab induced tumor regressions...Taken together, these results support the idea that HER2 selective inhibition by tucatinib can block oncogenic signaling elicited by mutant HER2, and that it could potentially provide clinical benefit in patients with cancers with activating HER2 mutations.
DOI:
10.1158/1538-7445.AM2020-4222