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Association details:
Biomarker:NRAS mutation
Cancer:Non Small Cell Lung Cancer
Drug:KO-947 (ERK inhibitor)
Direction:Sensitive
Evidence:
Evidence Level:
Sensitive: C2 – Inclusion Criteria
Title:

First-in-Human Study of KO-947 in Non-Hematological Malignancies

Excerpt:
...Malignancy of non-squamous histology that carries a BRAF, KRAS, NRAS or HRAS mutation(s)....
Trial ID:
Evidence Level:
Sensitive: D – Preclinical
Title:

Abstract 5168: KO-947, a potent ERK inhibitor with robust preclinical single agent activity in MAPK pathway dysregulated tumors

Excerpt:
KO-947 blocks ERK signaling and proliferation of tumor cells exhibiting dysregulation of MAPK pathway signaling, including mutations in BRAF, NRAS or KRAS, at low nanomolar concentrations...In cell-line derived xenograft studies, the drug profoundly suppresses ERK signaling for up to five days after a single dose and induces regressions in RAS- and RAF-mutant melanoma, NSCLC and pancreatic cancer models on administration schedules ranging from daily to weekly.
DOI:
10.1158/1538-7445.AM2017-5168