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    Association details:
    Biomarker:BRAF V600E
    Cancer:Colorectal Cancer
    Drug:temuterkib (LY3214996) (ERK2 inhibitor, ERK1 inhibitor)
    Direction:Sensitive
    Evidence:
    Evidence Level:
    Sensitive: C2 – Inclusion Criteria
    Source:
    clinicaltrials.gov
    Title:

    A Study of LY3214996 Administered Alone or in Combination With Other Agents in Participants With Advanced/Metastatic Cancer

    Excerpt:
    ...- Part E: Metastatic BRAF V600E colorectal cancer....
    Trial ID:
    NCT02857270
    Evidence Level:
    Sensitive: D – Preclinical
    Source:
    AACR-II 2020
    Title:

    Temporal inhibition of ERK is sufficient for tumor growth inhibition in KRAS-mutant or BRAF-mutant tumors

    Published date:
    05/15/2020
    Excerpt:
    Colo205 BRAF V600E colorectal carcinoma and HCT116 KRAS G13D colorectal carcinoma. Additionally, an infusion study with LY3214996 was conducted in rats implanted with HCT116 colorectal carcinoma tumors…Overall assessment of the data in different models suggested that ≥50% target inhibition for 8-16h is enough for significant tumor growth inhibition and regressions by an ERK inhibitor in BRAF-mutant or KRAS-mutant tumors...Therefore, we believe that the PK profile of LY3214996 offers flexibility with dose and schedule to balance efficacy and safety, and to achieve a better therapeutic index in combination therapy for RAS/MAPK pathway altered cancers.