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    Association details:
    Biomarker:BTK C481S
    Cancer:Chronic Lymphocytic Leukemia
    Drug:Jaypirca (pirtobrutinib) (BTK inhibitor)
    Direction:Sensitive
    Evidence:
    Evidence Level:
    Sensitive: C3 – Early Trials
    Source:
    ASH 2019
    Title:

    Results from a First-in-Human, Proof-of-Concept Phase 1 Trial in Pretreated B-Cell Malignancies for Loxo-305, a Next-Generation, Highly Selective, Non-Covalent BTK Inhibitor

    Published date:
    11/06/2019
    Excerpt:
    At doses ≥50 mg QD, LOXO-305 exposure exceeded the calculated IC90 for wild-type and C481S mutated BTK….Phase 1 data with LOXO-305 demonstrate a favorable safety profile and provide proof-of-concept evidence of efficacy in heavily pretreated CLL and MCL patients, including patients with acquired resistance to available BTKis and venetoclax.
    DOI:
    https://doi.org/10.1182/blood-2019-127509
    Trial ID:
    BRUIN
    Evidence Level:
    Sensitive: D – Preclinical
    Source:
    ASH 2019
    Title:

    LOXO-305: Targeting C481S Bruton Tyrosine Kinase in Patients with Ibrutinib-Resistant CLL

    Published date:
    11/06/2019
    Excerpt:
    Our findings show that LOXO-305 potently inhibits cell survival and BCR signaling in both treatment naïve and C481S CLL patient cells, and therefore may prove an effective treatment in both treatment naïve and ibrutinib-resistant CLL patients.
    DOI:
    10.1182/blood-2019-124362