^
    3years
    Novel preclinical patient-derived lung cancer models reveal inhibition of HER3 and MTOR signaling as therapeutic strategies for NRG1 fusion-positive cancers. (PubMed, J Thorac Oncol)
    We identify the MTOR pathway as a candidate vulnerability in NRG1 fusion-positive lung adenocarcinoma that may warrant further pre-clinical evaluation, with the eventual goal of finding additional therapeutic options for patients in whom ERBB-directed therapy fails. Moreover, our results uncover heterogeneity in downstream oncogenic signaling among NRG1-rearranged cancers, possibly histology-dependent, the therapeutic significance of which requires additional investigation.
    Preclinical • Journal
    |
    ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • NRG1 (Neuregulin 1) • SLC3A2 (Solute Carrier Family 3 Member 2) • EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1)
    |
    NRG1 fusion
    |
    sirolimus • GSK2849330 • QTORIN 3.9% (rapamycin topical)
    4years
    ImmunoPET imaging to assess target engagement: Experience from Zr-anti-HER3 mAb (GSK2849330) in patients with solid tumors. (PubMed, J Nucl Med)
    In this immunoPET study, dose-dependent inhibition of tumor uptake of Zr-GSK2849330 by unlabeled mAb confirmed target engagement of mAb to the HER3 receptor. This study further validates the use of immunoPET to directly visualize tissue drug disposition in patients with a non-invasive approach and to measure target engagement at the site of action, offering the potential for dose selection.
    Clinical • Journal
    |
    EGFR (Epidermal growth factor receptor) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3)
    |
    GSK2849330