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    DRUG:

    naquotinib (ASP8273)

    i
    Other names: ASP8273
    Company:
    Astellas
    Drug class:
    EGFR inhibitor
    Related drugs:
    over3years
    In vitro and in silico growth inhibitory, anti-ovarian & anti-lung carcinoma effects of 1,5 diarylpenta-1,4-dien-3-one as synthetically modified curcumin analogue. (PubMed, J Biomol Struct Dyn)
    The obtained results were compared with the reference compound 7 and drugs 8-10 (7: GO-035; 8: Quinazolin; 9: Naquotinib and 10: Ribofuranuronamide)...In vitro anti-proliferative activity was tested via MTT method against human ovarian carcinoma (PA-1) and human lung adenocarcinoma (A549) cells and further screened for apoptotic parameters such as nuclear fragmentation and ROS generation. Compound 4 exhibits good dose-dependent anti-proliferative activity (IC 73 and 79.7 µM) against human ovarian carcinoma and human lung adenocarcinoma, respectively.Communicated by Ramaswamy H. Sarma.
    Preclinical • Journal
    |
    EGFR (Epidermal growth factor receptor) • KDR (Kinase insert domain receptor) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
    |
    naquotinib (ASP8273)
    4years
    Beyond osimertinib: The development of 3-generation EGFR Tyrosine Kinase Inhibitors. (PubMed, J Thorac Oncol)
    In this review, we profiled many of the third-generation EGFR TKIs in late stage clinical development (e.g. almonertinib, lazertinib, alflutinib, rezivertinib, ASK120069, SH-1028, D-0316 and abivertinib) of their interim results of phase 1-3 trials and their chemical structures when publicly available. Additionally, we summarized the results of clinical trials that previously reported third-generation EGFR TKIs (rociletinib, olmutinib, nazartinib, maverlertinib) including phase 3 results of rociletinib and naquotinib. We further profiled the next-generation combination clinical trial design of third-generation EGFR TKIs including FLAURA2 (NCT04035486), MARIPOSA (NCT04487080), ACROSS1 (NCT04500704) and ACROSS2 (NCT04500717).
    Review • Journal
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR T790M
    |
    Tagrisso (osimertinib) • Ameile (aumolertinib) • Ivesa (firmonertinib) • Lazcluze (lazertinib) • Xegafri (rociletinib) • nazartinib (EGF816) • Semena (befotertinib) • naquotinib (ASP8273) • Olita (olmutinib) • Rui Bi Da (rezivertinib) • Fujovee (abivertinib) • Sanrisso (rilertinib)
    almost6years
    An Open Study of ASP8273 in Patients With Non-Small-Cell Lung Cancer (NSCLC) Who Have Epidermal Growth Factor Receptor (EGFR) Mutations (clinicaltrials.gov)
    P1/2, N=124, Recruiting, Astellas Pharma Inc
    Clinical • New P1/2 trial
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR expression • EGFR L861Q • EGFR G719X
    |
    naquotinib (ASP8273)