^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG CLASS:

    DDX5 degrader

    Related drugs:
    10d
    Design, synthesis and investigation of biological activity and mechanism of fluoroaryl-substituted derivatives at the FL118 position 7. (PubMed, Eur J Med Chem)
    Interestingly, although both 7h and SN38 exhibited similar inhibitory effects on Top1 activity, only 7h, and not SN38, could inhibit DDX5. These findings not only pave the way for deeper mechanistic explorations of FL118 and its derivatives in cancer research but also position the identified compound 7h as a promising candidate for further development.
    Journal
    |
    DDX5 (DEAD-Box Helicase 5)
    |
    FL118
    2ms
    FL118 Enhances Therapeutic Efficacy in Colorectal Cancer by Inhibiting the Homologous Recombination Repair Pathway through Survivin-RAD51 Downregulation. (PubMed, Cancers (Basel))
    Given that SN38 is the active metabolite of irinotecan, FL118 reduces cell viability and RAD51 in SN38-resistant LOVO cells. Our findings provide effective insights into the antitumor activity of FL118 and its potential as a therapeutic agent for overcoming irinotecan resistance in CRC.
    Journal
    |
    HRD (Homologous Recombination Deficiency) • RAD51 (RAD51 Homolog A) • BIRC5 (Baculoviral IAP repeat containing 5)
    |
    BIRC5 expression
    |
    irinotecan • FL118
    8ms
    FL118 Is a Potent Therapeutic Agent against Chronic Myeloid Leukemia Resistant to BCR-ABL Inhibitors through Targeting RNA Helicase DDX5. (PubMed, Int J Mol Sci)
    Furthermore, FL118 potently induced apoptosis not only in Ba/F3 cells expressing BCR-ABL, but also in those expressing the BCR-ABL T315I mutant, which is resistant to BCR-ABL inhibitors. Collectively, these results revealed that DDX5 is a critical therapeutic target in CML and that FL118 is an effective candidate compound for the treatment of BCR-ABL inhibitor-resistant CML.
    Journal
    |
    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • BIRC5 (Baculoviral IAP repeat containing 5) • CASP3 (Caspase 3) • DDX5 (DEAD-Box Helicase 5)
    |
    BIRC5 expression • BCR expression
    |
    FL118
    8ms
    FL118 for Treating Patients With Advanced Pancreatic Ductal Adenocarcinoma (clinicaltrials.gov)
    P1, N=84, Not yet recruiting, Roswell Park Cancer Institute | Trial completion date: May 2027 --> Oct 2027 | Initiation date: Apr 2024 --> Oct 2024 | Trial primary completion date: May 2027 --> Oct 2027
    Trial completion date • Trial initiation date • Trial primary completion date • Metastases
    |
    FL118