^
    2years
    Phase 1b Study of the BET Inhibitor GS-5829 as Monotherapy and Combined with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer. (PubMed, Clin Cancer Res)
    GS-5829 was generally tolerated but demonstrated limited efficacy and lack of dose-proportional increases in plasma concentrations in patients with mCRPC.
    P1 data • Journal
    |
    CCR2 (C-C Motif Chemokine Receptor 2) • HEXIM1 (HEXIM P-TEFb Complex Subunit 1)
    |
    Xtandi (enzalutamide capsule) • abiraterone acetate • alobresib (GS-5829)
    4years
    The BET inhibitor GS-5829 targets chronic lymphocytic leukemia cells and their supportive microenvironment. (PubMed, Leukemia)
    The antileukemia activity of GS-5829 increased synergistically in combinations with B-cell receptor signaling inhibitors, the BTK inhibitor ibrutinib, the PI3Kδ inhibitor idelalisib, and the SYK inhibitor entospletinib. In cocultures that mimic the lymph node microenvironment, GS-5829 inhibited signaling pathways within nurselike cells and their growth, indicating that BET inhibitors also can target the supportive CLL microenvironment. Collectively, these data provide a rationale for the clinical evaluation of BET inhibitors in CLL.
    Journal
    |
    BCL2L1 (BCL2-like 1) • SYK (Spleen tyrosine kinase)
    |
    Imbruvica (ibrutinib) • Zydelig (idelalisib) • entospletinib (GS-9973) • alobresib (GS-5829)