^
    3ms
    BGB-A317-3111-10188-101: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov)
    P1/2, N=97, Completed, BeiGene | Active, not recruiting --> Completed
    Trial completion • Combination therapy
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR
    |
    paclitaxel • Tevimbra (tislelizumab-jsgr) • Brukinsa (zanubrutinib) • BGB-10188
    3ms
    A highly selective PI3Kδ inhibitor BGB-10188 shows superior preclinical anti-tumor activities and decreased on-target side effects on colon. (PubMed, Neoplasia)
    BGB-10188 showed significant antitumor effects in human B cell lymphoma xenograft models as single agent or in combination with the BTK inhibitor zanubrutinib. BGB-10188 showed significant Treg inhibition in blood but not in colon, along with less drug accumulation in colon compared with idelalisib, which is an approved PI3Kdelta inhibitor with high incidence of gastrointestinal side effects in clinic. In summary, BGB-10188 is a novel PI3Kδ inhibitor with high selectivity, potency and improved safety profile shown in preclinical studies, which is showing the potential as a best-in-class PI3Kδ inhibitor.
    Preclinical • Journal • Adverse events
    |
    PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta)
    |
    Brukinsa (zanubrutinib) • Zydelig (idelalisib) • BGB-10188
    5ms
    BGB-A317-3111-10188-101: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov)
    P1/2, N=97, Active, not recruiting, BeiGene | Recruiting --> Active, not recruiting | Trial completion date: Dec 2025 --> Sep 2024 | Trial primary completion date: May 2025 --> Sep 2024
    Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy
    |
    MSI (Microsatellite instability)
    |
    paclitaxel • Tevimbra (tislelizumab-jsgr) • Brukinsa (zanubrutinib) • BGB-10188
    7ms
    BGB-A317-3111-10188-101: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov)
    P1/2, N=113, Recruiting, BeiGene | Trial completion date: Feb 2025 --> Dec 2025
    Trial completion date • Combination therapy
    |
    MSI (Microsatellite instability)
    |
    paclitaxel • Tevimbra (tislelizumab-jsgr) • Brukinsa (zanubrutinib) • BGB-10188
    over1year
    BGB-A317-3111-10188-101: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov)
    P1/2, N=126, Recruiting, BeiGene | Trial completion date: Nov 2025 --> Feb 2025
    Trial completion date • Combination therapy
    |
    MSI (Microsatellite instability)
    |
    MSI-H/dMMR
    |
    paclitaxel • Tevimbra (tislelizumab-jsgr) • Brukinsa (zanubrutinib) • BGB-10188
    over2years
    BGB-A317-3111-10188-101: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov)
    P1/2, N=150, Recruiting, BeiGene | Trial completion date: Apr 2025 --> Nov 2025
    Trial completion date • Combination therapy
    |
    PD-L1 (Programmed death ligand 1) • MSI (Microsatellite instability)
    |
    MSI-H/dMMR
    |
    paclitaxel • Tevimbra (tislelizumab-jsgr) • Brukinsa (zanubrutinib) • BGB-10188
    over2years
    PI3K Inhibitors for the Treatment of Chronic Lymphocytic Leukemia: Current Status and Future Perspectives. (PubMed, Cancers (Basel))
    The dual PI3Kδ/γ inhibitor duvelisib is approved for use in CLL patients but with similar toxicities to idelalisib. Umbralisib, a highly selective inhibitor of PI3Kδ and casein kinase-1ε (CK1ε), was found to be efficient and safe in monotherapy and in combination regimens in phase 3 trials in patients with CLL. Novel PI3Kis are under evaluation in early phase clinical trials. In this paper we present the mechanism of action, efficacy and toxicities of PI3Ki approved in the treatment of CLL and developed in clinical trials.
    Review • Journal
    |
    TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • IGH (Immunoglobulin Heavy Locus) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • PIK3CB (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta)
    |
    TP53 mutation • TP53 mutation + Chr del(17p)
    |
    Aliqopa (copanlisib) • Zydelig (idelalisib) • Copiktra (duvelisib) • Ukoniq (umbralisib) • parsaclisib (INCB50465) • BGB-10188 • zandelisib (ME-401)
    over4years
    Brief Title: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov)
    P1/2, N=150, Recruiting, BeiGene | Not yet recruiting --> Recruiting
    Clinical • Enrollment open • Combination therapy
    |
    PD-L1 (Programmed death ligand 1) • MSI (Microsatellite instability)
    |
    MSI-H/dMMR
    |
    Tevimbra (tislelizumab-jsgr) • Brukinsa (zanubrutinib) • BGB-10188
    almost5years
    Brief Title: Study of BGB-10188 as Monotherapy, and in Combination With Zanubrutinib, and Tislelizumab (clinicaltrials.gov)
    P1/2, N=150, Not yet recruiting, BeiGene
    Clinical • New P1/2 trial • Combination therapy
    |
    PD-L1 (Programmed death ligand 1) • MSI (Microsatellite instability)
    |
    MSI-H/dMMR
    |
    Tevimbra (tislelizumab-jsgr) • Brukinsa (zanubrutinib) • BGB-10188