^
    5d
    Acalabrutinib (ACP-196) in Combination With ACP-319, for Treatment of B-Cell Malignancies (clinicaltrials.gov)
    P1/2, N=40, Completed, Acerta Pharma BV | Active, not recruiting --> Completed | Trial completion date: Apr 2026 --> Oct 2025
    Trial completion • Trial completion date
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    Calquence (acalabrutinib) • ACP-319
    7d
    Dual PI3Kδ/γ inhibition enhances radiotherapy-induced antitumor immunity via macrophage-dependent cGAS-STING-type I interferon signaling. (PubMed, Biochem Biophys Res Commun)
    In the syngeneic CT26 model, dual PI3Kδ/γ inhibition (BR101801 or duvelisib), unlike selective PI3Kδ inhibition (idelalisib), synergized with RT (7.5 Gy) to suppress tumor growth and induce durable immune memory. Furthermore, blockade of the IFN-I receptor abolished CD8+ T cell infiltration and M2-like macrophage suppression, abrogating antitumor efficacy and confirming the requirement for IFN-I signaling. These findings identify macrophage-driven activation of the cGAS-STING-IFN-I axis as a key mechanism by which dual PI3Kδ/γ inhibition potentiates RT, providing a strong scientific rationale for its development as an immunomodulatory radiosensitizer.
    Journal
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    CD8 (cluster of differentiation 8) • CXCL10 (Chemokine (C-X-C motif) ligand 10) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • PIK3CD (Phosphatidylinositol-4 5-Bisphosphate 3-Kinase Catalytic Subunit Delta) • STING (stimulator of interferon response cGAMP interactor 1) • CGAS (Cyclic GMP-AMP Synthase)
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    Zydelig (idelalisib) • Copiktra (duvelisib) • bosmolisib (BR101801)
    8d
    Silico, in vitro, and in vivo studies of a 2-substituted quinazolin-4(3H)-one in T-cell acute lymphoblastic leukemia. (PubMed, Toxicol Appl Pharmacol)
    Comparative analysis with idelalisib revealed similar toxicity profiles to Qona11, distinct from vincristine. In vivo studies in NOD/SCID mice bearing Jurkat xenografts showed that Qona11 (100 mg.kg-1) was well tolerated with no systemic toxicity, although it did not inhibit leukemia cell proliferation in immune-independent models. Overall, Qona11 exhibits promising anticancer activity and low systemic toxicity, warranting further preclinical investigation in solid tumor models and combination therapies.
    Preclinical • Journal
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    CASP3 (Caspase 3)
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    Zydelig (idelalisib) • vincristine
    10d
    Phase 2 Study of PI3K Inhibitor Copanlisib in Combination With Fulvestrant in Selected ER+ and/or PR+ Cancers With PI3K (PIK3CA, PIK3R1) and/or PTEN Alterations (clinicaltrials.gov)
    P2, N=7, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Aug 2025 --> Feb 2027
    Trial completion date
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PGR (Progesterone receptor) • PTEN (Phosphatase and tensin homolog) • PIK3R1 (Phosphoinositide-3-Kinase Regulatory Subunit 1) • PI3K (Phosphoinositide 3-kinases)
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    PIK3CA mutation • PTEN deletion
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    fulvestrant • Aliqopa (copanlisib)
    12d
    PI3Kδ Inhibitor Parsaclisib Combined With Chidamide for the Treatment of Relapsed/Refractory Peripheral T-cell Lymphoma (clinicaltrials.gov)
    P1, N=12, Terminated, Henan Cancer Hospital | Phase classification: P1/2 --> P1 | Trial completion date: Feb 2025 --> Aug 2025
    Phase classification • Trial completion date
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    ALK (Anaplastic lymphoma kinase)
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    ALK positive • ALK negative
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    Epidaza (chidamide) • parsaclisib (INCB50465)
    12d
    Efficacy and Safety of Tenalisib in Patients With Metastatic Triple Negative Breast Cancer (TNBC) (clinicaltrials.gov)
    P2, N=40, Recruiting, Rhizen Pharmaceuticals SA | Trial completion date: Mar 2026 --> Mar 2027 | Trial primary completion date: Oct 2025 --> Dec 2026
    Trial completion date • Trial primary completion date
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    tenalisib (RP6530)
    12d
    Integrative bioinformatics and machine learning approach unveils potential biomarkers linking coronary atherosclerosis and glutamine metabolism-associated gene. (PubMed, J Cardiothorac Surg)
    This study successfully discovered nine GlnMgs that are associated with AS. These findings provide valuable insights into potential novel biomarkers for AS and offer prospects for monitoring disease progression.
    Journal
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    MIR21 (MicroRNA 21) • NOS3 (Nitric oxide synthase 3) • SIRT4 (Sirtuin 4)
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    acalisib (GS-9820)
    20d
    HEMA-MED: A Study of Roginolisib in Combination With Ruxolitinib in Patients With Myelofibrosis (MF) Who Are Unresponsive to JAK Inhibitors (clinicaltrials.gov)
    P1/2, N=26, Recruiting, iOnctura | Initiation date: May 2025 --> Nov 2025
    Trial initiation date
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    Jakafi (ruxolitinib) • roginolisib (IOA-244)
    27d
    PDCD1 as a targetable immune checkpoint hub: therapeutic insights for ibrutinib-resistant CLL management. (PubMed, Clin Exp Med)
    Using two independent datasets (GSE249956 and GSE98206), differentially expressed genes (DEGs) were identified between ibrutinib-resistant and sensitive CLL samples. In the broader context, PD-1 expression in CLL cells is linked to active proliferation and immune escape. Overall, our findings emphasize PDCD1's central role in ibrutinib resistance through immune checkpoint pathways and support the rationale for combining BTK inhibitors with immune checkpoint blockade therapies in resistant CLL cases.
    Journal • PD(L)-1 Biomarker • IO biomarker
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    PD-1 (Programmed cell death 1) • ITGB2 (Integrin Subunit Beta 2) • CD1C (CD1c Molecule)
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    PD-L1 expression
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    Imbruvica (ibrutinib) • acalisib (GS-9820)
    1m
    BrUOG360: A phase Ib/II study of copanlisib in combination with rucaparib in patients with metastatic castration-resistant prostate cancer (mCRPC). (PubMed, Cancer Res Commun)
    Copa/R had a favorable safety profile with a signal of efficacy supporting future studies of PARPi with PI3Ki.
    P1/2 data • Journal
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    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • PTEN (Phosphatase and tensin homolog) • CDK12 (Cyclin dependent kinase 12) • FANCA (FA Complementation Group A) • RAD51C (RAD51 paralog C)
    |
    Rubraca (rucaparib) • Aliqopa (copanlisib)
    1m
    Duvelisib Plus Docetaxel In Recurrent/Metastatic HNSCC (clinicaltrials.gov)
    P2, N=26, Completed, Glenn J. Hanna | Active, not recruiting --> Completed
    Trial completion
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression
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    docetaxel • Copiktra (duvelisib)
    1m
    Alpha-enolase influences ATP pool of cytoplasm and lactate homeostasis by regulating glycolysis in gastric cancer. (PubMed, Signal Transduct Target Ther)
    Furthermore, pharmacological studies revealed that metformin combined with copanlisib significantly inhibited tumors by blocking the energy metabolism pathways PI3K/AKT and AMPK/mTOR. Rationally, targeting multiple nodes along the ENO1-ATP/lactate-AMPK/PI3K/AKT-mTOR axis may be effective for GC treatment, as indicated by the significant suppression of tumor growth by metformin (which inhibits ATP production) plus syrosingopine (which disrupts lactate homeostasis). In conclusion, the complex interplay between metabolism and tumor stemness offers novel therapeutic directions and potential treatment strategies for GC.
    Journal
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    ENO1 (Enolase 1)
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    Aliqopa (copanlisib) • metformin • syrosingopine