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    DRUG CLASS:

    DNA PK inhibitor

    Related drugs:
    4d
    Construction and evaluation of a bladder cancer prognosis model based on super-enhancer-associated genes. (PubMed, Discov Oncol)
    Three genes (MXRA7, PLEKHG4B and ATP2B4) were identified to construct a SERG-related model in BLCA, which provides a basis for understanding BLCA pathogenesis and new insights into BLCA treatment.
    Journal
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    KRAS (KRAS proto-oncogene GTPase) • CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
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    KRAS G12C • KRAS G12
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    JQ-1 • AZD8186 • NU7441
    20d
    CAMO959A12103: A clinical trial to learn about the effects of AMO959 given with AAA617 and an androgen receptor pathway inhibitor (ARPI) in adults with PSMA-positive prostate cancer that has spread to other parts of the body.athway inhibitor (ARPI) in adults with PSMA-positive prostate cancer that has spread to other parts of the body. (2025-521859-23-00)
    P1/2, N=61, Not yet recruiting, Novartis Pharma AG
    New P1/2 trial
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    Xtandi (enzalutamide) • abiraterone acetate • Pluvicto (lutetium Lu 177 vipivotide tetraxetan) • Firmagon (degarelix) • Orgovyx (relugolix)
    1m
    Testing the Combination of New Anti-cancer Drug Peposertib With Avelumab and Radiation Therapy for Advanced/Metastatic Solid Tumors and Hepatobiliary Malignancies (clinicaltrials.gov)
    P1/2, N=103, Active, not recruiting, National Cancer Institute (NCI) | Suspended --> Active, not recruiting
    Enrollment closed • Tumor mutational burden
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    Bavencio (avelumab) • peposertib (M3814)
    1m
    Discovery of Novel Heterotetracyclic DNA-Dependent Protein Kinase (DNA-PK) Inhibitors with Improved Oral Bioavailability and Potent Cancer Immunotherapy-Potentiating Activity. (PubMed, J Med Chem)
    Remarkably, D11 exhibited excellent pharmacokinetics in SD rats (oral bioavailability: 42.6%; half-life: 50 h) and outperformed the clinical candidate AZD-7648 in LoVo xenografts (TGI = 72.9% vs 54.6% at 50 mg/kg, p.o.). It also synergized with anti-PD-L1 mAb to enhance CD8+ T-cell infiltration. Overall, D11 is a promising heterotetracyclic DNA-PK inhibitor with superior in vivo efficacy, favorable pharmacokinetics, and immunomodulatory potential, supporting further development.
    Journal
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    CD8 (cluster of differentiation 8)
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    AZD7648
    2ms
    A Study of Bosmolisib (BR101801) in Participants With R/R PTCL. (clinicaltrials.gov)
    P2, N=44, Not yet recruiting, Boryung Pharmaceutical Co., Ltd | Initiation date: Sep 2025 --> Feb 2026
    Trial initiation date
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    bosmolisib (BR101801)
    2ms
    Testing the Combination of New Anti-cancer Drug Peposertib With Avelumab and Radiation Therapy for Advanced/Metastatic Solid Tumors and Hepatobiliary Malignancies (clinicaltrials.gov)
    P1/2, N=103, Suspended, National Cancer Institute (NCI) | Trial completion date: Dec 2025 --> Jul 2027 | Trial primary completion date: Dec 2025 --> Jul 2027
    Trial completion date • Trial primary completion date • Tumor mutational burden
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    Bavencio (avelumab) • peposertib (M3814)
    3ms
    Testing the Addition of an Anti-cancer Drug, M3814, to the Usual Treatment (Mitoxantrone, Etoposide, and Cytarabine) for Relapsed or Refractory Acute Myeloid Leukemia (clinicaltrials.gov)
    P1, N=48, Active, not recruiting, National Cancer Institute (NCI) | Suspended --> Active, not recruiting
    Enrollment closed
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    RARA (Retinoic Acid Receptor Alpha) • PML (Promyelocytic Leukemia) • CD4 (CD4 Molecule)
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    cytarabine • etoposide IV • mitoxantrone • peposertib (M3814) • Starasid (cytarabine ocfosfate)
    3ms
    Concurrent XRD-0394 With Radiation Therapy for High Grade Gliomas (clinicaltrials.gov)
    P1, N=39, Recruiting, NYU Langone Health | Not yet recruiting --> Recruiting | Initiation date: Apr 2025 --> Nov 2025
    Enrollment open • Trial initiation date
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    temozolomide • XRD-0394
    3ms
    NRG-HN008: Testing the Addition of M3814 (Peposertib) to Radiation Therapy for Patients With Advanced Head and Neck Cancer Who Cannot Take Cisplatin (clinicaltrials.gov)
    P1, N=21, Active, not recruiting, National Cancer Institute (NCI) | N=42 --> 21 | Trial completion date: Dec 2025 --> Dec 2026
    Enrollment change • Trial completion date
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    CD4 (CD4 Molecule)
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    peposertib (M3814)
    4ms
    Testing the Addition of An Anti-cancer Drug, M3814 (Peposertib), to the Usual Radiation-Based Treatment (Lutetium Lu 177 Dotatate) for Pancreatic Neuroendocrine Tumors (clinicaltrials.gov)
    P1, N=29, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Oct 2025 --> Jun 2026 | Trial primary completion date: Oct 2025 --> Jun 2026
    Trial completion date • Trial primary completion date
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    peposertib (M3814) • Lutathera (lutetium Lu 177 dotatate)
    4ms
    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)
    4ms
    Testing the Combination of New Anti-cancer Drug Peposertib With Avelumab and Radiation Therapy for Advanced/Metastatic Solid Tumors and Hepatobiliary Malignancies (clinicaltrials.gov)
    P1/2, N=103, Suspended, National Cancer Institute (NCI) | Recruiting --> Suspended
    Trial suspension • Tumor mutational burden
    |
    Bavencio (avelumab) • peposertib (M3814)