^
    14d
    D5330C00004: Ascending Doses of Ceralasertib in Combination With Chemotherapy and/or Novel Anti Cancer Agents (clinicaltrials.gov)
    P1/2, N=357, Active, not recruiting, AstraZeneca | Trial completion date: Dec 2025 --> Jun 2026
    Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ATM (ATM serine/threonine kinase) • HRD (Homologous Recombination Deficiency) • BRCA (Breast cancer early onset) • RAD51C (RAD51 paralog C) • RAD51D (RAD51 paralog D)
    |
    HER-2 negative • HRD • PALB2 mutation • RAD51C mutation • BRCA mutation
    |
    Lynparza (olaparib) • carboplatin • Imfinzi (durvalumab) • ceralasertib (AZD6738) • saruparib (AZD5305)
    16d
    TUVASTRAT: Tuvusertib in Astrocytoma With ATRX Mutation (clinicaltrials.gov)
    P2, N=56, Recruiting, Grupo Español de Investigación en Neurooncología
    New P2 trial
    |
    TP53 (Tumor protein P53) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • ATRX (ATRX Chromatin Remodeler)
    |
    TP53 mutation
    |
    tuvusertib (M1774)
    16d
    Tuvusertib Combined With Niraparib or Lartesertib in Participants With Epithelial Ovarian Cancer (DDRiver EOC 302) (clinicaltrials.gov)
    P2, N=63, Active, not recruiting, EMD Serono Research & Development Institute, Inc. | Trial completion date: Jan 2028 --> Jun 2026 | Trial primary completion date: Jan 2028 --> Sep 2025
    Trial completion date • Trial primary completion date
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency)
    |
    BRCA1 mutation • HRD
    |
    Zejula (niraparib) • tuvusertib (M1774) • lartesertib (M4076)
    17d
    GEINO-2401: Efficacy of Tuvusertib in Recurrent IDH mutant Astrocytoma with ATRX mutation, a phase II prospective trial. (2025-521843-19-00)
    P1/2, N=56, Recruiting, Grupo Espanol De Investigacion En Neurooncologia
    New P1/2 trial
    |
    TP53 (Tumor protein P53) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • ATRX (ATRX Chromatin Remodeler)
    |
    TP53 mutation
    |
    tuvusertib (M1774)
    19d
    Design, synthesis and anti-breast cancer activity evaluation of 6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidine-based PARP1/ATR dual inhibitors. (PubMed, J Enzyme Inhib Med Chem)
    Mechanistically, 38a arrested cell cycle progression, induced apoptosis, inhibited colony formation and migration, and suppressed DNA damage repair pathways, outperforming combined Niraparib and AZD6738. These findings underscore the therapeutic potential of PARP1/ATR dual inhibitors for breast cancer and support further investigation.
    Journal • BRCA Biomarker • PARP Biomarker
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
    |
    BRCA2 mutation • BRCA1 mutation
    |
    Zejula (niraparib) • ceralasertib (AZD6738)
    22d
    Efficacy of the ATR inhibitor ceralasertib in patients with ARID1A-deficient gynecologic and other solid tumor malignancies. (PubMed, Clin Cancer Res)
    Ceralasertib monotherapy demonstrated promising anti-tumor activity in ARID1A-deficient gynecologic malignancies. Tumor molecular and immune correlates may inform the further development of ATR inhibitors in this patient population.
    Journal
    |
    ARID1A (AT-rich interaction domain 1A)
    |
    ARID1A mutation
    |
    ceralasertib (AZD6738)
    29d
    Targeting Galectin-9 to overcome immunosuppression and potentiate ATR inhibitor therapy. (PubMed, Cancer Lett)
    CD8+ T cell depletion completely abrogates the anti-tumor effects, suggesting their essential role in mediating therapeutic responses. These findings establish Gal-9 upregulation as a critical adaptive immune resistance mechanism constraining ATRi efficacy, providing a compelling rationale for clinical translation of ceralasertib/Gal-9 blockade combinations.
    Journal
    |
    CD8 (cluster of differentiation 8) • HAVCR2 (Hepatitis A Virus Cellular Receptor 2) • STING (stimulator of interferon response cGAMP interactor 1) • LGALS9 (Galectin 9)
    |
    ceralasertib (AZD6738)
    1m
    DDRiver Solid Tumours 301: Tuvusertib (M1774) in Participants With Metastatic or Locally Advanced Unresectable Solid Tumors (DDRiver Solid Tumors 301) (clinicaltrials.gov)
    P1, N=161, Active, not recruiting, EMD Serono Research & Development Institute, Inc. | Trial completion date: Jan 2026 --> Jan 2027 | Trial primary completion date: Jan 2026 --> Jan 2027
    Trial completion date • Trial primary completion date • First-in-human
    |
    ARID1A (AT-rich interaction domain 1A) • ATRX (ATRX Chromatin Remodeler)
    |
    ATM mutation • ARID1A mutation
    |
    Zejula (niraparib) • tuvusertib (M1774)
    1m
    ATR inhibitors: from targeting the DNA damage response to exploiting synthetic lethality-A paradigm shift in Cancer therapy. (PubMed, Bioorg Chem)
    We provide a detailed analysis of the structure-activity relationships (SAR) of leading clinical candidates, including berzosertib, ceralasertib, and elimusertib, focusing on strategic chemical modifications such as scaffold hopping and sulfoximine substitution to optimize selectivity and druggability. Critical challenges, specifically dose-limiting hematological toxicities and acquired resistance, are analyzed alongside the search for robust predictive biomarkers. By synthesizing current pharmacological and clinical data, this work outlines the trajectory for next-generation ATR-targeted precision medicine.
    Review • Journal
    |
    ATR (Ataxia telangiectasia and Rad3-related protein)
    |
    berzosertib (M6620) • ceralasertib (AZD6738) • elimusertib (BAY 1895344)
    1m
    Loss of BOK increases vulnerability of p53 deficient non-small cell lung cancer cells to ATR inhibition through its role in uridine metabolism. (PubMed, Cell Death Differ)
    We exploited this vulnerability by inhibiting the ATR-mediated DNA damage response pathway with the selective ATR inhibitor ceralasertib (AZD6738)...Given the frequent inactivation of p53 in lung cancer, our study offers a rationale for clinical exploration of ATR inhibitors, in combination with standard chemotherapy, in the context of reduced BOK function. Future investigations into the broader role of BOK in genomic stability and nucleotide metabolism may uncover additional therapeutic strategies for cancers with repressed BOK.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2)
    |
    ceralasertib (AZD6738)
    1m
    An Phase Ib/II Clinical Trial of TCC1727 Combination Therapy in Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=266, Recruiting, Beijing Tide Pharmaceutical Co., Ltd
    New P1/2 trial
    |
    EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • NRAS (Neuroblastoma RAS viral oncogene homolog) • MSI (Microsatellite instability) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
    |
    EGFR mutation • MSI-H/dMMR • BRAF mutation • NRAS mutation • RAS mutation • RET mutation • MET mutation
    |
    Lynparza (olaparib) • topotecan • Andewei (benmelstobart)
    1m
    Testing the Addition of AZD6738 (Ceralasertib) to Immunotherapy to Increase Time Without Cancer for Patients With Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P3, N=630, Suspended, National Cancer Institute (NCI) | Recruiting --> Suspended
    Trial suspension • Checkpoint inhibition
    |
    Imfinzi (durvalumab) • ceralasertib (AZD6738)