^
    Contact us  to learn more about
    our Premium Content:  News alerts, weekly reports and conference planners
    DRUG:

    ceralasertib (AZD6738)

    i
    Other names: AZD6738, AZD 6738, AZD-6738
    Company:
    AstraZeneca
    Drug class:
    ATR inhibitor
    Related drugs:
    7d
    Phase 1 study of ceralasertib, an ATR kinase inhibitor, in combination with durvalumab in patients with recurrent or metastatic NSCLC or HNSCC. (PubMed, Br J Cancer)
    Ceralasertib plus durvalumab was tolerated and associated with antitumour activity in advanced/metastatic NSCLC and HNSCC.
    P1 data • Journal
    |
    ATR (Ataxia telangiectasia and Rad3-related protein)
    |
    Imfinzi (durvalumab) • ceralasertib (AZD6738)
    9d
    D907HC00001: A Phase I Dose Escalation and Dose Expansion Study to Investigate the Pharmacokinetics and Safety of Subcutaneous Durvalumab. (2025-521639-34-00)
    P1, N=4, Not yet recruiting, AstraZeneca AB
    New P1 trial
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR wild-type • ALK wild-type
    |
    Imfinzi (durvalumab) • Imjudo (tremelimumab-actl) • ceralasertib (AZD6738)
    11d
    Liposomal Vitamin C as a Modulator of the Efficacy of Ceralasertib Therapy in Ovarian Cancer. (PubMed, Int J Mol Sci)
    The formation of DNA double-strand breaks suggests replication fork collapse. Our findings demonstrates that this synthetic targeted therapy, combining a novel liposomal formulation of VitC with an ATR inhibitor, not only enhances DNA damage and the cytotoxic efficacy of ceralasertib but also effectively drives ovarian cancer cells toward cell death.
    Journal
    |
    ACSL4 (Acyl-CoA Synthetase Long Chain Family Member 4)
    |
    ceralasertib (AZD6738)
    15d
    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, Active, not recruiting, National Cancer Institute (NCI) | Suspended --> Active, not recruiting
    Enrollment closed • Checkpoint inhibition
    |
    Imfinzi (durvalumab) • ceralasertib (AZD6738)
    22d
    Testing the Combination of Two Anti-cancer Drugs, DS-8201a and AZD6738, for The Treatment of Advanced Solid Tumors Expressing the HER2 Protein or Gene, The DASH Trial (clinicaltrials.gov)
    P1, N=51, Recruiting, National Cancer Institute (NCI) | Trial completion date: Mar 2026 --> Mar 2027 | Trial primary completion date: Mar 2026 --> Mar 2027
    Trial completion date • Trial primary completion date
    |
    CD4 (CD4 Molecule)
    |
    HER-2 positive • HER-2 amplification • HER-2 expression
    |
    Enhertu (fam-trastuzumab deruxtecan-nxki) • ceralasertib (AZD6738)
    24d
    Targeted therapy for DNA damage response and homologous recombination repair defects: The Olaparib Combinations trial. (PubMed, Cancer)
    The study failed to meet its primary end point of ORR. DDR and homologous recombination repair defects are not consistently actionable with olaparib as monotherapy or in combination with other targeted therapies in a histology-agnostic manner.
    Journal • PARP Biomarker
    |
    HRD (Homologous Recombination Deficiency) • ARID1A (AT-rich interaction domain 1A)
    |
    ARID1A mutation
    |
    Lynparza (olaparib) • Truqap (capivasertib) • ceralasertib (AZD6738)
    25d
    ATR Blockade Potentiates the Effects of Genotoxic Agents In Vitro and Promotes Antitumor Immunity in a Mouse Model of Non-Small Cell Lung Cancer. (PubMed, Cancers (Basel))
    These results demonstrate that ATR blockade concurrently enhances the efficacy of genotoxic agents and immune checkpoint inhibitors, thus paving the way for combination therapies in NSCLC.
    Preclinical • Journal • PD(L)-1 Biomarker • IO biomarker
    |
    CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
    |
    cisplatin • ceralasertib (AZD6738)
    28d
    VIOLETTE: To Assess Safety and Efficacy of Agents Targeting DNA Damage Repair With Olaparib Versus Olaparib Monotherapy. (clinicaltrials.gov)
    P2, N=273, Active, not recruiting, AstraZeneca | Trial completion date: Dec 2025 --> Sep 2026
    Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    Lynparza (olaparib) • adavosertib (AZD1775) • ceralasertib (AZD6738)
    2ms
    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)
    2ms
    ATARI: ATr Inhibitor in Combination With Olaparib/Durvalumab (MEDI4736) in Gynaecological Cancers With ARId1A Loss or no Loss (clinicaltrials.gov)
    P2, N=174, Active, not recruiting, Institute of Cancer Research, United Kingdom | Recruiting --> Active, not recruiting | Trial completion date: Apr 2026 --> Aug 2026 | Trial primary completion date: Apr 2026 --> Aug 2026
    Enrollment closed • Trial completion date • Trial primary completion date
    |
    MUC16 (Mucin 16, Cell Surface Associated)
    |
    Lynparza (olaparib) • Imfinzi (durvalumab) • ceralasertib (AZD6738)
    2ms
    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)
    2ms
    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)