^
    4d
    Novel therapeutic potential of the PARP inhibitor talazoparib in synovial sarcoma and its combined effect with ATR inhibitor. (PubMed, Discov Oncol)
    Talazoparib combined with ATR inhibitor possesses potential application as a therapeutic option for SS.
    Journal • PARP Biomarker
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    CHEK1 (Checkpoint kinase 1) • ANXA5 (Annexin A5)
    |
    Talzenna (talazoparib) • ceralasertib (AZD6738)
    18d
    POP-ART: A Study on Tuvusertib (Oral ATR Inhibitor) in Combination With PLX038 (Topo1 Inhibitor) in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=10, Terminated, Institut Curie | N=92 --> 10 | Trial completion date: Sep 2029 --> Nov 2025 | Recruiting --> Terminated | Trial primary completion date: Sep 2028 --> Nov 2025; Although no safety signal has been observed, given that the industrial development of tuvusertib has been halted regardless of the results, we see no scientific and ethical justification for continuing the study
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
    |
    PLX038 • tuvusertib (M1774)
    27d
    Rb1 deficiency induces synthetic lethality with ATR and PKMYT1 coinhibition in breast cancer cell lines and patient-derived xenografts. (PubMed, Sci Transl Med)
    Here, we demonstrate that coinhibition of ATR (RP-3500) and PKMYT1 (RP-6306) induces synthetic lethality in Rb1-deficient breast cancers by disrupting both S-G2 and G2-M checkpoints...Clinically, a retrospective analysis of stage IV breast cancer datasets revealed that Rb1-low tumors display reduced DNA repair pathway activity in triple-negative and CDK4/6 inhibitor-resistant luminal breast cancers. These results identify Rb1 loss as a predictive biomarker for ATR/PKMYT1-targeted therapy, offering a potential precision treatment strategy for advanced breast cancers.
    Preclinical • Journal
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    RB1 (RB Transcriptional Corepressor 1) • PKMYT1 (Protein Kinase Membrane Associated Tyrosine/Threonine 1)
    |
    camonsertib (RP-3500)
    1m
    AUSTRAL: Phase II Study of Radiotherapy Followed by Durvalumab and Ceralasertib in Stage III NSCLC Patients With Thoracic Relapses +/- Oligometastases After PACIFIC Regimen (clinicaltrials.gov)
    P2, N=21, Recruiting, Mario Negri Institute for Pharmacological Research | Not yet recruiting --> Recruiting | Trial completion date: Jan 2028 --> Jan 2029 | Trial primary completion date: Jan 2027 --> Jun 2028
    Enrollment open • Trial completion date • Trial primary completion date
    |
    Imfinzi (durvalumab) • ceralasertib (AZD6738)
    1m
    A Study of RP-3500 in Combination With Standard Radiation Therapy in People With Solid Tumor Cancer (clinicaltrials.gov)
    P1/2, N=49, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Recruiting --> Active, not recruiting | N=84 --> 49
    Enrollment closed • Enrollment change
    |
    ATM (ATM serine/threonine kinase)
    |
    ATM mutation
    |
    camonsertib (RP-3500)
    1m
    Testing the Addition of an Anti-Cancer Drug, Camonsertib, to Radiation Therapy for Recurrent Head and Neck Squamous Cell Carcinoma (clinicaltrials.gov)
    P1, N=39, Not yet recruiting, National Cancer Institute (NCI) | Initiation date: Dec 2025 --> Mar 2026
    Trial initiation date • Tumor mutational burden
    |
    camonsertib (RP-3500)
    1m
    A Study to Evaluate the Safety and Pharmacokinetics of Ceralasertib in Combination With Durvalumab in Chinese Patients With Advanced Solid Tumours (clinicaltrials.gov)
    P1, N=14, Active, not recruiting, AstraZeneca | Trial completion date: Oct 2025 --> Mar 2026
    Trial completion date
    |
    Imfinzi (durvalumab) • ceralasertib (AZD6738)
    2ms
    Ceralasertib, an ATR kinase inhibitor, as monotherapy in Japanese patients with advanced solid malignancies: Results from a phase 1 study. (PubMed, Invest New Drugs)
    Ceralasertib monotherapy was generally well tolerated in Japanese patients with advanced solid tumors. The small number of patients enrolled prevents definitive conclusions on the efficacy of ceralasertib monotherapy to be made.
    P1 data • Journal
    |
    ATR (Ataxia telangiectasia and Rad3-related protein)
    |
    ceralasertib (AZD6738)
    2ms
    Prognostic alternative mRNA splicing in lung adenocarcinoma. (PubMed, Front Oncol)
    Molecular docking identified YM-201636 and VE-822 (Berzosertib) as potential drugs targeting CDKN2A, both showing promise for LUAD treatment in vivo. PASEs constitute a comprehensive biomarker for predicting prognosis and monitoring the TIME in LUAD patients. Specifically, CDKN2A stands out as a potential prognostic biomarker and drug target for LUAD.
    Journal
    |
    CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
    |
    berzosertib (M6620)
    2ms
    NCI 10211: A Phase II, Single-Arm Study of Berzosertib in Combination with Irinotecan in Patients with Advanced TP53 Mutant Gastroesophageal Cancer. (PubMed, Oncologist)
    This novel combination of ATR inhibitor berzosertib with irinotecan did not lead to objective responses in patients with TP53-mutated, advanced gastroesophageal adenocarcinoma. The combination regimen was well tolerated without unexpected adverse events. This trial was registered with ClinicalTrials.gov (NCT03641313).
    P2 data • Journal
    |
    TP53 (Tumor protein P53)
    |
    TP53 mutation
    |
    irinotecan • berzosertib (M6620)
    2ms
    LATIFY: A Phase III Study of Ceralasertib Plus Durvalumab Versus Docetaxel in Patients With Non Small Cell Lung Cancer (NSCLC) Whose Disease Progressed On or After Prior Anti PD (L)1 Therapy And Platinum Based Chemotherapy (clinicaltrials.gov)
    P3, N=594, Active, not recruiting, AstraZeneca | Trial completion date: Oct 2025 --> Oct 2026
    Trial completion date
    |
    EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase)
    |
    EGFR wild-type • ALK wild-type
    |
    Imfinzi (durvalumab) • docetaxel • ceralasertib (AZD6738)