^
    7d
    Phase II Study of Radiotherapy Followed by Durvalumab (MEDI4736) and Ceralasertib (AZD6738) in Stage III NSCLC Patients With Thoracic Relapses +/- Oligometastases After PACIFIC Regimen (AUSTRAL) (clinicaltrials.gov)
    P2, N=21, Not yet recruiting, Mario Negri Institute for Pharmacological Research
    New P2 trial
    |
    Imfinzi (durvalumab) • ceralasertib (AZD6738)
    9d
    CORONADO CLL: RP-3500 and Olaparib in DNA Damage Repair Pathway Deficient Relapsed/Refractory Chronic Lymphocytic Leukemia (clinicaltrials.gov)
    P1/2, N=5, Terminated, University of Utah | N=39 --> 5 | Trial completion date: Aug 2027 --> Oct 2024 | Recruiting --> Terminated; This study was terminated due to sponsor de-activation of all programs associated with RP-3500 (camonsertib).
    Enrollment change • Trial completion date • Trial termination
    |
    TP53 (Tumor protein P53) • BCL2 (B-cell CLL/lymphoma 2) • CD20 (Membrane Spanning 4-Domains A1) • SF3B1 (Splicing Factor 3b Subunit 1) • CCND1 (Cyclin D1) • CD5 (CD5 Molecule) • POT1 (Protection of telomeres 1) • FCER2 (Fc Fragment Of IgE Receptor II)
    |
    TP53 mutation • ATM mutation • Chr t(11;14) • SF3B1 mutation
    |
    Lynparza (olaparib) • camonsertib (RP-3500)
    11d
    ABOYA-119: Study of ATRN-119 in Patients with Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=132, Recruiting, Aprea Therapeutics | N=45 --> 132
    Enrollment change • Metastases
    |
    ATRN-119
    17d
    Chemo-Immunotherapy Followed by Durvalumab and Ceralasertib in Treatment Naïve Patients With Extensive Stage Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=30, Recruiting, Muhammad Furqan | Trial completion date: Sep 2024 --> Sep 2025 | Trial primary completion date: Sep 2024 --> Sep 2025
    Trial completion date • Trial primary completion date
    |
    cisplatin • carboplatin • Imfinzi (durvalumab) • etoposide IV • ceralasertib (AZD6738)
    20d
    A Translational Study of the ATR Inhibitor Berzosertib as Monotherapy in Four Molecularly Defined Cohorts of Advanced Solid Tumors. (PubMed, Clin Cancer Res)
    Across cohorts, only SDH-mutant GIST patients experienced prolonged disease control. Despite evidence of target engagement, patients enrolled to all other cohorts had short PFS, suggesting rapid adaptation to ATR inhibitor monotherapy. Among these patients, those with tumors expressing SLFN11 during berzosertib exposure derived the most clinical benefit.
    Journal • Metastases
    |
    ATM (ATM serine/threonine kinase) • SLFN11 (Schlafen Family Member 11) • ATRX (ATRX Chromatin Remodeler) • CHEK1 (Checkpoint kinase 1)
    |
    ATM mutation • ATRX mutation
    |
    berzosertib (M6620)
    24d
    ATR inhibition increases reliance on PARP-mediated DNA repair revealing an improved therapeutic strategy for cervical cancer. (PubMed, Gynecol Oncol)
    Our findings show that ATRi increased reliance on PARP for metabolic viability, the combination of ATRi and PARPi induced synthetic lethality in cervical cancer in vitro, and reduced tumor burden in vivo.
    Journal • PARP Biomarker
    |
    HRD (Homologous Recombination Deficiency) • RAD51 (RAD51 Homolog A) • PARP1 (Poly(ADP-Ribose) Polymerase 1)
    |
    Lynparza (olaparib) • ceralasertib (AZD6738)
    27d
    Genomic biomarkers predict response to combined ATR inhibition and radiotherapy. (PubMed, Clin Cancer Res)
    A recent study reports the novel ATR kinase inhibitor, RP-3500, synergizes with radiation to control Atm-/- tumors in vivo. RP-3500 did not radiosensitize wild-type or Brca-1 deficient tumors, highlighting the need for a genotype-tailored approach.
    Journal • BRCA Biomarker
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA (Breast cancer early onset)
    |
    camonsertib (RP-3500)
    28d
    NCI-2015-01779: Testing the Safety of M6620 (VX-970) When Given With Standard Whole Brain Radiation Therapy for the Treatment of Brain Metastases From Non-small Cell Lung Cancer, Small Cell Lung Cancer, or Neuroendocrine Tumors (clinicaltrials.gov)
    P1, N=15, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Sep 2024 --> Sep 2025
    Trial completion date
    |
    RAD51 (RAD51 Homolog A)
    |
    berzosertib (M6620)
    29d
    Inhibition of ATM or ATR in combination with hypo-fractionated radiotherapy leads to a different immunophenotype on transcript and protein level in HNSCC. (PubMed, Front Oncol)
    The toxic and immunogenic effects of the smKI AZD0156 (ATMi) and VE-822 (ATRi) in combination with a hypo-fractionated scheme of 2x5Gy RT on HPV-negative (HSC4, Cal-33) and HPV-positive (UM-SCC-47, UD-SCC-2) HNSCC cell lines were analyzed as follows: cell death (necrosis, apoptosis; detected by AnxV/PI), expression of immunostimulatory (ICOS-L, OX40-L, TNFSFR9, CD70) and immunosuppressive (PD-L1, PD-L2, HVEM) checkpoint marker using flow cytometry; the release of cytokines using multiplex ELISA and the gene expression of Cal-33 on mRNA level 48 h post-RT. This includes pro-inflammatory signaling induced by RT + ATRi but also anti-inflammatory signals. These findings were confirmed by RNAseq analysis, which further highlighted the immune-suppressive nature of RT + ATMi.
    Journal • Combination therapy • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • IL6 (Interleukin 6) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • PD-L2 (Programmed Cell Death 1 Ligand 2) • CD70 (CD70 Molecule) • ICOS (Inducible T Cell Costimulator) • EDIL3 (EGF Like Repeats And Discoidin Domains 3)
    |
    berzosertib (M6620) • AZD0156
    1m
    Combined MEK1/2 and ATR inhibition promotes myeloma cell death through a STAT3-dependent mechanism in vitro and in vivo. (PubMed, Br J Haematol)
    Co-administration of the ATR inhibitor (ATRi) BAY1895344 (BAY) and MEK1/2 inhibitors, for example, cobimetinib, synergistically increased cell death in diverse MM cell lines...Similar events occurred in highly bortezomib-resistant (PS-R) cells, in the presence of patient-derived conditioned medium, and with alternative ATR (e.g. M1774) and MEK1/2 (trametinib) inhibitors...Finally, the ATR inhibitor/cobimetinib regimen significantly improved survival in MM xenografts, including bortezomib-resistant models, with minimal toxicity. Collectively, these findings suggest that combined ATR/MEK1/2 inhibition triggers dual STAT3 Tyr705 and Ser727 dephosphorylation, pronounced downregulation of cytoprotective targets and MM cell death, warranting attention as a novel therapeutic strategy in MM.
    Preclinical • Journal
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MAP2K1 (Mitogen-activated protein kinase kinase 1) • BCL2L1 (BCL2-like 1) • STAT3 (Signal Transducer And Activator Of Transcription 3) • CD34 (CD34 molecule) • SDC1 (Syndecan 1)
    |
    Mekinist (trametinib) • Cotellic (cobimetinib) • bortezomib • elimusertib (BAY 1895344) • tuvusertib (M1774)
    1m
    Base-excision repair pathway regulates transcription-replication conflicts in pancreatic ductal adenocarcinoma. (PubMed, Cell Rep)
    Co-treatment with ATR inhibitor (VX970) and BER inhibitor (methoxyamine) at clinically relevant doses synergistically enhanced DNA damage and reduced cell proliferation in PDAC cells. The study provides mechanistic insights into the regulation of TRCs in PDAC by the BER pathway, which has biologic and therapeutic implications.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    berzosertib (M6620) • methoxyamine (TRC102)
    1m
    D5330C00004: Ascending Doses of Ceralasertib in Combination With Chemotherapy and/or Novel Anti Cancer Agents (clinicaltrials.gov)
    P1/2, N=466, Recruiting, AstraZeneca | Trial completion date: Jul 2026 --> Mar 2025 | Trial primary completion date: Jul 2026 --> Mar 2025
    Trial completion date • Trial primary 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 • RAD51 mutation
    |
    Lynparza (olaparib) • carboplatin • Imfinzi (durvalumab) • ceralasertib (AZD6738) • saruparib (AZD5305)
    2ms
    ATR inhibition activates cancer cell cGAS/STING-interferon signaling and promotes antitumor immunity in small-cell lung cancer. (PubMed, Sci Adv)
    This study shows that targeting ATR up-regulates major histocompatibility class I expression in preclinical models and SCLC clinical samples collected from a first-in-class clinical trial of ATR inhibitor, berzosertib, with topotecan in patients with relapsed SCLC. Targeting ATR represents a transformative vulnerability of SCLC and is a complementary strategy to induce STING-interferon signaling-mediated immunogenicity in SCLC.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    STING (stimulator of interferon response cGAMP interactor 1)
    |
    berzosertib (M6620) • topotecan
    2ms
    Study of Avelumab and Tuvusertib in Participants With Advanced Urothelial Cancer That Has Progressed on Prior Anti-PD-(L)1 Therapy (JAVELIN DDRiver Bladder) (clinicaltrials.gov)
    P2, N=0, Withdrawn, EMD Serono Research & Development Institute, Inc. | Not yet recruiting --> Withdrawn | N=70 --> 0
    Enrollment change • Trial withdrawal • Combination therapy • Metastases
    |
    Bavencio (avelumab) • tuvusertib (M1774)
    2ms
    Tuvusertib (M1774) in Combination With Cemiplimab in Participants With Non-Squamous NSCLC (DDRiver NSCLC 322) (clinicaltrials.gov)
    P1/2, N=61, Active, not recruiting, EMD Serono Research & Development Institute, Inc. | Recruiting --> Active, not recruiting | N=180 --> 61 | Trial completion date: Sep 2026 --> Mar 2025 | Trial primary completion date: Aug 2026 --> Jun 2024
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date • Combination therapy
    |
    Libtayo (cemiplimab-rwlc) • tuvusertib (M1774)
    3ms
    D5330C00004: Ascending Doses of Ceralasertib in Combination With Chemotherapy and/or Novel Anti Cancer Agents (clinicaltrials.gov)
    P1/2, N=466, Recruiting, AstraZeneca | Trial completion date: Dec 2026 --> Jul 2026 | Trial primary completion date: Dec 2026 --> Jul 2026
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    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)
    |
    Lynparza (olaparib) • carboplatin • Imfinzi (durvalumab) • ceralasertib (AZD6738) • saruparib (AZD5305)
    3ms
    Study to Evaluate IMP9064 as a Monotherapy or in Combination in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=61, Recruiting, Impact Therapeutics, Inc. | Phase classification: P1/2 --> P1
    Phase classification • Combination therapy • Metastases
    |
    senaparib (IMP4297) • IMP9064
    3ms
    Testing the Combination of Two Anti-cancer Drugs, Peposertib (M3814) and M1774 for Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=66, Recruiting, National Cancer Institute (NCI) | Trial completion date: Aug 2024 --> Aug 2026 | Trial primary completion date: Aug 2024 --> Aug 2026
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    ATM (ATM serine/threonine kinase) • ARID1A (AT-rich interaction domain 1A) • CCNE1 (Cyclin E1) • PBRM1 (Polybromo 1) • FBXW7 (F-Box And WD Repeat Domain Containing 7) • ATRX (ATRX Chromatin Remodeler) • ARID1B (AT-Rich Interaction Domain 1B) • ARID2 (AT-Rich Interaction Domain 2) • SMARCA2 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily A, Member 2) • SS18 (SS18 Subunit Of BAF Chromatin Remodeling Complex)
    |
    peposertib (M3814) • tuvusertib (M1774)
    3ms
    M9466 as Single Agent or in Combination With Tuvusertib in Advanced Solid Tumors (DDRiver 501) (clinicaltrials.gov)
    P1, N=70, Recruiting, EMD Serono Research & Development Institute, Inc. | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    tuvusertib (M1774) • M9466
    3ms
    A Study of AZD6738 and Acalabrutinib in Subjects With Relapsed or Refractory Chronic Lymphocytic Leukemia (CLL) (clinicaltrials.gov)
    P1, N=11, Active, not recruiting, Acerta Pharma BV | Trial completion date: Jun 2024 --> Aug 2026
    Trial completion date • Combination therapy
    |
    Calquence (acalabrutinib) • ceralasertib (AZD6738)
    3ms
    Sculpting the tumour microenvironment by combining radiotherapy and ATR inhibition for curative-intent adjuvant immunotherapy. (PubMed, Nat Commun)
    We also observe increased richness in the TCR repertoire and emergence of numerous and large TCR clonotypes that cluster based on antigen specificity in response to NKG2A/PD-L1/ATRi/RT. Collectively, our data point towards potential combination approaches for the treatment of HNSCC.
    Journal
    |
    CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • CD40LG (CD40 ligand) • KLRC1 (Killer Cell Lectin Like Receptor C1)
    3ms
    ATTACC: Study of RP-3500 (Camonsertib) With Niraparib or Olaparib in Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=196, Active, not recruiting, Repare Therapeutics | Recruiting --> Active, not recruiting | Phase classification: P1b/2 --> P1/2
    Enrollment closed • Phase classification • Metastases
    |
    Lynparza (olaparib) • Zejula (niraparib) • camonsertib (RP-3500)
    3ms
    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 primary completion date: May 2025 --> Aug 2025
    Trial primary completion date • Metastases
    |
    EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase)
    |
    Imfinzi (durvalumab) • docetaxel • ceralasertib (AZD6738)
    3ms
    Genotype-Directed Synthetic Cytotoxicity of ATR Inhibition with Radiotherapy. (PubMed, Clin Cancer Res)
    We investigated the synergistic potential of the ATR inhibitor (ATRi) RP-3500 and RT in two Atm-null and isogenic murine models, both in vitro and in vivo...Lastly, early results from our clinical trial showed complete responses in patients. Genotype-directed radiosensitization with ATRi and RT can unleash significant therapeutic benefit and could represent a novel approach to develop more effective combinatorial synthetic cytotoxic RT-based treatments.
    Journal • BRCA Biomarker
    |
    BRCA1 (Breast cancer 1, early onset) • ATM (ATM serine/threonine kinase)
    |
    camonsertib (RP-3500)
    3ms
    An Open-Label Phase 1 Study of Ceralasertib in Japanese Patients With Advanced Solid Malignancies (clinicaltrials.gov)
    P1, N=12, Completed, AstraZeneca | Active, not recruiting --> Completed | Trial completion date: Dec 2024 --> Mar 2024
    Trial completion • Trial completion date • Metastases
    |
    ceralasertib (AZD6738)
    4ms
    Tuvusertib Combined With Niraparib or Lartesertib in Participants With Epithelial Ovarian Cancer (DDRiver EOC 302) (clinicaltrials.gov)
    P2, N=60, Recruiting, EMD Serono Research & Development Institute, Inc. | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy
    |
    Zejula (niraparib) • tuvusertib (M1774) • lartesertib (M4076)
    4ms
    PTEN Depletion Increases Radiosensitivity in Response to Ataxia Telangiectasia-Related-3 (ATR) Inhibition in Non-Small Cell Lung Cancer (NSCLC). (PubMed, Int J Mol Sci)
    Overall, our study demonstrates that ceralasertib and RT combined preferentially sensitises PTEN-depleted NSCLC models in vitro and in vivo, with no impact on early inflammatory response indicative of RP. These findings provide a rationale for evaluating ATR inhibition in combination with RT in NSCLC patients with PTEN mutations.
    Journal
    |
    PTEN (Phosphatase and tensin homolog)
    |
    ceralasertib (AZD6738)
    4ms
    Methylation of FAM110C is a synthetic lethal marker for ATR/CHK1 inhibitors in pancreatic cancer. (PubMed, J Transl Int Med)
    Loss of FAM110C expression sensitizes PDAC cells to VE-822 (an ATR inhibitor) and MK-8776 (a CHK1 inhibitor). FAM110C methylation is a potential diagnostic and prognostic marker in PDAC, and its epigenetic silencing sensitizes PDAC cells to ATR/CHK1 inhibitors.
    Journal • Synthetic lethality
    |
    HMGB1 (High Mobility Group Box 1)
    |
    berzosertib (M6620) • MK-8776
    4ms
    Testing Olaparib and AZD6738 in IDH1 and IDH2 Mutant Tumors (clinicaltrials.gov)
    P2, N=50, Active, not recruiting, National Cancer Institute (NCI) | Suspended --> Active, not recruiting
    Enrollment closed
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
    |
    Lynparza (olaparib) • ceralasertib (AZD6738)
    4ms
    D5330C00004: Ascending Doses of Ceralasertib in Combination With Chemotherapy and/or Novel Anti Cancer Agents (clinicaltrials.gov)
    P1/2, N=466, Recruiting, AstraZeneca | Trial completion date: Aug 2026 --> Dec 2026 | Trial primary completion date: Aug 2026 --> Dec 2026
    Trial completion date • Trial primary completion date • Combination therapy • Metastases
    |
    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)
    |
    Lynparza (olaparib) • carboplatin • Imfinzi (durvalumab) • ceralasertib (AZD6738) • saruparib (AZD5305)
    4ms
    Avelumab and M1774 in ARID1A-mutated Endometrial Cancer (Prior IO) (clinicaltrials.gov)
    P2, N=25, Not yet recruiting, Panagiotis Konstantinopoulos, MD, PhD
    New P2 trial • Combination therapy • IO biomarker
    |
    Bavencio (avelumab) • tuvusertib (M1774)
    4ms
    Dual inhibition of ATR and DNA-PKcs radiosensitizes ATM-mutant prostate cancer. (PubMed, bioRxiv)
    Compound B effectively radiosensitized ATM-deficient CRPC in vitro and in vivo , and impacted replication fork dynamics. Overall, dual targeting of both ATR and DNA-PKcs is necessary to block DDR in ATM-deficient CRPC, and Compound B could be utilized as a novel therapy in combination with irradiation in these patients.
    Journal
    |
    ATM (ATM serine/threonine kinase) • AVEN (Apoptosis And Caspase Activation Inhibitor) • RUVBL1 (RuvB Like AAA ATPase 1)
    4ms
    ATRIUM: A Study of ATG-018 (ATR Inhibitor) Treatment in Patients With Advanced Solid Tumors and Hematological Malignancies (clinicaltrials.gov)
    P1, N=22, Terminated, Antengene Discovery Limited | N=88 --> 22 | Trial completion date: Jun 2024 --> Jan 2024 | Recruiting --> Terminated | Trial primary completion date: Jun 2024 --> Jan 2024; Lack of efficacy of study compound
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date • Metastases
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • ATM (ATM serine/threonine kinase) • ARID1A (AT-rich interaction domain 1A) • MSH2 (MutS Homolog 2) • CDK12 (Cyclin dependent kinase 12) • ATRX (ATRX Chromatin Remodeler) • CHEK2 (Checkpoint kinase 2) • RAD51 (RAD51 Homolog A) • FANCA (FA Complementation Group A) • RAD51B (RAD51 Paralog B) • BRIP1 (BRCA1 Interacting Protein C-terminal Helicase 1) • RAD51C (RAD51 paralog C) • RAD51D (RAD51 paralog D) • BARD1 (BRCA1 Associated RING Domain 1) • NBN (Nibrin Nijmegen Breakage Syndrome 1 (Nibrin)) • FANCF (FA complementation group F) • FANCM (FA Complementation Group M) • FANCD2 (FA Complementation Group D2) • FANCE (FA Complementation Group E) • FANCC (FA Complementation Group C)
    |
    ATG-018
    4ms
    Olaparib With Ceralasertib in Recurrent Osteosarcoma (clinicaltrials.gov)
    P2, N=63, Recruiting, Dana-Farber Cancer Institute | Trial primary completion date: Jun 2024 --> Dec 2024
    Trial primary completion date • Combination therapy
    |
    Lynparza (olaparib) • ceralasertib (AZD6738)
    4ms
    Hypoxia-Responsive Prodrug of ATR Inhibitor, AZD6738, Selectively Eradicates Treatment-Resistant Cancer Cells. (PubMed, Adv Sci (Weinh))
    In addition, ICT10336 exhibited a superior and efficient multicellular penetration ability in 3D tumor models, and selectively eradicated cells at the hypoxic core compared to AZD6738. In summary, the preclinical data demonstrate a new strategy of tumor-targeted delivery of ATR inhibitors with significant potential of enhancing the therapeutic index.
    Journal
    |
    HIF1A (Hypoxia inducible factor 1, alpha subunit)
    |
    ceralasertib (AZD6738)
    4ms
    Phase Ib/II Study of HRS2398 in Combination With Adebrelimab in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=88, Recruiting, Shanghai Hengrui Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Combination therapy • Metastases
    |
    Ariely (adebrelimab)
    5ms
    Combination ATR and PARP Inhibitor (CAPRI) Trial With AZD6738 and Olaparib in Recurrent Ovarian Cancer (clinicaltrials.gov)
    P2, N=86, Active, not recruiting, University of Pennsylvania | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    HRD (Homologous Recombination Deficiency) • BRCA (Breast cancer early onset) • MUC16 (Mucin 16, Cell Surface Associated)
    |
    Lynparza (olaparib) • ceralasertib (AZD6738)
    5ms
    PEPN2112: Elimusertib for the Treatment of Relapsed or Refractory Solid Tumors (clinicaltrials.gov)
    P1/2, N=23, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Jun 2024 --> Dec 2024 | Trial primary completion date: Jun 2024 --> Dec 2024
    Trial completion date • Trial primary completion date
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • ATM (ATM serine/threonine kinase) • MSH2 (MutS Homolog 2) • CDK12 (Cyclin dependent kinase 12) • WT1 (WT1 Transcription Factor) • ATRX (ATRX Chromatin Remodeler) • CHEK2 (Checkpoint kinase 2) • RAD51 (RAD51 Homolog A) • FANCA (FA Complementation Group A) • POLD1 (DNA Polymerase Delta 1) • FOXO1 (Forkhead box O1) • XRCC2 (X-Ray Repair Cross Complementing 2) • ATF1 (Activating Transcription Factor 1) • PAX3 (Paired Box 3)
    |
    elimusertib (BAY 1895344)
    5ms
    MONETTE: A Study of Ceralasertib Monotherapy and Ceralasertib Plus Durvalumab in Patients With Melanoma and Resistance to PD-(L)1 Inhibition (clinicaltrials.gov)
    P2, N=194, Active, not recruiting, AstraZeneca | Trial completion date: Apr 2024 --> Jun 2025
    Trial completion date • Metastases
    |
    BRAF (B-raf proto-oncogene)
    |
    Imfinzi (durvalumab) • ceralasertib (AZD6738)
    5ms
    PLANETTE: A Study Investigating DNA-damage Response Agents in Molecularly Altered Advanced Cancer (clinicaltrials.gov)
    P2, N=54, Active, not recruiting, AstraZeneca | Trial completion date: Feb 2024 --> Feb 2025
    Trial completion date • Metastases
    |
    ATM (ATM serine/threonine kinase)
    |
    ceralasertib (AZD6738)
    5ms
    DDRiver Solid Tumours 301: Tuvusertib (M1774) in Participants With Metastatic or Locally Advanced Unresectable Solid Tumors (DDRiver Solid Tumors 301) (clinicaltrials.gov)
    P1, N=204, Active, not recruiting, EMD Serono Research & Development Institute, Inc. | Trial completion date: Jul 2024 --> Jan 2025 | Trial primary completion date: May 2024 --> Jan 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    ARID1A (AT-rich interaction domain 1A) • ATRX (ATRX Chromatin Remodeler)
    |
    Zejula (niraparib) • tuvusertib (M1774)
    5ms
    Chemo-phosphoproteomic profiling with ATR inhibitors berzosertib and gartisertib uncovers new biomarkers and DNA damage response regulators. (PubMed, Mol Cell Proteomics)
    We also show that SCAF1 deficiency partly rescues RAD51 loading in cells lacking the BRCA1 tumour suppressor. Taken together these data reveal potential new ATR biomarkers and new genome maintenance factors.
    Journal • BRCA Biomarker • PARP Biomarker
    |
    BRCA1 (Breast cancer 1, early onset) • RAD51 (RAD51 Homolog A)
    |
    Lynparza (olaparib) • berzosertib (M6620) • gartisertib (M4344)