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DRUG CLASS:

ATR inhibitor

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
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ATR (Ataxia telangiectasia and Rad3-related protein)
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Imfinzi (durvalumab) • 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
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ACSL4 (Acyl-CoA Synthetase Long Chain Family Member 4)
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ceralasertib (AZD6738)
15d
Enrollment closed • Checkpoint inhibition
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Imfinzi (durvalumab) • ceralasertib (AZD6738)
20d
STELLA: A Study of ART0380 for the Treatment of Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
P1/2, N=442, Recruiting, Artios Pharma Ltd | Trial completion date: Dec 2026 --> Dec 2027
Trial completion date
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ATM (ATM serine/threonine kinase) • HRD (Homologous Recombination Deficiency) • BRCA (Breast cancer early onset)
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HRD • BRCA mutation
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gemcitabine • irinotecan • alnodesertib (ART0380)
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
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CD4 (CD4 Molecule)
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HER-2 positive • HER-2 amplification • HER-2 expression
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Enhertu (fam-trastuzumab deruxtecan-nxki) • ceralasertib (AZD6738)
23d
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
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HRD (Homologous Recombination Deficiency) • ARID1A (AT-rich interaction domain 1A)
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ARID1A mutation
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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
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CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
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cisplatin • 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
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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)
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HER-2 negative • HRD • PALB2 mutation • RAD51C mutation • BRCA mutation
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Lynparza (olaparib) • carboplatin • Imfinzi (durvalumab) • ceralasertib (AZD6738) • saruparib (AZD5305)
2ms
TUVASTRAT: Tuvusertib in Astrocytoma With ATRX Mutation (clinicaltrials.gov)
P2, N=56, Recruiting, Grupo Español de Investigación en Neurooncología
New P2 trial
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TP53 (Tumor protein P53) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • ATRX (ATRX Chromatin Remodeler)
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TP53 mutation
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tuvusertib (M1774)
2ms
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
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency)
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BRCA1 mutation • HRD
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Zejula (niraparib) • tuvusertib (M1774) • lartesertib (M4076)
2ms
New P1/2 trial
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TP53 (Tumor protein P53) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • ATRX (ATRX Chromatin Remodeler)
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TP53 mutation
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tuvusertib (M1774)
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
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
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BRCA2 mutation • BRCA1 mutation
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Zejula (niraparib) • ceralasertib (AZD6738)