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2d
ASCERTAIN: A Study to Investigate the Biological Effects of Saruparib (AZD5305), Darolutamide, and in Combination in Men With Newly Diagnosed Prostate Cancer. (clinicaltrials.gov)
P1, N=120, Recruiting, AstraZeneca | Trial completion date: Feb 2026 --> Aug 2026 | Trial primary completion date: Feb 2026 --> Aug 2026
Trial completion date • Trial primary completion date
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Nubeqa (darolutamide) • saruparib (AZD5305)
2d
CJNJ-67652000 and Prednisone for Treatment of Metastatic Castration-Resistant Prostate Cancer and SPOP Gene Mutations (clinicaltrials.gov)
P2, N=30, Recruiting, Mayo Clinic | Trial completion date: Sep 2025 --> Mar 2027 | Trial primary completion date: Sep 2025 --> Mar 2027
Trial completion date • Trial primary completion date
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SPOP (Speckle Type BTB/POZ Protein)
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Akeega (abiraterone/niraparib)
10d
Enrollment closed
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Xtandi (enzalutamide) • abiraterone acetate • Nubeqa (darolutamide) • apalutamide • saruparib (AZD5305)
22d
Combination therapy overcomes secondary PARPi resistance in ATM-deficient prostate cancer. (PubMed, NPJ Precis Oncol)
To address this, we generated in vitro prostate cancer models of acquired PARPi resistance to olaparib and saruparib, a novel selective PARP1 inhibitor and pursued functional characterization and drug sensitivity studies. Consistently, we demonstrate in vivo that the combination of PARPi-ATRi in resistant models restores treatment sensitivity through enhancing replication stress. Collectively, these findings highlight an interplay between ATM-ATR signaling as a key mediator of PARPi sensitivity in ATM-deficient mPC and identify a promising therapeutic combination to prolong treatment response and potentially improve patients' outcomes.
Journal
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ATM (ATM serine/threonine kinase) • HRD (Homologous Recombination Deficiency) • CHEK1 (Checkpoint kinase 1)
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Lynparza (olaparib) • saruparib (AZD5305)
24d
CERTIS1: Study of AZD9574 as Monotherapy and in Combination With Anti-cancer Agents in Participants With Advanced Solid Malignancies (clinicaltrials.gov)
P1/2, N=695, Recruiting, AstraZeneca | Trial completion date: Apr 2027 --> Aug 2027 | Trial primary completion date: Apr 2027 --> Aug 2027
Trial completion date • Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • HRD (Homologous Recombination Deficiency) • RAD51C (RAD51 paralog C) • RAD51D (RAD51 paralog D)
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HER-2 negative • PALB2 mutation • RAD51C mutation • RAD51D mutation
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temozolomide • Enhertu (fam-trastuzumab deruxtecan-nxki) • Datroway (datopotamab deruxtecan-dlnk) • AZD9574
24d
A novel 18 F-labeled brain penetrant PET ligand for imaging poly(ADP-ribose) polymerase-1. (PubMed, bioRxiv)
In 22Rv1 xenograft mouse models, the tracer demonstrated significant tumor accumulation that was specific to PARP-1, and ex vivo biodistribution confirmed organ uptake consistent with specific tumor binding and PARP-1 expression. Together, these findings establish [ 18 F]AZD9574 as a promising PARP-1-targeted imaging agent with strong potential for advancing cancer research and therapeutic monitoring.
Journal • PARP Biomarker
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HRD (Homologous Recombination Deficiency) • PARP1 (Poly(ADP-Ribose) Polymerase 1)
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AZD9574
28d
Enrollment closed
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saruparib (AZD5305)
2ms
Discovery of selective PARP1/EZH2 inhibitor inducing PANoptosis in triple-negative breast cancer. (PubMed, Eur J Med Chem)
In this study, we combined the structure of the latest second-generation selective PARP1 inhibitor AZD5305 to design and synthesize a series of second-generation selective PARP1/EZH2 dual inhibitors...Meanwhile, compared with the previous first-generation inhibitors, its permeability has improved, but its overall pharmacokinetic characteristics still need to be further optimized. However, as a novel selective PARP multifunctional molecule, it remains a highly promising potential compound for the for the treatment of TNBC.
Journal
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PARP2 (Poly(ADP-Ribose) Polymerase 2)
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saruparib (AZD5305)
3ms
CERTIS1: Study of AZD9574 as Monotherapy and in Combination With Anti-cancer Agents in Participants With Advanced Solid Malignancies (clinicaltrials.gov)
P1/2, N=695, Recruiting, AstraZeneca | Trial completion date: Feb 2027 --> Jun 2027 | Trial primary completion date: Feb 2027 --> Jun 2027
Trial completion date • Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • HRD (Homologous Recombination Deficiency) • RAD51C (RAD51 paralog C) • RAD51D (RAD51 paralog D)
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HER-2 negative • PALB2 mutation • RAD51C mutation • RAD51D mutation
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temozolomide • Enhertu (fam-trastuzumab deruxtecan-nxki) • Datroway (datopotamab deruxtecan-dlnk) • AZD9574