berzosertib

an ATR kinase inhibitor

Also Known As:

2-PYRAZINAMINE, 3-(3-(4-((METHYLAMINO)METHYL)PHENYL)-5-ISOXAZOLYL)-5-(4-((1-METHYLETHYL)SULFONYL)PHENYL)-; 3-(3-(4-((METHYLAMINO)METHYL)PHENYL)-1,2-OXAZOL-5-YL)-5-(4-(PROPANE-2-SULFONYL)PHENYL)PYRAZIN-2-AMINE; VE-822; VX-970

Networked: 42 relevant articles (7 outcomes, 13 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Isoxazoles: 155
      - berzosertib: 42
  - Pyrazines: 150
    - berzosertib: 42

Experts

1.	Shapiro, Geoffrey I: 6 articles (04/2022 - 01/2020)
2.	Plummer, Ruth: 5 articles (04/2022 - 01/2018)
3.	Diaz-Padilla, Ivan: 4 articles (04/2022 - 01/2021)
4.	Dean, Emma: 3 articles (04/2022 - 01/2021)
5.	Falk, Martin: 3 articles (01/2021 - 01/2021)
6.	Hendriks, Bart S: 3 articles (01/2021 - 01/2021)
7.	Pollard, John: 3 articles (01/2021 - 01/2018)
8.	Dong, Jennifer: 2 articles (04/2022 - 01/2022)
9.	Ferrer-Playan, Jordi: 2 articles (04/2022 - 01/2022)
10.	Fleuranceau-Morel, Patricia: 2 articles (04/2022 - 01/2022)

Related Diseases

1.	Ovarian Neoplasms (Ovarian Cancer) 01/01/2020 - "We hypothesised that the combination of the selective ATR inhibitor, berzosertib, and gemcitabine could show acceptable toxicity and superior efficacy to gemcitabine alone in high-grade serous ovarian cancer. " 01/01/2020 - "Treatment of ovarian cancer cells with ATR specific siRNA or ATR inhibitor VE-822 led to significant apoptosis and inhibition of cellular proliferation, with reduced phosphorylation of Chk1 (p-Chk1), Cdc25c (p-Cdc25c), Cdc2 (p-Cdc2), and increased expression of cleaved PARP and γH2AX. " 01/01/2020 - "ATR-specific small interfering RNA (siRNA) and ATR inhibitor VE-822 were applied to determine the effects of ATR inhibition on ovarian cancer cell proliferation, apoptosis, and DNA damage. " 01/01/2021 - "In a trial of patients with high grade serous ovarian cancer (HGSOC), addition of the ATR inhibitor berzosertib to gemcitabine improved progression free survival (PFS) compared to gemcitabine alone but biomarkers predictive of treatment are lacking. " 01/01/2020 - "This study shows a benefit of adding berzosertib to gemcitabine in platinum-resistant high-grade serous ovarian cancer. "
2.	Neoplasms (Cancer) 01/01/2021 - "Population pharmacokinetics of ATR inhibitor berzosertib in phase I studies for different cancer types." 12/01/2021 - "Berzosertib distribution is heterogenous within the tumor, wherein concentrations are substantially lower in normal brain and invasive tumor rim (wherein the BBB is intact) when compared with those in the tumor core (wherein the BBB is leaky). " 11/01/2018 - "In conclusion, VX-970 is a tumor-specific radiosensitizer for TNBC. " 12/06/2012 - "VE-822 decreased maintenance of cell-cycle checkpoints, increased persistent DNA damage and decreased homologous recombination in irradiated cancer cells. " 12/06/2012 - "Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation."
3.	Esophageal Neoplasms (Esophageal Cancer) 11/01/2016 - "VX-970 is an effective chemo/radiosensitizer which could be readily integrated in the current treatment paradigm to improve the treatment response in esophageal cancer and we plan to test it prospectively in the forthcoming phase I dose escalation safety study combining the ATR inhibitor VX-970 with chemoradiotherapy in esophageal cancer (EudraCT number: 2015-003965-27)." 11/01/2016 - "Here, we tested the hypothesis that an ATR inhibitor, VX-970, used in combination with standard therapies for esophageal cancer could improve treatment outcome. " 07/01/2021 - "By analyzing the synthetic efficiency of NVP-BEZ235 (PI3K inhibitor) and VE-822 (an ATR inhibitor), we found that the combination of NVP-BEZ235 and VE-822 increased cytotoxicity in NRN1 methylated esophageal cancer cells, as well as KYSE150 cell xenografts. " 11/01/2016 - "Using esophageal cancer cell lines we evaluated the efficacy of combining VX-970 with cisplatin and carboplatin in vitro and with radiation in vitro and in vivo. "
4.	Glioblastoma (Glioblastoma Multiforme) 12/01/2021 - "SIGNIFICANCE STATEMENT: This study examined the brain delivery and efficacy of berzosertib in patient-derived xenograft models of glioblastoma multiforme (GBM). " 12/01/2021 - "Brain Distribution of Berzosertib: An Ataxia Telangiectasia and Rad3-Related Protein Inhibitor for the Treatment of Glioblastoma."
5.	Non-Small-Cell Lung Carcinoma (Carcinoma, Non-Small Cell Lung) 01/01/2022 - "A phase 1b study evaluating the safety and preliminary efficacy of berzosertib in combination with gemcitabine in patients with advanced non-small cell lung cancer." 01/01/2022 - "We assessed the safety, tolerability, preliminary efficacy, and pharmacokinetics (PK) of berzosertib plus gemcitabine in an expansion cohort of patients with advanced non-small cell lung cancer (NSCLC). "

Related Drugs and Biologics

1.	Gemcitabine
2.	Cisplatin (Platino)
3.	Biomarkers (Surrogate Marker)
4.	Carboplatin (JM8)
5.	Immunoconjugates (Immunoconjugate)
6.	sacituzumab govitecan
7.	Phosphotransferases (Kinase)
8.	Topotecan (Hycamtin)
9.	Irinotecan (Camptosar)
10.	Platinum

Related Therapies and Procedures

1.	Radiotherapy
2.	Drug Therapy (Chemotherapy)
3.	Chemoradiotherapy
4.	Neoadjuvant Therapy
5.	Intravenous Infusions