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Target Overview
Poly [ADP-ribose] polymerases (PARPs) are a group of proteins known to be involved in the repair of single-strand breaks in DNA.1
A healthy cell’s DNA undergoes damage every day, with approximately 10,000 spontaneous single-strand breaks that require repair.1
Inhibition of PARP1 with AZD9574 leads to the trapping of PARP1 bound to DNA single-strand breaks, stalling of replication forks, their collapse and the generation of DNA double-strand breaks and cancer cell death. In tumor cells that already have compromised DNA repair mechanisms (such as loss of BRCA1 or BRCA2 function, affecting double-strand break repair), inhibition of PARP1 leads to excessive accumulation of DNA damage and may cause death of the cell.1,2
Compound Overview
AZD9574 is an investigational, next generation brain penetrant PARP inhibitor. It is designed to selectively inhibit and trap PARP1 as well as specifically penetrate the blood-brain barrier.3,4 AZD9574 is being clinically evaluated in recurrent CNS tumors and tumors with homologous recombination deficiency that may develop, or have developed, CNS metastases.5
Mechanism of Action
References
1. Underhill C, Toulmonde M, Bonnefoi H. Ann Oncol. 2011;22(2):268-279. 2. Yelamos J, Farres J, Llacuna L, et al. Am J Cancer Res. 2011;1(3):328-346. 3. Ghosh A, Hande SM, Balazs A, et al. AACR 2022, Virtual, 5-13 April 2022. 4. Pike A, Balazs A, Cselenyi Z, et al. AACR 2022, e-poster April 2022, New Orleans, USA. 5. Study NCT05417594. ClinicalTrials.gov website.
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Abbreviations
BRCA 1/2
breast cancer susceptibility gene 1/2
CNS
central nervous system
DNA
deoxyribonucleic acid
PARP
poly (ADP-ribose) polymerase
PARP1
poly (ADP-ribose) polymerase 1
Target Overview
Poly [ADP-ribose] polymerases (PARPs) are a group of proteins known to be involved in the repair of single-strand breaks in DNA.1
A healthy cell’s DNA undergoes damage every day, with approximately 10,000 spontaneous single-strand breaks that require repair.1
Inhibition of PARP1 with AZD9574 leads to the trapping of PARP1 bound to DNA single-strand breaks, stalling of replication forks, their collapse and the generation of DNA double-strand breaks and cancer cell death. In tumor cells that already have compromised DNA repair mechanisms (such as loss of BRCA1 or BRCA2 function, affecting double-strand break repair), inhibition of PARP1 leads to excessive accumulation of DNA damage and may cause death of the cell.1,2
Compound Overview
AZD9574 is an investigational, next generation brain penetrant PARP inhibitor. It is designed to selectively inhibit and trap PARP1 as well as specifically penetrate the blood-brain barrier.3,4 AZD9574 is being clinically evaluated in recurrent CNS tumors and tumors with homologous recombination deficiency that may develop, or have developed, CNS metastases.5
Mechanism of Action
References
1. Underhill C, Toulmonde M, Bonnefoi H. Ann Oncol. 2011;22(2):268-279. 2. Yelamos J, Farres J, Llacuna L, et al. Am J Cancer Res. 2011;1(3):328-346. 3. Ghosh A, Hande SM, Balazs A, et al. AACR 2022, Virtual, 5-13 April 2022. 4. Pike A, Balazs A, Cselenyi Z, et al. AACR 2022, e-poster April 2022, New Orleans, USA. 5. Study NCT05417594. ClinicalTrials.gov website.
Clinical trial information
Select trial for more information
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Abbreviations
BRCA 1/2
breast cancer susceptibility gene 1/2
CNS
central nervous system
DNA
deoxyribonucleic acid
PARP
poly (ADP-ribose) polymerase
PARP1
poly (ADP-ribose) polymerase 1