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PARP inhibitors are a group of pharmacological inhibitors of the enzyme poly ADP ribose polymerase (PARP). They are developed for multiple indications, including the treatment of heritable cancers. [1] Several forms of cancer are more dependent on PARP than regular cells, making PARP (PARP1, PARP2 etc.) an attractive target for cancer therapy.
Rucaparib, sold under the brand name Rubraca, is a PARP inhibitor used as an anti-cancer agent. [2] Rucaparib is a first-in-class pharmaceutical drug targeting the DNA repair enzyme poly-ADP ribose polymerase-1 (PARP-1).
Talazoparib, sold under the brand name Talzenna, is an anti-cancer medication used for the treatment of breast cancer and prostate cancer. [6] It is an orally available poly ADP ribose polymerase PARP inhibitor marketed by Pfizer for the treatment of advanced breast cancer with germline BRCA mutations. [9]
Staging breast cancer is the initial step to help physicians determine the most appropriate course of treatment. As of 2016, guidelines incorporated biologic factors, such as tumor grade, cellular proliferation rate, estrogen and progesterone receptor expression, human epidermal growth factor 2 (HER2) expression, and gene expression profiling into the staging system.
Pamiparib is a member of the PARP inhibitor drug class. [ 1 ] In China, it is approved for the treatment of germline BRCA mutation -associated recurrent advanced ovarian , fallopian tube , and primary peritoneal cancers previously treated with two or more lines of chemotherapy.
Iniparib (INN, [1] previously known as BSI 201) was a drug candidate for cancer treatment.It was originally believed to act as an irreversible inhibitor of PARP1 (hence, a PARP inhibitor) and possibly other enzymes through covalent modification, [2] [3] but its effects against PARP were later disproven.
Olaparib acts as an inhibitor of the enzyme poly ADP ribose polymerase (PARP), and is termed a PARP inhibitor. BRCA1/2 mutations may be genetically predisposed to development of some forms of cancer, and may be resistant to other forms of cancer treatment. However, these cancers sometimes have a unique vulnerability, as the cancer cells have ...
A substantial body of preclinical and clinical data has accumulated with PARP inhibitors in various forms of cancer. In this context, the role of PARP in single-strand DNA break repair is relevant, leading to replication-associated lesions that cannot be repaired if homologous recombination repair (HRR) is defective, and leading to the ...
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