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It is a PARP1 and PARP2 inhibitor. [31] [32] Started Phase II: Olaparib (developed by AstraZeneca) for breast, ovarian and colorectal cancer. [33] [34] Olaparib TOPARP-A trial for use in advanced prostate cancer (published c. April 21, 2015). [35] Rucaparib for metastatic breast and ovarian cancer. Veliparib for metastatic melanoma.
PARP1 inhibitors are being tested for effectiveness in cancer therapy. [33] It is hypothesized that PARP1 inhibitors may prove highly effective therapies for cancers with BRCAness, due to the high sensitivity of the tumors to the inhibitor and the lack of deleterious effects on the remaining healthy cells with functioning BRCA HR pathway.
It first-in-class selective inhibitor of poly-ADP ribose polymerase 1 (PARP1), designed to treat cancers with homologous recombination repair (HRR) deficiencies as a result of mutations in BRCA1, BRCA2, PALB2, RAD51C, or RAD51D genes. [2]
Olaparib, sold under the brand name Lynparza, is a medication for the maintenance treatment of BRCA-mutated advanced ovarian cancer in adults.It is a PARP inhibitor, inhibiting poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.
The PARP family comprises 17 members (10 putative). [2] They vary greatly in structure and function within the cell. PARP1, PARP2, VPARP (), Tankyrase-1 and -2 (PARP-5a or TNKS, and PARP-5b or TNKS2) have a confirmed PARP activity.
Niraparib is an inhibitor of the enzymes PARP1 and PARP2. [10] Pharmacokinetics. The inactive main metabolite M1 is the carboxylic acid derivative of niraparib.
Veliparib (ABT-888) [1] is a potential anti-cancer drug acting as a PARP inhibitor.It kills cancer cells by blocking a protein called PARP, thereby preventing the repair of DNA or genetic damage in cancer cells and possibly making them more susceptible to anticancer treatments.
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.