Table 1. FDA approved PARP inhibitors.
Drug | Date of FDA Approval | Population | Indication | Dosing | References | Specificity | Ki | Relative trapping capacity (28,29) |
---|---|---|---|---|---|---|---|---|
Olaparib | 2017 | gBRCAm advanced ovarian cancer | Received three or more prior lines of chemotherapy | 300 mg BID | (30) | PARP1, PARP2 | 5 nM, 1 nM | +++ |
2018 | Recurrent epithelial ovarian, fallopian tube, primary peritoneal cancer | Tumors must have CR/PR to platinum-based chemotherapy | 300 mg BID | (31) | ||||
2018 | gBRCAm HER2-negative metastatic breast cancer | Previous treatment with chemotherapy in the neoadjuvant, adjuvant, or metastatic setting | 300 mg BID | (32) | ||||
2019 | gBRCAm metastatic pancreatic adenocarcinoma | No disease progression after 16 weeks of a first-line platinum-based chemotherapy regimen | 300 mg BID | (30) | ||||
Rucaparib | 2018 | Recurrent epithelial ovarian, fallopian tube, primary peritoneal cancer | Tumors must have CR/PR to platinum-based chemotherapy | 600 mg BID | (33) | PARP1 | 4 nM | +++ |
Niraparib | 2017 | Recurrent epithelial ovarian, fallopian tube, primary peritoneal cancer | Tumors must have CR/PR to platinum-based chemotherapy | 300 mg QD | (34) | PARP1, PARP2 | 3.2 nM, 4 nM | ++++ |
2019 | Advanced ovarian, fallopian tube, primary peritoneal cancer with HRD-positive status | Previous treatment with three or more chemotherapy regimens | 300 mg QD | (35) | ||||
Talazoparib | 2018 | gBRCAm HER2-negative breast cancer, locally advanced or metastatic | Patient selection for therapy is based on FDA-approved companion diagnostic for talazoparib | 1 mg QD | (36) | PARP1, PARP2 | 1.2 nM, 0.9 nM | +++++ |
Data as of February 2020. PARP, poly (ADP-ribose) polymerase; gBRCAm, germline BRCA-mutated; CR, complete response; PR, partial response; BID, twice daily; QD, once daily; Ki, catalytic inhibitory constant; HRD, homologous recombination deficiency; HER2, human epidermal growth factor receptor 2.