Table 1. PARP inhibitors in Phase III clinical trial development for ovarian cancer, 2015.
| Agent | Company | IC 50 | Ongoing clinical trials | Patient population | Indication |
|---|---|---|---|---|---|
| Olaparib (AZD2281) | AstraZeneca | 5 nM (PARP1) 1 nM (PARP2) (Menear et al, 2008) | SOLO1 (NCT01844986) | BRCA-mutated, advanced (FIGO Stage III–IV), high-grade serous/endometrioid; response (CR or PR) to initial platinum-based chemotherapy | First line |
| SOLO2 (NCT01874353) | BRCA-mutated, high-grade serous/endometrioid; response (CR or PR) following ⩾2 lines of platinum-based chemotherapy | Relapsed | |||
| SOLO3 (NCT02282020) | Germline BRCA-mutated, platinum-sensitive relapsed, high-grade serous/endometrioid | Relapsed | |||
| SOLOiST (NCT02392676) | Platinum-sensitive relapsed, high-grade epithelial; deficient DNA damage repair (must not be caused by a germline BRCA mutation) | Relapsed | |||
| Niraparib (MK4827) | Merck (licensed to Tesaro) | 3.8 nM (PARP1) 2.1 nM (PARP2) (Jones et al, 2009) | NOVA (NCT01847274) | BRCA-mutated or high-grade serous; sensitive to penultimate platinum-based regimen; response (CR or PR) to current platinum-based chemotherapy | Relapsed |
| Rucaparib (AG014699) | Clovis Oncology | 1.4 nM (Ki; PARP1) 0.5 nM (Ki; PARP2) (Thomas et al, 2007) | ARIEL3 (NCT01968213) | High-grade serous/endometrioid; sensitive to penultimate platinum-based regimen; response (CR or PR) to current platinum-based chemotherapy | Relapsed |
| Talazoparib (BMN-673) | Medivation | 0.58 nM (PARP1) (Shen et al, 2013) | None | — | — |
| Veliparib (ABT-888) | AbbVie and BMS | 5.2 nM (PARP1) 2.9 nM (PARP2) (Donawho et al, 2007) | NCT02470585 | Advanced (FIGO Stage III or IV), high-grade serous | First line |
Abbreviations: CR=complete response; FIGO=Féderation Internationale de Gynécologie et d'Obstétrique; IC50=the concentration of a drug required for 50% inhibition; PR=partial response.