Table 1 PARP inhibitors under development
PARP inhibitor | Route | PARP catalyitic inhibition (IC50)(Murai et al, 2012, 2014) | In vitro Cytotoxicity ( Murai et al, 2012, 2014) | In vitro PARP trapping ( Murai et al, 2012, 2014) | Treatment | Cancer types |
|---|---|---|---|---|---|---|
Olaparib (AZD-2281) (AstraZeneca) | Oral | 1.2 nmol l−1 | ++ | ++ | •Monotherapy | •BRCA1/2MUT+ associated |
|  |  |  |  |  | •Combination with cytotoxic chemotherapy | •BrCa/OvCa •BRCA-like tumours |
|  |  |  |  |  | •Combination with targeted agents | •Advanced hematologic malignancies and solid tumours |
|  |  |  |  |  | •Combination with RTs | •Maintenance study following remission in platinum sensitive OvCa |
Veliparib (ABT-888) (Abbvie) | Oral | 10.5 nmol l−1 | + | + | •Monotherapy | •BRCA1/2MUT+ associated BrCa/OvCa |
|  |  |  |  |  | •Combinations with cytotoxic chemotherapy | •BRCA-like tumours, •Advanced hematologic malignancies and solid tumours |
|  |  |  |  |  | •Combinations with targeted agents |  |
|  |  |  |  |  | •Combinations with RT |  |
Talazoparib (BMN 673) (Pfizer) | Oral | 4 nmol l−1 | ++++ | ++++ | •Monotherapy | •Advanced hematologic malignancies and solid tumours |
Rucaparib (Clovis) | Oral | 21 nmol l−1 | ++ | ++ | •Monotherapy | •Advanced solid tumours |
|  |  |  |  |  | •Combinations (carboplatin) | •Recurrent OvCa, •BRCA1/2MUT+ associated BrCa/OvCa |
Niraparib (MK-4827) (TesaroBio) | Oral | 50.5 nmol l−1 | +++ | +++ | •Monotherapy | •Advanced hematologic malignancies and solid tumours |
|  |  |  |  |  | •Combinations (temozolomide) | •BRCA1/2MUT+ associated and HER2 negative BrCa, •Maintenance study following remission in platinum sensitive •OvCa |
