ABT-888

ABT-888 (Veliparib) is a potent inhibitor of PARP-1 and PARP-2 with Ki values of 5.2nM and 2.9nM respectively. ABT-888 (Veliparib) inhibits PARPs, thereby inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents. ABT-888 (Veliparib) has good oral bioavailability, can cross the blood-brain barrier, and potentiates temozolomide, platinums, cyclophosphamide, and radiation in syngeneic and xenograft tumor models. This broad spectrum of chemopotentiation and radiopotentiation makes this compound an attractive candidate for clinical evaluation. Phase I study of PARP inhibitor ABT-888 in combination with topotecan in adults reveal that PARP inhibition can modulate the capacity to repair topoisomerase I-mediated DNA damage in the clinic.