Table 3 PARP inhibitors in development

Benzamide

BSI-201 (iniparib)

Phase III

Gemcitabine and carboplatin ± BSI-201 in breast and lung cancers; phase I/II: single agent or combination with chemotherapy in various cancer types including glioma and ovarian cancer

Phthalazinone

AZD2281 (olaparib)

Phase I/II

Single agent or combination with chemotherapy in various cancer types including breast, ovarian and colorectal cancers

Tricyclic indole

Phase II

Single agent in BRCA-associated breast or ovarian cancer; Phase I: combination with chemotherapy in advanced solid tumors

Benzimidazole

ABT-888

(Veliparib)

Phase II

Combination with chemotherapy in various cancer types including breast cancer, colorectal cancer, glioblastoma multiforme and melanoma; phase I: combination with radiation

Indazole

MK-4827

Phase I

Single agent; combination with carboplatin-containing regimens

Pyrrolocarbazole

CEP-9722

Phase I

Combination with temozolomide in advanced solid tumors

Phthalazinone

E7016

(GPI-21016)

Phase I

Combination with temozolomide in advanced solid tumors

Isoindolinone

INO-1001

Phase I

Combination with temozolomide in melanoma (completed) without further investigation in oncology; phase II in cardiovascular disease

Structure undisclosed

MP-124

Phase I in acute ischemic stroke

Structure undisclosed

LT-00673

Preclinical

Structure undisclosed

NMS-P118

Preclinical

Structure undisclosed

XAV939

Preclinical, highly selective against PARP-5 (tankyrase)