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Table 3 PARP inhibitors in development

From: Novel targeted therapeutics: inhibitors of MDM2, ALK and PARP

Chemical series Therapeutics Development stage
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 AG-014699
(PF-01367338)
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)
  1. Reference; [94, 96, 97, 100, 101, 103, 106, 108, 115117, 119, 122125, 151156]