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) |