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. Author manuscript; available in PMC: 2022 Jul 19.
Published in final edited form as: Blood Rev. 2020 May 7;45:100696. doi: 10.1016/j.blre.2020.100696

Table 1.

Characterization of PARP inhibitors with preclinical data in hematological malignancies

Name of Inhibitor Structure IC50 In vitro effects In vivo effects Stage of Development
Talazoparib (BMN673) graphic file with name nihms-1801347-t0002.jpg 0.6nM Combination with DNMTis synergistic toxicity and reduced colony formation. Combination with DNMTis resulted in increase in overall survival and significant anti-tumor response. Recruiting/Phase 1
Olaparib (Ku-0059436) graphic file with name nihms-1801347-t0003.jpg 5nM Anti-proliferative and apoptotic events in AML cell lines, accumulation of S phase cell cycle arrest. Synergistic anti-leukemic effects in combination with HDACi, WEE1 inhibition, GO. Increase in overall survival in combination with AZD1775 Phase 1
Phase 2
PJ34 HCl graphic file with name nihms-1801347-t0004.jpg N/A Dose-dependent decrease in cell viability, induces apoptosis in AML cell lines. Alleviated hepatomegaly and splenomegaly and reduced level of C1498 cells. N/A
Veliparib (ABT 888) graphic file with name nihms-1801347-t0005.jpg 5nM Anti-leukemic activity in combination with DNMTis. Synergistic anti-proliferative effects in combination with TRAIL. Enhances activity of TMZ. Veliparib combined with Cisplatin achieved significant tumor growth inhibition. Phase I Active not yet recruiting
Niraparib (MK-4827) graphic file with name nihms-1801347-t0006.jpg 4nM N/A N/A N/A
Rucaparib (AG-0146991,PF-01367338) graphic file with name nihms-1801347-t0007.jpg 1nM Increased sensitivity in AML cell lines at 0.1–100M. Significant improvement in overall survival in combination with fluororacil. N/A