Table 2.
Structure and indications of mature anticancer PARP1-based drugs entered clinical trials.
| Drug | Structure | Active Structural Group | Biophysical Parameters (PARP1) | Well Studied Cancer Types | Typical Clinical Trials No. (The Latest Stage) | Phase | REF |
|---|---|---|---|---|---|---|---|
| Olaparib (AZD2281) |  |
Amide motif enclosed in cyclic ring | IC50 = 5 nM | Ovarian carcinoma | NCT02476968 (Phase 4) | 1–4 | [1,73] |
| Breast carcinoma | NCT02032823 (Phase 3) | 1–3 | |||||
| Prostate carcinoma | NCT02987543 (Phase 3) | 1–3 | |||||
| Pancreatic carcinoma | NCT02184195 (Phase 3) | 1–3 | |||||
| Ewing’s sarcoma | NCT01583543 (Phase 2) | 1–2 | |||||
| Gastric carcinoma | NCT01924533 (Phase 3) | 1–3 | |||||
| Lung carcinoma | NCT03009682 (Phase 2) | 1–2 | |||||
| Germ Cell Tumor | NCT02533765 (Phase 2) | 1–2 | |||||
| Colorectal carcinoma | NCT00912743 (Phase 2) | 1–2 | |||||
| Unknown solid tumors | NCT03233204 (Phase 2) | 1–2 | |||||
| Niraparib (MK-4827) |  |
Conventional embedded primary amide | IC50 = 3.2 nM | Ovarian carcinoma | NCT01847274 (Phase 3) | 1–3 | [76,93] |
| Breast carcinoma | NCT01905592 (Phase 3) | 1–3 | |||||
| Endometrial carcinoma | NCT03016338 (Phase 2) | 1–2 | |||||
| Uveal melanoma | NCT03207347 (Phase 2) | 1–2 | |||||
| Fallopian tube carcinoma | NCT02657889 (Phase 2) | 1–2 | |||||
| Peritoneal carcinoma | NCT02657889 (Phase 2) | 1–2 | |||||
| Rucaparib (AG-014669, PF-01367338) |  |
Amide motif enclosed in cyclic ring | IC50 = 1.4 nM | Ovarian carcinoma | NCT02855944 (Phase 3) | 1–3 | [78,80,96] |
| Fallopian tube carcinoma | NCT02855944 (Phase 3) | 1–3 | |||||
| Peritoneal carcinoma | NCT01968213 (Phase 3) | 1–3 | |||||
| Prostate carcinoma | NCT02975934 (Phase 3) | 1–3 | |||||
| Pancreatic carcinoma | NCT02042378 (Phase 2) | 1–2 | |||||
| Breast carcinoma | NCT02505048 (Phase 2) | 1–2 | |||||
| Veliparib (ABT-888) |  |
Conventional embedded primary amide | Ki = 5.2 nM | Breast carcinoma | NCT02032277 (Phase 3) | 1–3 | [82,97,98] |
| Ovarian carcinoma | NCT02470585 (Phase 3) | 1–3 | |||||
| Non-small cell lung carcinoma | NCT02106546 (Phase 3) | 1–3 | |||||
| Solid tumors | NCT01193140 (Phase 2) | 1–2 | |||||
| Testicular carcinoma | NCT02860819 (Phase 2) | 1–2 | |||||
| Talazoparib (BMN-673) |  |
Amide motif enclosed in cyclic ring | IC50 = 1.2 nM | Breast carcinoma | NCT01945775 (Phase 3) | 1–3 | [85,86,99,100] |
| Prostate carcinoma | NCT03148795 (Phase 2) | 1–2 | |||||
| Ovarian carcinoma | NCT02326844 (Phase 2) | 1–2 | |||||
| Endometrial carcinoma | NCT02127151 (Phase 2) | 1–2 | |||||
| Acute Myeloid Leukemia | NCT02878785 (Phase 2) | 1–2 |