TABLE 1.
Clinically approved Pt(II) drugs [adapted from Wheate et al. (2010); Ali et al. (2013); Han et al. (2015); Johnstone et al. (2016); Imran et al. (2018); Ghosh (2019)] and Pt(IV) prodrugs that have entered clinical trials [adapted from Tutsch et al. (1999); Wheate et al. (2010); Imran et al. (2018)].
| Name | Year of approval/phase status | Country/region of approval | Mode of administration | LD50 (mg/kg) | Indication | Side effect/limitation | |
|---|---|---|---|---|---|---|---|
| Pt(II) drugs | Cisplatin (also CDDP or Platinol) | 1978 | Global | Intraperitoneal | 12 | Testicular, ovarian, bladder, head and neck, and lung cancers | Nephrotoxicity, neurotoxicity, ototoxicity, and acute emesis |
| Carboplatin (also JM8 or paraplatin) | 1989 | Global | Intraperitoneal | 120 | Ovarian and lung cancer | Myelosuppression, platelet disorders, drug resistance, and peripheral neurotoxicity | |
| Nedplatin (also 254-S or Aquila | 1995 | Japan | Intravenous | 44.1 | Lung, head and neck, and esophageal cancers | Bone marrow suppression and mild nausea | |
| Heptaplatin (also, SKI 2053R or SunPla) | 1999 | Korea | Intraperitoneal | 196.2 | Advanced gastric cancer | Hepatotoxicity and myelosuppression | |
| Oxaliplatin (also 1-OHP or Eloxatin) | 2002 | Global | Intraperitoneal | 19.8 | Colorectal cancer | Neurotoxicity and alimentary canal toxicity | |
| Lobaplatin (also D-19466) | 2010 | China | Intraperitoneal | 25.7 | Testicular, ovarian, and lung cancers | Anemia and leukopenia | |
| Pt(IV) prodrugs | Ormaplatin (or tetraplatin) | Phase I | — | Intraperitoneal and intravenous | 23 | Breast, ovarian, and myeloma cancers | Too rapid reduction in plasma and severe neurotoxicity |
| Iproplatin (or JM9) | Phase III | — | Intraperitoneal | 54 | Ovary, breast, gastric, pancreatic, and metastatic epidermoid cancer of head and neck | Low cytotoxicity | |
| Satraplatin (or JM216) | Phase III | — | Oral | 30 | Ovarian cancer, non-small-cell lung cancer, and small-cell lung cancer | No overall survival benefit | |
| LA-12 | Phase I continued | — | Oral | N.A a | Ovary cancer cell lines | N.A. |
not available.