Table 1.
Ferroptosis inducing agents tested in vivo, their mechanism of action, and clinical status
| Ferroptosis agents | Mechanism | Cancer model | Used in clinic | Ref |
|---|---|---|---|---|
| Artesunate | Lipid peroxidation | Pancreatic cancer | Yes | (128) |
| Buthionine Sulfoximine (BSO) | γ-glutamylcysteine synthetase inhibitor | Clear cell renal cell carcinoma | Yes | (129) |
| Cyst(e)inase | Depletes extracellular cysteine/cystine | Pancreatic, prostate, breast carcinoma | No | (78, 111, 112) |
| Dihydroartemisinin | Degradation of ferritin, lipid ROS | Lung cancer | Yes | (130) |
| Imidazole Ketone Erastin (IKE) | System xC− inhibitor | Diffuse large B cell lymphoma (DLBCL) | No | (110) |
| JQ1 | Elevated iron, lipid ROS | Lung cancer | Yes | (131) |
| Piperazine Erastin (PE) | System xC− inhibitor | Fibrosarcoma | No | (25) |
| Sulfasalazine | System xC− inhibitor | Head and neck cancer | Yes | (126) |
| Sorafenib | System xC− inhibitor | Hepatocellular carcinoma | Yes | (132) |
| Withaferin A | Depletion and inactivation of GPX4 | Neuroblastoma | No | (133) |
| Ionizing Radiation (IR) | ROS, lipid ROS, increased ACSL4 | Lung cancer | Yes | (114, 115) |
| Immune checkpoint blockade: anti-PD-L1, anti-CTLA4 | IFNγ secretion, xCT suppression, lipid ROS | Melanoma, ovarian cancer | Yes | (86) |
Abbreviations: ACSL4, acyl-CoA synthetase long-chain family member 4; CTLA4, cytotoxic T-lymphocyte-associated protein 4; GPX4, glutathione peroxidase 4; GSH, glutathione; IFNγ, interferon gamma, PD-L1, programmed death-ligand 1; ROS, reactive oxygen species.