Table 4 Preclinical drugs associated with ferroptosis.
From: Regulatory pathways and drugs associated with ferroptosis in tumors
Preclinical drugs | Mechanisms of action | Clinical/preclinical findings | Reference |
|---|---|---|---|
Erastin | Inhibit System Xc-, GSH depletion | Gastric cancer treatment | [112] |
Sulfasalazine | Inhibit System Xc-, GSH depletion | Ovarian cancer and breast cancer treatment | |
RSL3 | GPX4 inactivation | Ovarian cancer | [150] |
ML162 | Inhibit GPX4, induces lipid peroxidation | Induced head and neck cancer cell death | [161] |
ML210 | Covalently modified selenocysteine of GPX4 | Mesenchymal-high cancers | [163] |
FIN56 | Deplete CoQ10, decreases GPX4 level | Breast carcinoma cells | [166] |
Buthionine sulfoximine (BSO) | Decreases GSH and GPX4 level | Pancreatic cancer | [170] |
Dihydroartemisinin | Induces ROS, decreases GSH and GPX4 level | Glioma cells | [174] |
Artemisinin | Induces iron-dependent death | Head and neck carcinoma cells | [175] |
Artesunate | Induces lipid peroxidation | Hepatocellular carcinoma | [176] |
Sorafenib | Inhibit System Xc-, GSH depletion | Hepatocellular carcinoma and lung adenocarcinoma | |
FINO2 | Induces lipid peroxidation | Renal cancer cells | [186] |
Statins | Deplete CoQ10, decreases GPX4 level | Triple-negative breast cancer | [179] |
BAY-87–2243 | increased cellular ROS levels, stimulated lipid peroxidation, and reduced glutathione levels | Melanoma cells | [185] |
lapatinib | Disrupt iron transport or inactivates GPX4 | Breast cancer and NSCLC cells | |
Withaferin A | Targets KEAP1 or inactivates GPX4 | Neuroblastoma and myeloma cells treatment |
