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. 2020 Sep 25;10:571127. doi: 10.3389/fonc.2020.571127

Table 2.

The synergistic effect of anti-tumor therapy together with ferroptosis inducers.

Treatment Drugs Drugs Target Cancer type Mechanism References
Chemotherapy Cisplatin RSL3 GPX4 Lung cancer Inhibition of GPX4 via RSL3 could enhance the anticancer effect of cisplatin (17)
Erastin GSH-GPXs NSCLC Cisplatin can deplete the GSH and inactivate the GPXs together with erastin (18)
Colorectal cancer
Erastin System Xc- PDAC Both SLC7A11-KO cell lines exhibit amino acid stress with induction of ATF4 and cell death (30)
Erastin System Xc- Ovarian cancer Erastin can inhibit system Xc- and potentiate the cytotoxic effects of cisplatin to eradicate tumor cells (31)
Erastin/SAHA ROS NSCLC SAHA and erastin, the inducers of ROS-mediated cell death, strongly enhanced the effect of cisplatin in WT EGFR cells (32)
Gemcitabine Erastin System Xc- PDAC Both SLC7A11-KO cell lines exhibit amino acid stress with induction of ATF4 and cell death (30)
Paclitaxel RSL3 System Xc- HPSCC The combination therapy upregulates mtp53 expression, which mediated transcriptional regulation of SLC7A11 (33)
TMZ Erastin System Xc- Glioma Erastin sensitizes glioblastoma cells to TMZ by restraining SLC7A11 and CTH function (26)
ALZ003 GPX4 Glioblastoma AR suppressor ALZ003 can inhibit TMZ-resistant glioblastoma through inhibiting GPX4 (34)
Artesunate Trigonelline NRF2 Head and neck cancer NRF2 inhibitor trigonelline can induce lipid peroxide accumulation (16)
Cytarabine/ara-C and Doxorubicin /adriamycin Erastin Acute myeloid leukemia JNK and p38 cooperatively participate in cell death induced by erastin in HL-60 cells (35)
SSZ CN-A and PL Pancreatic cancer PL markedly depletes GSH and may inhibit GPX activity (36)
PL Pancreatic cancer PL markedly depletes GSH and may inhibit GPX activity (36)
Target therapy Lapatinib Siramesine Fe Breast cancer The combination therapy induces ferroptosis by elevating the intracellular iron level (37)
Lapatinib Siramesine Fe Breast cancer The combination therapy induces ferroptosis by elevating the intracellular iron level (37)
Lapatinib Siramesine Fe, Lipid peroxidation Glioma The combination therapy induces ferroptosis by elevating the intracellular iron level (38)
Lung adenocarcinoma
Sorafenib X1 Lipid peroxidation HCC The combination therapy increases oxidative stress and mitochondrial dysfunction through activation of JNKs (39)
Sorafenib Trigonelline NRF2 HCC NRF2 inhibitor trigonelline can induce lipid peroxide accumulation (27)
Radiotherapy X-ray irradiation Erastin GPX4 Cervical adenocarcinom Erastin induces ferroptosis and decreases the expression levels of GSH and GPX4 protein (40)
Lung adenocarcinoma
SSZ System Xc- Melanoma SSZ decreases the intratumoral level of GSH, leading to enhanced susceptibility to radiation therapy (41)
Laser irradiation Gallic acid GPX4, Lipid peroxidation Breast cancer Using pre-red laser irradiation could improve anticancer effects of gallic acid through decreasing GPX4 activity (42)
Melanoma
Microbeam irradiation IKE/RSL3/sorafinib System Xc-, GPX4 Sarcoma System xc- or GPX4 inhibitors synergize with cytoplasmic irradiation to induce ferroptosis by enhancing cytoplasmic lipid peroxidation (43)
Glioblastoma
Lung cancer
Gamma knife radiosurgery SSZ System Xc- Glioblastomas SSZ treatment significantly reduced cystine uptake and GSH levels, and significantly increased the levels of ROS (44)
γ-radiation Erastin System Xc- Breast cancer System Xc- enhanced GSH synthesis. GSH is used to control ROS, which are therapeutic effectors of radiation therapy (45)
Ionizing radiation Anti-PD-L1/Anti-CTLA4 mAb System Xc- Sarcoma ATM activated by radiotherapy and IFN derived from activated CD8+ T cells synergistically inhibited the expression of SLC7A11 (46)
Melanoma
Ovarian cancer
Other therapy Statins Erlotinib/Gefitinib GPX4 Lung cancer Statins block the synthesis of GPX4 (47)
Acetaminophen Erastin Iron, Lipid peroxidation NSCLC Acetaminophen enhances the sensitivity of erastin-induced ferroptosis by regulating the NRF2/HO-1 signaling pathway (48)
Bromelain Erastin ACSL4 Colorectal cancer Bromelain induces ROS-induced ferroptosis via the modulation of ACSL4 (49)
Metadherin ML162 /ML210 SLC3A2, GPX4 Endometrial cancer MTDH can inhibit the activities of GPX4 and SLC3A2 (50)
Erastin ACSL4 Breast cancer Bromelain induces ROS-induced ferroptosis in Kras mutant Colorectal cancer cells via ACSL4
SCD1 inhibitors RSL3/Erastin
PEITC
Lipid peroxidation
ROS
Ovarian Cancer Stearoyl-CoA desaturase 1 inhibitors decrease an endogenous membrane antioxidant CoQ10
CN-A and PEITC synergistically trigger ROS accumulation
(51)
CN-A Pancreatic cancer (52)
PL ROS, GSH, GPX Pancreatic cancer PL markedly depletes GSH and may inhibit GPX activity (36)
SSZ and PL ROS Pancreatic cancer PL markedly depletes GSH and may inhibit GPX activity (36)
Immunotherapy Dichloroacetate Albiziabioside A GPX4 Breast cancer AlbA-DCA can inhibit GPX4 and eliminate M2-TAMs to suppress tumor progression (53)
SSZ and PL Melonoma PL markedly depleted GSH and may inhibit GPX activity
Pa Ti Melanoma Pa and Ti cooperately polarize M2-TAMs into M1-TAMs and promote the Fenton reaction with Fe ions discharged from magnetic nanoclusters (54)
Breast cancer
Oxygen-boosted PDT Ferroptosis inducers Breast cancer PDT induces lymphocytes infiltration in the tumor site and stimulates the secretion of IFN-γ (55)

PDAC, Pancreatic ductal adenocarcinoma; HCC, Hepatocarcinoma; CN-A, Cotylenin A; PEITC, Phenethyl isothiocyanate; PL, Piperlongumine; PDT, Photodynamic therapy; Pa, PD-1 antibody; Ti, TGF-β inhibitor; IKE, Imidazole ketone erastin; HPSCC, Hypopharyngeal squamous carcinoma; SSZ, Sulfasalazine; TMZ, Temozolomide; AR, Androgen receptor; WT, wild-type; EGFR, Epidermal growth factor receptor; TKI, tyrosine kinase inhibitor; PFS, Progression-free survival; NSCLC, Non-small cell lung cancer; TAM, Tumor-associated macrophage; ATM, Ataxia-Telangiectasia mutated gene; CTH, cystathionine γ-lyase.