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. 2020 Sep 20;23(9):811–817. [Article in Chinese] doi: 10.3779/j.issn.1009-3419.2020.104.16

2.

铁死亡诱导治疗相关的临床药物和化合物

Clinical drugs and compounds related to ferroptosis-inducing treatment

Classification Drugs/Compounds Target Phenomena/Conclusion
GSH: glutathione; SASP: sulfasalazine; IN OPs: iron-oxide nanoparticles; LIP: labile iron pool; SQS: squalene synthase.
Existing clinical drugs Cisplatin[30] GSH/GPX4 Combination therapy of cisplatin with erastin showed significant synergistic effect on their anti-tumor activity[30]
Lapatinib[31] LIP Lapatinib and siramesine treatment induced ferroptosis in breast cancer cells[31]
FINs Calss Ⅰ FIN SASP[35] System Xc-/GSH SASP restrained growth of NCI-H69 and LU-SCLC tissue xenografts[35]
Sorafenib[36] Sorafenib induced ferroptosis in NCI-H460 cells[36]
Class Ⅱ FIN - GPX4 Not suitable for in vivo use due to poor pharmacokinetic[37]
Class Ⅲ FIN - SQS/GPX4 Cerivastatin and simvastatin inhibit mevalonate pathway enzyme, making cells sensitive to ferroptosis [39]
Class Ⅳ FIN Iron compound[40, 42-44] LIP Iron compounds induced ferroptosis in cancer cells
HMOX1[40, 41]
FINO2[45, 46]
New prospects IN OPs LIP Ferumoxytol has been used to inhibt the growth of lung cancer metastases[49]
IN OPs with cisplatin(Ⅳ) prodrugs enhanced anticancer activity but minimized systemic toxicity [50]
Immunotherapy System Xc- Immunotherapy-activated CD8+ T cells enhance lipid peroxidation in cancer cells[51]
Radiation therapy GSH/GPX4 IR induces ferroptosis in cancer cells and class Ⅰ, Ⅱ, Ⅲ FINs exhibit radiosensitization[55]