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. 2022 Nov 7;11(11):2202. doi: 10.3390/antiox11112202

Table 1.

List of OXPHOS inhibitors under clinical trials or potential.

OXPHOS Inhibitor Identifier Phase Cancer Type ECT Target Ref.
Metformin NCT04275713, NCT04414540, NCT04945148, NCT04387630 II, II, II, II Cervical cancer, head and neck squamous cell carcinoma, glioblastoma (IDH-wildtype), breast cancer Complex I [92]
Phenformin NCT03026517 I Melanoma Complex I [92]
Arsenic Trioxide NCT02066870, NCT03503864 I, II Non-small-cell lung cancer, neuroblastoma Complex I [93]
Papaverine NCT05136846, NCT03824327 I, I Locally advanced or unresectable non-small-cell lung cancer Complex I [95]
Atovaquone NCT04648033, NCT02628080 I, I Locally advanced non-small-cell lung cancer, non-small-cell lung cancer Complex III [96]
Proguanil N.A. N.A. Acts synergistically with atovaquone Complex I [97]
Pyrvinium Pamoate NCT05055323 I Resectable pancreatic ductal adenocarcinoma Complex I [98]
Vitamin E NCT01871454 II Non-small-cell lung cancer Complex II [99]
ONC201 NCT04055649 II Platinum-resistant epithelial ovarian, fallopian tube, or primary peritoneal cancer, diffuse midline gliomas Complex I, II [100]
Mitoxantrone NCT04927481, NCT03839446, NCT03258320, NCT04718402 II, II, I, I Breast cancer, acute myeloid leukemia, prostate cancer patients, advanced gastric carcinoma Complex V [101]
Ivermectin N.A. N.A. Induces the death of renal cancer cells, chronic myeloid leukemia cells, and glioblastoma cells * Complex I [102]
Anonacin N.A. N.A. Delays the growth of pancreatic cancer cells * Complex I [103]
Trifluoperazine N.A. N.A. Induces pancreatic ductal adenocarcinoma cell death in combination with bortezomib * Mitochondrial Stress [104]

* indicates that the drug has not been validated by clinical trials but has been confirmed in in vitro cell experiments and in vivo xenograft models.