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Table 1 List of OXPHOS inhibitors tested in this study

From: Characterizing OXPHOS inhibitor-mediated alleviation of hypoxia using high-throughput live cell-imaging

OXPHOS inhibitor

Mitochondrial complex targeted

Selected clinical trials as anticancer therapeutic

Tested in selected trial as hypoxia modifier

Purpose

Remarks

IACS-010759

I

NCT02882321

No

Phase I, assess safety and efficacy in advanced solid tumors and acute myeloid leukemia

Both trials discontinued due to toxicities

NCT03291938

No

Metformin

I

NCT02394652

Yes

Phase II, window-of-opportunity trial in locally advanced cervical cancer

 

Atovaquone

III

NCT0268080

Yes

Phase I, window-of-opportunity trial in NSCLC

 

NCT04648033

Yes

Phase I, determine MTD of ATO in combination with concurrent CRT in NSCLC

 

Mito-Atovaquone

I, III

-

-

 

Pre-clinical study: anti-tumor effect of In Situ vaccination with Mito-ATO

Mito-PEG-Atovaquone

I, III

-

-

-

 

Tamoxifen

I, II, III, IV

NCT03280563

No

Phase II, assess safety, efficacy and pharmacokinetics of anti-PD-L1 mAb also combined with tamoxifen in metastatic breast cancer

 

NCT00003857

No

Phase III, effectiveness of radiotherapy with or without Tamoxifen in ductal carcinoma in situ

 

MitoTam

I

MitoTam-01, EudraCt 2017-004441-25

No

Phase I/Ib, evaluate drug safety and MTD, and long term toxicity

 
  1. Abbreviations: NSCLC Non-small Cell Lung Carcinoma, MTD Maximum tolerated dose, CRT Chemoradiotherapy