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. 2019 Feb 15;42(2):113–127. doi: 10.1007/s12272-019-01127-y

Table 1.

Drugs with anticancer efficacy via targeting mitochondrial bioenergetics

Target Drug Cancer types Developmental phase References
Mitochondrial biogenesis
 Mitochondrial HSP90 Gamitrinib Melanoma, glioblastoma Preclinical (Zhang et al. 2016; Ghosh et al. 2015)
 Mitochondrial ribosome Several antibiotics Multiple types Repositioning (Lamb et al. 2015; De Luca et al. 2015)
Oxidative phosphorylation
 Mitochondrial complex I Biguanides Multiple types Repositioning (Birsoy et al. 2014; Hirsch et al. 2009)
Rotenone Glioblastoma Repositioning (Janiszewska et al. 2012)
BAY 87-2243 Melanoma Preclinical (Schöckel et al. 2015)
IACS-010759 AML and solid tumors Phase 1 clinical (Molina et al. 2018)
 Mitochondrial complexes Graphene Multiple types Preclinical (Zhou et al. 2014)
 MCT1/2 AR-C155858 Breast cancer Preclinical (Lamb et al. 2014)
 Unknown Nitazoxanide Colorectal cancer Repositioning (Senkowski et al. 2015)
Niclosamide Breast cancer, Ovarian cancer Repositioning (Wang et al. 2013; Yo et al. 2012)
Fatty acid oxidation
 CPT1 Etomoxir Multiple types Repositioning (Camarda et al. 2016; Lin et al. 2017; Tan et al. 2018)
Perhexiline Multiple types Repositioning (Rodriguez-Enriquez et al. 2015)
ST1326 Lymphoma, leukemia Preclinical (Samudio and Konopleva 2015)
 Unknown Avocatin B AML Preclinical (Lee et al. 2015b)
 PPARα NXT629 Melanoma, Ovarian cancer Preclinical (Stebbins et al. 2017)