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Table 1 Examples of mitochondrial toxicity-related drugs in MitoTox

From: MitoTox: a comprehensive mitochondrial toxicity database

Indication

Drug Name

Mechanism of mitochondrial toxicity

Status

Toxicity

t1/2 (h)a

Protein binding (%)a

LD50 (rat)a

Antidiabetic

Troglitazone

Inhibition of ETC

Withdrawn, 2000

Hepatotoxicity

16–34

> 99%

1.9768 mol/kg

Rosiglitazone

Inhibition of ETC

Approved, investigational

Cardiotoxicity

3–4

99.8%

2.4515 mol/kg

Pioglitazone

Inhibition of ETC

Approved, investigational

Cardiotoxicity

3–7/16–24

> 99%

2.0115 mol/kg

Ciglitazone

Inhibition of ETC

Discontinued

NA

NA

NA

NA

Darglitazone

Inhibition of ETC

Discontinued

NA

NA

NA

NA

Muraglitazar

Inhibition of ETC

Discontinued

NA

NA

NA

NA

Metformin

Inhibition of complex I; uncoupling; impaired TCA cycle

Approved

Lactic acidosis

6.2

> 90%

1000 mg/kg

Anticancer

Doxorubicin

Increased ROS; mtDNA adduct; iron overload

Approved

Cardiotoxicity

20–48

74–76%

21.8 mg/kg

Cisplatin

Inhibition of Complex I

Approved

Nephrotoxicity

0.3–0.7

> 90%

2.7612 mol/kg

Hyperlipidemia

Fenofibrate

Inhibition of complex I

Approved

Hepatotoxicity

20

~ 99%

> 2000 mg/kg

Clofibrate

Inhibition of complex I

Approved

Hepatotoxicity

18–22

95–97%

940 mg/kg

Ciprofibrate

Inhibition of complex I

Approved

Hepatotoxicity

NA

NA

NA

Psychotropic

Valproic acid

Inhibition of TCA cycle

Approved

Coma and respiratory depression

9–16

90%

670 mg/kg

Clozapine

Inhibition of the ETC

Approved

Metabolic syndrome

8

97%

3.0838 mol/kg

Fluoxetine

Uncoupler

Approved

CNS, GI effects

1–3 days

94.5%

2.6048 mol/kg

Nefazodone

Inhibition of Complex I and complex IV

Withdrawn

Hepatotoxicity

2–4

> 99%

2.9067 mol/kg

Analgesic

Acetaminophen

Oxidative stress

Approved

Hepatotoxicity

1–4

25%

1944 mg/kg

Aspirin

mPTP potentiation

Approved

Cardiotoxicity, GI effects

0.25

99.5%

920–1480 mg/kg

Diclofenac

Inhibition of ETC and ATP synthase

Approved

Nephrotoxicity

2

> 99%

3.6447 mol/kg

Antibacterial

Imipenem

Oxidative stress

Approved

Nephrotoxicity

1.3–5.1

20%

1.8089 mol/kg

Chloramphenicol

Depletion of iron

Approved

Aplastic anemia

1.5–3.5

50–60%

2500 mg/kg

Antiviral

Zidovudine

mtDNA replication (inhibit mtDNA polymerase-γ)

Approved

Myopathy

0.5–2.9

30–38%

NA

  1. aFrom DrugBank (https://www.drugbank.ca/)