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Table 1 Summary of the evidence of anti-neoplastic role of the anti-parasitic drugs: their current indications, cellular cytotoxic mechanisms of cancers, BBB penetration profile and radiosensitivity response

From: Targeting tumor hypoxia and mitochondrial metabolism with anti-parasitic drugs to improve radiation response in high-grade gliomas

Drug Name Indications Mechanism of Action Efficacy in Cancers Efficacy in Brain Cancers BBB Penetrability Radiosensitivity Source
Atovaquone FDA-labelled:
• Pneumocystis Pneumonia
Non-FDA labelled:
• Malaria
• Toxoplasma Encephalitis
• Toxoplasmosis
• Babesiosis
• Mitochondrial dysfunction and oxidative stress
• Akt/AMPK/mTOR pathway Inhibitor
• STAT3 Inhibitor
• Breast Cancer
• Hypopharyngeal carcinoma
• Colorectal Carcinoma
• Lung Carcinoma
• Cervical Cancer
• Retinoblastoma
• Renal Cell Carcinoma
• Acute Myeloid Leukemia
• Thyroid Carcinoma
• Glioblastoma Yes • Hypopharyngeal Carcinoma [84,85,86,87,88,89,90,91,92]
Ivermectin FDA-labelled:
• Infection by Onchocerca volvulus
• Intestinal strongyloidiasis
• Pediculosis Capitis
• Rosacea
Non-FDA labelled:
• Ascariasis
• Infection by Loa loa
• Cutaneous larva migrans
• Enterobiasis
• Infection by Wuchereria bancrofti
• Infestation by Phthirus pubis
• Mansonelliasis
• Scabies
• Mitochondrial dysfunction and oxidative stress
• Akt/mTOR pathway inhibitor
• Induces cytostatic autophagy by targeting PAK1/Akt axis
• Induces chloride dependent membrane hyperpolarization
• WNT/TCF pathway inhibitor
• Induces DNA fragmentation and chromatin condensation
• Inhibition of ROS-TFE3-dependent autophagy and enhancing apoptosis
• Renal Cell Carcinoma
• Chronic Myeloid Leukemia
• Breast Cancer
• Ovarian Cancer
• Colon Cancer
• Leukemia
• Melanoma
• Oesophageal squamous cell carcinoma
• Cervical Cancer
• Glioblastoma
• Neuroglioma
Limited (increases with increase in concentration)   [93,94,95,96,97,98,99,100,101,102,103,104]
Mefloquine FDA-labelled:
• Malaria
• PI3K/Akt/mTOR inhibitor
• Mitochondrial dysfunction and oxidative stress
• Lysosomal disruption
• Disrupts endolysosomal RAB5/7
• Targets B-catenin pathway
• Inhibits NF-κB signaling
• Induces autophagy and endoplasmic reticulum stress
• Prostate Cancer
• Gastric Cancer
• Cervical Cancer
• Acute Myeloid Leukemia
• Chronic Lymphocytic Leukemia
• Colorectal cancer
• Liver cancer
• Breast Cancer
• Glioblastoma Yes   [105,106,107,108,109,110,111,112,113,114]
Proguanil FDA-labelled:
• Malaria, Plasmodium Falciparum
Non-FDA labelled:
• Malaria, Plasmodium Vivax
• Mitochondrial dysfunction and oxidative stress • Colon Cancer
• Bladder Cancer
  Yes   [115]
Quinacrine Non-FDA labelled:
• Malaria
• Giardiasis
• Tapeworm infection
• Systemic Lupus erythematosus
• Rheumatoid arthritis
• Malignant pleural effusions
• Prevention of recurrent pneumothorax
• Female sterilization
• DNA intercalator, inhibits DNA repair pathways
• FACT c-trapping
• Induces apoptosis via TRAIL signaling, modulating topoisomerases, inhibiting NF-κB and inducing p53
• Arachidonic acid pathway inhibitor
• Induces cytostatic autophagy and inhibits cytoprotective autophagy
• Modulates cell cycle arrest
• Breast Cancer
• Colon Carcinoma
• Ovarian Cancer
• Non-small cell lung cancer
• Diffuse large B-cell lymphoma
• Colorectal Cancer
• Leukemia
• Renal Cell Carcinoma
• Melanoma
• Gastric Cancer
• Anaplastic Thyroid Cancer
• Glioblastoma Yes   [116,117,118,119,120,121,122,123,124,125,126,127]