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. 2021 Apr 18;13(8):1953. doi: 10.3390/cancers13081953

Table 2.

Drug class, specific drug, drug target, and current clinical phase of repurposed agents currently undergoing clinical investigation.

Drug Class Drugs Targets Clinical Trial Stage References
Antiepileptic Drugs Valproic Acid HDAC Phase II [70,84,85,86,87,88]
Disulfiram Disulfiram PLK1, Ubiquitin–Proteasome Pathway, AIF Phase II/III [89,90,91]
Antifungals Azoles Hexokinase II Phase I [92,93,94]
Clioquinol BAX, BCL-2 Phase I [92,95]
Antimalarials Atovaquone STAT3 Preclinical [31]
Chloroquine Unclear Preclinical [26,41,86,96,97]
Hydroxychloroquine LC3-II Phase I/II [98]
Mefloquine NMDA Phase I/II [99,100,101]
Antiparasitics Mebendazole Microtubules, VEGF Phase I [102,103,104,105,106]
Antihypertensives ARBs, ACEis Unclear Retrospective [32,44,45,107,108]
Anti-inflammatories Celecoxib COX-2 Phase I–II [109,110,111]
Immunosuppressants Temsirolimus mTOR, MCL-1 Phase I [42]
Everolimus Phase I/II [112,113,114,115,116]
Antineoplastics Vorinostat HDAC Phase I/II [117]
Cabozantinib TK Phase II [118]
Arsenic Trioxide Cytochrome C Phase I/II [119]
Marizomib Proteasome Phase I [120,121]
Fimepinostat PI3K, HDAC Phase I [122]
Carbonic-Anhydrase Inhibitors Acetazolamide CA, BCL3 Phase I [123,124,125]
Checkpoint Inhibitors Nivolumab PD-1 Phase II–III [126,127,128,129,130,131]
Pembrolizumab PD-1 Phase I–II [132,133,134]
Ipilimumab CTLA-4 Phase I [129]
Diabetic Agents Metformin AMPK, Cl-Channels, mTOR Phase I/II [46,135,136,137,138,139,140,141,142,143,144,145,146,147]
Small Molecules and Biologics Cetuximab EGFR Phase I [148]
5-ALA Not Applicable Phase III [149,150,151,152]
Cocktails CUSP-9 Survival Pathways Phase I [5,153,154,155,156,157]
CLOVA GSK-3B Phase I [153]
Celecoxib, Vinblastine, Cyclophosphamide COX-2, Microtubules, DNA Phase I [158]

Abbreviations: Histone deacetylase (HDAC); polo-like kinase 1 (PLK1); apoptosis inducing factor (AIF); Bcl-2-associated X protein (BAX); B-cell lymphoma 2 (BCL2); signal transducer and activator of transcription 3 (STAT3); light chain 3 phosphatidylethanolamine conjugate (LC3-II); N-methyl-D-aspartate receptor (NMDAR); vascular-endothelial growth factor 2 (VEGF); cyclooxygenase 2 (COX2); mechanistic target of rapamycin (mTOR); myeloid cell leukemia-1 (MCL-1); tyrosine kinase (TK); phosphoinositide 3-kinase (PI3K); carbonic anhydrase (CA); B-cell lymphoma 3-encoded protein (BCL-3); programmed cell death 1 (PD-1); cytotoxic T-lymphocyte-associated protein 4 (CTLA4); AMP-activated protein kinase (AMPK); epidermal growth factor receptor (EGFR); glycogen synthase kinase (GSK) 3β; deoxyribonucleic acid (DNA).