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).