Table 1 List of repurposed drugs that have gone or are undergoing clinical trials for anti- cancer indications.
Highest Phase of Clinical Trials | Drug | Original Indication | Reported Targets | Cancer Types |
|---|---|---|---|---|
Pre-clinical | Cimetidine | Reduce stomach acid [127] | H2 receptor antagonist | Lung adenocarcinoma [41] |
Clomiphene citrate | Luteal phase dysfunction [128] | Oestrogen agonist | GB [129] | |
Etomoxir | Chronic heart failure, Diabetes mellitus [130] | Inhibitor of CPT1, prevent FAO | Bladder cancer [130] | |
Phase I | Imipramine | Depression [131] | Serotonin receptor, glutamate receptors | Breast cancer [132] NCT03122444 GB [42] |
Thioridazine | Anti-psychotic [133] | DRD2 | AML [80] NCT02096289 | |
Repaglinide | Diabetes mellitus [134] | Inhibits potassium efflux | Prostate cancer [135] NCT04664725 Ovarian cancer NCT04718740 | |
Phase II | Quinacrine | Malaria, giardiasis, rheumatoid arthritis [90] | p53, FACT-CK2-p53 axis | Colorectal adenocarcinoma NCT01844076 NSSLC [136] NCT01839955 |
Auranofin | Arthritis [38] | TrxR | CLL [137] NCT01419691 Ovarian cancer NCT03456700 | |
Itraconazole | Anti-fungal agent [90] | mTOR-cholesterol trafficking, VDAC1, PDGF-Akt–mTOR axis | NSSLC [138] NCT03664115 BCC and other skin cancers NCT01108094 | |
Niclosamide | Anti-helminthic drug [90] | Wnt/β-catenin, STAT3, NF-κB, Notch, ROS, mTORC1 | Prostate cancer NCT02807805 Colorectal cancer NCT02519582 [139] | |
Disulfiram | NSAID, alcohol-aversion drug [90] | ALDH, NAD+-dependent proteins | NSSLC [140] NCT00312819 GB NCT01907165 | |
Diclofenac | NSAID, analgesia [141] | cGMP system, COX-1/2, | BCC NCT01358045 [142] | |
Chlorpromazine | Anti-psychotic [143] | DRD2 agonist PI3K/mTOR | GB [144] NCT04224441 | |
Lovastatin | HMG-CoA reductase, inhibits some RAS isoprenylation | Ovarian cancer [147] NCT00585052 | ||
Phase III | Chloroquine | Malaria, rheumatoid arthritis [90] | Autophagy, PPT1 | GB [148] NCT00224978 Breast cancer NCT02333890 |
Nelfinavir | HIV [149] | Autophagy and apoptosis, HIV protease | Cervical carcinoma NCT03256916 [74] | |
Curcumin | Dermatological diseases [150] | hTERT, Wnt/β-catenin, cytokines, Hippo/YAP | Prostate cancer NCT03769766 Colon cancer [151] NCT00295035 | |
Genistein | Menopause, osteoporosis, obesity [152] | hTERT, Wnt/β-catenin, cAMP/PKA | Prostate cancer NCT00584532 Bladder cancer NCT00118040 [153] | |
Berberine | Bacterial diarrhoea [90] | Ephrin-B2, MMP-2/MMP-9, EMT, miR-101, VEGF | Colorectal adenoma [154] NCT02226185 NCT03281096 | |
Mebendazole | Intestinal helminthiasis [90] | Chk2, Nbs1, PARP-1, DHODH | Colon cancer NCT03925662 [155] | |
Aspirin | NSAID for pain and fever [90] | COX-1/2, ANXA1- NF–κB axis, CDX2, COMMD1–RelA axis | Colon cancer NCT02467582 [156] | |
Propranolol | Anti-hypertensive [157] | β-adrenoceptor antagonist | Malignant melanoma [158] NCT02962947 | |
Phase IV | Ritonavir | HIV [90] | p53, CDKs-RB axis, AKT-E2F-1-RB axis | Kaposi’s sarcoma NCT00444379 [159] |
Thalidomide | Sedative, anti-emetic [90] | Proangiogenic factors, VEGF receptor, NF-κB | T-cell Lymphoma NCT01664975 Multiple myeloma NCT00652041 Prostate cancer [160] NCT00020085 | |
Metformin | Type II diabetes mellitus [90] | AMPK, PI3K-mTOR pathways, BACH1 | Prostate Cancer NCT02511665 Breast cancer NCT05507398 NCT01905046 Endometrial carcinoma [49] NCT05192850 |
