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Table 1 Anti-melanoma repurposed candidate drug molecules and supporting information based on a wide range of data analyses

From: Active repurposing of drug candidates for melanoma based on GWAS, PheWAS and a wide range of omics data

Drug Name Current drug indication Stage Target Action mode Pathogenesis Supporting evidence
Erythromycin Respiratory tract infections Recruiting CYP3A7 Inhibitor GOF, human drug metabolizing enzyme (Neunzig et al. 2011) NA
Milrinone Congestive heart failure Recruiting PDE3A Inhibitor GOF, Targeting tumor cells (Nazir et al. 2017) (Murata et al. 2002)
Dapsone Leprosy and dermatitis herpetiformis Completed CYP3A7, NAT2 Substrate LOF, Arylamine n-acetyltransferase activity# (Kyllo et al. 2014)
Theophylline Chronic asthma NA CYP1A2, CYP1B1, CYP2D6, PDE3A Inhibitor, Substrate GOF, Phosphodiesterase Inhibitors# (Steinberg and Whittaker 1976; Wick 1981)
Gefitinib Metastatic nonsmall cell lung cancer Completed CYP1A1, EGFR Antagonist GOF, Ubiquitin protein ligase binding# (Djerf et al. 2009)
Omeprazole Duodenal ulcers Completed ABCC3, CYP1A1, CYP1A2 Inducer LOF, Organic anion transmembrane transporter activity# (Matsui et al. 2015)
Levonorgestrel Enopausal and postmenopausal disorders Completed CYP19A1, ESR1 Inhibitor GOF, Nuclear hormone receptor (Grostern et al. 2001) (Kjaeldgaard et al. 1988)
Mexiletine Ventricular fibrillation Completed CYP1A2 Inhibitor LOF, Oxidoreductase activity (Kuraishi et al. 2003) (Kuraishi et al. 2003; Andoh et al. 2008)
Rosiglitazone Type 2 diabetes mellitus Completed CYP2A6 Inhibitor GOF, Steroid hydroxylase activity# (Mossner et al. 2002)
Chloramphenicol Etracycline-resistant vibrios Recruiting CYP3A7 Inhibitor GOF, Oxygen binding# (Lamb et al. 2015)
Buspirone Anxiety disorders Completed CYP3A7 Substrate LOF, Oxygen binding# NA
Zidovudine Human immunovirus infections Completed CYP2A6, TERT Substrate, Inhibitor GOF, Steroid hydroxylase activity (Hahn et al. 1999) (Fang and Beland 2009)
Flutamide Prostate cancer Completed CYP1B1 Substrate, Inhibitor GOF, Oxygen binding# (Hsueh et al. 2003)
Cimetidine Peptic ulcer disease Completed SLC22A5, CYP3A7 Inhibitor GOF, Symporter activity (Flodgren et al. 1983) (Flodgren et al. 1983; Harland and Saihan 1989)
Diclofenac Osteoarthritis and rheumatoid arthritis Completed PLA2G2A Inhibitor GOF, Phospholipid binding# (Albano et al. 2013)
Monobenzone Skin vitiligo NA TYR Inhibitor GOF, Protein homodimerization activity (Chen et al. 2009) (van den Boorn et al. 2010)
Trazodone Depression Completed CYP3A7 Substrate LOF, Oxygen binding# (Chang and Lin 2011)
Verapamil Hypertension, angina, and cluster headache Completed SLC22A5 Inhibitor GOF, Symporter activity# (Robinson et al. 1986; Formelli et al. 1988)
Cefixime Various infections Completed SLC22A5 Inhibitor GOF, Symporter activity (Ganapathy et al. 2000) NA
Flurbiprofen Osteoarthritis and ankylosing spondylitis Completed UGT1A1 Inhibitor GOF, Steroid binding (Zhou et al. 2009) NA
Norethisterone Dysfunctional Uterine Bleeding Completed CYP3A7 Substrate LOF, Oxygen binding (Preissner et al. 2010) (Kjaeldgaard et al. 1988)
Risperidone Schizophrenic disorders Completed CYP3A7 Substrate LOF, Oxygen binding (Preissner et al. 2010) (Uzawa et al. 2014)
Hydrocortisone Acute Gouty Arthritis Completed CYP3A7 Substrate LOF, Oxygen binding (Preissner et al. 2010) (Wang et al. 2018; Rathore et al. 2016)
Estradiol Vasomotor symptoms Completed CYP1B1, CYP2C8, CYP3A7, UGT1A1, ESR1 Agonist LOF, Zinc ion binding# (Kanda and Watanabe 2001; Poletini et al. 2016; Li et al. 2017)
Tacrolimus Heart Transplant Rejection Completed CYP3A7 Substrate LOF, Oxygen binding# (Matsumoto et al. 2018; Puza et al. 2018)
Zalcitabine Human Immunodeficiency Virus Completed DCK Substrate GOF, Protein homodimerization activity (Rossi et al. 1999) (Hardeman et al. 2017)
Acetylsalicylic acid Moderate Pain Completed EDNRA Inhibitor GOF, Receptor for endothelin-1# (Kumar et al. 2018)
Rifampicin Tuberculosis Completed ABCC3, CYP2A6 Inducer, inhibitor GOF, Steroid hydroxylase activity# (Levavasseur et al. 2016)
Praziquantel Schistosoma infection Completed CYP3A7 Substrate LOF, Oxygen binding# NA
Norfloxacin Urinary tract infection Recruiting SLC22A5, CYP3A7 Inhibitor GOF, Symporter activity# (Gouvea et al. 2012)
Amiodarone Recurrent ventricular fibrillation Completed CYP2A6, CYP3A7 Inhibitor GOF, Steroid hydroxylase activity (Zhou et al. 2009) (Zuba et al. 2016)
Bupropion Depression, Bipolar Completed CYP2A6 Substrate LOF, Steroid hydroxylase activity# (Ashrafi et al. 2018)
Mitoxantrone Progressive relapsing Completed CYP1B1 Inhibitor GOF, Oxygen binding# (Yu et al. 2015; Yu et al. 2016)
Saquinavir Human Immunodeficiency Virus Completed CYP3A7 Substrate LOF, Oxygen binding# (Mijatovic et al. 2011; Donia et al. 2012)
Clomipramine Obsessive Compulsive Disorder Completed GSTP1 Inhibitor GOF, S-nitrosoglutathione binding# (Parker et al. 2012)
  1. #The information provided by OMIM database