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

Khosravi, Ali; Jayaram, B.; Goliaei, Bahram; Masoudi-Nejad, Ali

doi:10.1186/s10020-019-0098-x

Molecular Medicine

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)

^#The information provided by OMIM database

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