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Table 1 Summary of prioritized drug candidates

From: Prioritized polycystic kidney disease drug targets and repurposing candidates from pre-cystic and cystic mouse Pkd2 model gene expression reversion

Drug

Drug targets

Mechanism of action

Original indication

Approximate retail price

Amiloride

ADCY10; AOC1; ASIC1; ASIC2; ASIC3; ASIC4; PKD2; PKD2L1; PLAT; PLAU; SCNN1A; SCNN1B; SCNN1D; SCNN1G; SLC9A1; SLC9A2; SLC9A3; TRPC7; TRPV2

Sodium channel blocker

hypertension, congestive heart failure

$

Amisulpride

DRD3; HTR7

Dopamine receptor antagonist

Psychosis, bipolar disorder, schizophrenia

N/A

Amitriptyline

ADRA1A; ADRA1B; ADRA1D; ADRB1; ADRB2; ADRB3; CHRM1; CHRM4; CHRM5; CYP2C9; HRH1; HRH2; HRH4; HTR1B; HTR1D; HTR6; HTR7; KCNA1; KCND2; KCND3; KCNQ2; KCNQ3; NTRK1; NTRK2; OPRD1; OPRK1; OPRM1; ORM2; SIGMAR1; SLC6A2; SLC6A4

Norepinephrine inhibitor, norepinephrine reuptake inhibitor, serotonin receptor antagonist, serotonin–norepinephrine reuptake inhibitor (SNRI)

Depression

$

Bromocriptine

ADCY10; ADRA1A; ADRA1B; ADRA1D; ADRA2B; ADRA2C; DRD1; DRD3; DRD4; GH1; HTR1B; HTR1D; HTR2B; HTR6; HTR7; PRL; PRLR

Dopamine receptor agonist

Hyperprolactinemia, Parkinson's Disease, acromegaly

$$$$

Crizotinib

ALK; AXL; CYP2B6; CYP3A5; EPHA2; EPHA6; EPHB6; IRAK1; IRAK3; LTK; MAP3K2; MAP4K1; MAP4K2; MAP4K3; MAP4K5; MERTK; MET; MST1R; NTRK2; NTRK3; NUDT1; PLK4; ROS1; SLK; STK10; TEK; TIE1

Anaplastic lymphoma kinase (ALK) receptor tyrosine kinase inhibitor

Non-small cell lung cancer (NSCLC)

$$$$$

Diltiazem

CACNA1C; CACNA1S; CACNA2D1; CACNG1; CYP3A5; CYP3A7; EDN1; HTR3A; KCNA5

Calcium channel blocker

Hypertension, angina pectoris

$$$$

Fenofibrate

ABCD2; ABCD3; ABCD4; APOA1; APOB; APOC3; APOE; CCL2; CETP; CRAT; CRP; CYP2C8; CYP2C9; LPL; MMP25; NR1I2; PPARA; PPARD; PPARG; SERPINE1; SREBF2; VCAM1

Peroxisome proliferator-activated receptor (PPAR) receptor agonist

Hypercholesterolemia, hypertriglyceridemia

$$$

Fluoxetine

ANO1; CHRNA2; CHRNA3; CHRNB4; CKS1B; CYP2C9; HTR2B; KCNH2; SLC6A4

Selective serotonin reuptake inhibitor (SSRI)

Depression, obsessive compulsive disorder (OCD), bulimia nervosa, panic disorders, bipolar disorder

$$

Fluphenazine

ADCY10; AR; CALM1; CALM2; CALM3; CHRNA7; DRD1; HRH1; HTR1E; HTR6; HTR7

Dopamine receptor antagonist

Schizophrenia

$$$$

Fluvastatin

APOA1; APOB; APOE; CYBA; CYP2C8; CYP2C9; F3; HMGCR; ICAM1; LDLR; RHOA; SELP; SERPINE1

Hydroxymethylglutaryl-CoA reductase (HMGCR) inhibitor

Hypercholesterolemia, congenital heart defects

$$$$

Imipramine

ADRA1A; ADRA1B; ADRA1D; CHRM1; CHRM4; CHRM5; DRD1; FMO1; HRH1; HTR6; HTR7; KCND2; KCND3; KCNH1; KCNH2; ORM2; SLC22A3; SLC6A2; SLC6A3; SLC6A4

Norepinephrine reuptake inhibitor, serotonin reuptake inhibitor

Depression, nocturnal enuresis

$$$$

Mirtazapine

ADRA1A; ADRA1B; ADRA1D; ADRA2B; ADRA2C; ADRB1; ADRB2; DRD1; DRD3; HRH1; HRH3; HTR2B; HTR3A; HTR7; OPRK1; SLC6A2; SLC6A3; SLC6A4

Adrenergic receptor antagonist, serotonin receptor antagonist

Depression

$

Nicotine

AOX1; CHAT; CHRNA1; CHRNA10; CHRNA2; CHRNA3; CHRNA4; CHRNA5; CHRNA6; CHRNA7; CHRNA9; CHRNB2; CHRNB3; CHRNB4; CHRND; CHRNE; CYP19A1; CYP2A6; CYP2B6; CYP2E1; CYP2U1; FMO1; FMO2; FMO3; FMO4; FMO5; FMO6P; FOS; INMT; PNMT; TBXAS1; TH; TRPA1; UGT1A4; UGT2B10; UGT2B11

Acetylcholine receptor agonist

Smoking cessation

N/A

Paclitaxel

ABCB1; BCL2; CYP2C8; KIF11; KIF1A; KIF1B; KIF1C; KIF5B; MAP2; MAP4; MAPT; NDC80; NR1I2; NUF2; TLR4; TUBB; TUBB1

Tubulin polymerization inhibitor

Ovarian cancer, breast cancer, non-small cell lung cancer (NSCLC)

$$$

Perphenazine

AOX1; CALM1; CALM2; CALM3; DRD1; HRH1; HTR6; HTR7

Dopamine receptor antagonist

Schizophrenia, nausea, vomiting

$$

Pravastatin

ABCC2; APOB; CCL2; CETP; CRP; HMGCR; LCAT; SELP; SLCO1B1

Hydroxymethylglutaryl-CoA reductase (HMGCR) inhibitor

Hypercholesterolemia, myocardial infarction, hyperlipidemia

$

  1. For each drug, known drug targets, mechanism of action, original indication, and approximate retail price. Cost indicators are based on average prices by quartile after the removal of crizotinib as an outliner ($$$$$ = $17,955.50/month). $ is < $24/month, $$ is between $24 and $29/month, $$$ is between $29 and $38.69/month, $$$$ is between $38.69 and $82/month