Table 5.1 List of FDA-approved repurposed drugs classified according to on- and off-target approach indicating their cellular targets and original and

repositioned indications

Strategy

Drug

Cellular target

Original indication

Repositioned indication

Reference

On-

target

Sildenafil

• PDE5

Hypertension, angina

Erectile dysfunction

Ghofrani et al. (2006), Unegbu

et al. (2017), Sildenafil (2021)

Thalidomide

• TNF-α

Erythema nodosum laprosum

(ENL)

HIV/AIDS

Kim and Scialli (2011),

Thalidomide (2021)

Duloxetine

• Serotonin,

noradrenaline

Depression

Stress urinary incontinence

(SUI)

Ashburn and Thor (2004), Gupta

et al. (2007), Duloxetine (2021)

Finasteride

• Type II

5-α-reductase

Benign prostatic hyperplasia

Male pattern hair loss

McClellan and Markham (1999),

Henriksen et al. (2011),

Finasteride (2021)

Trastuzumab

• Receptor tyrosine-

protein kinase erbB-2

HER-2-positive breast cancer

HER-2-positive metastatic

gastric cancer

Boekhout et al. (2011), Rogers

et al. (2014), Trastuzumab

(2021)

Off-

target

Furosemide

• Carbonic anhydrase

2

• G protein-coupled

receptor 35

• Solute carrier family

12 member 1

Oedema associated with

congestive heart failure

Moderate to severe

hypertension

Divorty et al. (2018), Furosemide

(2021)

Mifepristone

• Progesterone

receptor

• Glucocorticoid

receptor

Pregnancy termination

Hyperglycaemia secondary to

hypercortisolism in Cushing’s

syndrome

Jang and Benet (1998), Fjerstad

et al. (2009), Mifepristone (2021)

(continued)

5

Genomic Approaches for Drug Repositioning

53