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Table 1 Current medications studied for radiation-induced fibrosis

From: Tissue fibrosis induced by radiotherapy: current understanding of the molecular mechanisms, diagnosis and therapeutic advances

Name

Molecular type

Target/action

Site

Stage of project trial

References

SOD-TAT

Ligand-modified SOD

Scavenging ROS and free radicals

Lung

Preclinical study

[296]

AEOL10113

Nonenzymatic SOD mimic

Suppressing redox-regulated pathways

Lung, rectum, prostate

Preclinical study

[300, 302, 305]

Melatonin

Indole-derived hormone

Scavenging ROS and RNS and activating antioxidative enzymes

Lung

Preclinical study

[307]

Combined PTX and Vit E

A methylxanthine derivative and a vitamin

antioxidant, anti-inflammatory and suppressing the TGF-β pathway

Neck and chest

In clinical use

[314,315,316,317]

Triptolide

Diterpenoid epoxide

Inhibiting the activity of alveolar macrophages and the IKKβ/NF-κB pathway

Lung

Preclinical study

[324]

SKI2162, EW-7197, LY2157299, LY2109761

TGFβR I inhibitor

Blocking TGF-β receptor I

Lung, skin

Preclinical study

[325,326,327,328]

P144

Hydrophobic peptide

Binding to soluble TGF-β1

Muscle

Preclinical study

[329]

Imatinib

Receptor tyrosine kinase inhibitor

Blocking PDGF receptor

Lung, skin

Preclinical study

[331]

Pamrevlumab

Monoclonal antibody

Blocking CTGF receptor

Lung

Preclinical study

[105]

sLRP6E1E2

Soluble Wnt receptor

Binding to extracellular Wnt ligands

Skin

Preclinical study

[101]

Curcumin

Natural polyphenol

Activating antioxidative enzymes, inhibiting NF-κB pathway and downregulating inflammatory factors

Lung, skin

Preclinical study

[364, 366]

Rosmarinic acid

Natural polyphenol

Inhibiting RhoA/Rock pathway

Lung, parotid glands

Preclinical study

[370, 371]

GSPs

Plant extract

Ameliorating mitochondrial dysfunction and inhibiting MAPK pathway

Lung, breast

In clinical trials (NCT00041223)

[377]

Pirfenidone

Pyridone analog

Inhibiting TGF-β1/Smad3 pathway

Lung, skin

In clinical trials (NCT03902509)

[385]

Nintedanib

Receptor tyrosine kinase inhibitor

VEGF receptor, FGF receptor and PDGF receptor

Lung

Preclinical study

[386]

Esomeprazole

Proton pump inhibitor

inducing of MAPK/Nrf2/HO1 pathway and inhibiting of DDAH/iNOS pathway

Skin

Preclinical study

[345]

Metformin

 

activating AMPK and Inhibiting respiratory chain complex I

Lung, heart, skin

Preclinical study

[390,391,392,393,394]

Losartan

ACEI

inhibiting TGF-β/Smad signaling pathway

Heart, breast

In clinical trials (NCT05637216) (NCT05607017)

[354]

Deferoxamine

Iron chelator

Inhibiting HIF-1α

Skin

Preclinical study

[356,357,358]

Methoxyestradiol

Metabolite of estradiol

inhibiting HIF-1α

Lung, skin

Preclinical study

[359, 361]

MSCs

 

secreting anti-inflammatory and antifibrotic factors

Lung, parotid glands

In clinical trials (NCT02513238) (NCT02277145)

[400]

  1. SOD superoxide dismutase; PTX pentoxifylline; Vit E vitamin E; GSPs Grape seed proanthocyanidins; MSCs Mesenchymal stem cells