Table 3.

Single-component drugs targeting both extra- and intracellular factors.

Target			Drug			Clinical trialb		Reference
Target or mechanism type	Target or mechanism	Organsa	Drug Name	Mechanism	Class	Disease	Phase	Reference/Trial identifierc
LOXd	LOXL2d	Liver, Kidney, Lung, Heart, Skin, Gut	β-aminopropionitrile (BAPN)	Inhibitor	Small molecule	Cardiac fibrosis	Preclinical	Martinez-Martinez et al., 2016
			Simtuzumab (GS-6624)	Inhibitor	Monoclonal antibody	Liver fibrosis; IPFd	2(completed); 2(terminated)	NCT01452308; NCT01769196
ROSd	NOX1d/NOX4	Liver, Kidney, Lung, Heart, Pancreas, Skin	GM-CT-01	Inhibitor	Polymer	Liver fibrosis	Preclinical	Traber and Zomer, 2013
			GR-MD-02	Inhibitor	Polymer	Liver fibrosis	2(completed)	NCT02421094
			GCS-100	Inhibitor	Polymer	Renal fibrosis	2(completed)	NCT01843790
	ROS		GKT137831	Inhibitor	Small molecule	Liver fibrosis	Preclinical	Aoyama et al., 2012
			N-acetylcysteine*	Inhibitor	Small molecule	IPF	Approved| Preclinical	Demedts et al., 2005; Zhang et al., 2014
			Mitoquinone	Inhibitor	Small molecule	Liver fibrosis	Preclinical	Vilaseca et al., 2017
			Salvianolic acid B*	Inhibitor	Small molecule	Liver fibrosis; Renal fibrosis; IPF	Preclinical	Liu et al., 2002, 2016; Pan et al., 2011
			Resveratrol*	Inhibitor	Small molecule	Liver fibrosis	3(completed)	NCT02030977
	Vitamin (mimic)	Liver, Kidney, Lung, Heart, Pancreas, Skin, Gut	Pyridoxamine	Inhibitor	Small molecule	Renal fibrosis	2(completed)	NCT00320060
			α-tocopherol	Inhibitor	Small molecule	IPF	Approved| Preclinical	Deger et al., 2007
	Collagen (mimic)	Liver, Kidney, Lung, Skin	IW001	Inhibitor	Collagen	IPF	1(completed)	NCT01199887

^*Drug belongs to monomer extracted from natural products.

^aOrgans that had study report of corresponding targets in fibrosis treatment.

^bClinical trial resource are from http://Clinicaltrials.gov.

^cTrial Identifier is the clinical trail identifier of corresponding drug.

^dLOX, lysyl oxidase; LOXL2, lysyl oxidase homolog 2; IPF, idiopathic pulmonary fibrosis; ROS, reactive oxygen species; NOX1, NADPH oxidase 1.