Review Article

Clinical Advancements in the Targeted Therapies against Liver Fibrosis

Table 1

Summary of the registered clinical trials (Clinicaltrials.gov).

Drug typeDisease conditionPhaseStudy typeTrial number

Small molecule drugs
Farglitazar (GI262570), PPARγ agonistLiver fibrosis with chronic HCV infection2Safety/efficacy studyNCT00244751
Pioglitazone, PPARγ agonistNASH2Safety/efficacy studyNCT01068444
Pioglitazone, PPARγ agonist + vitamin ENAFLD with diabetes mellitus type 2 (T2DM)4Efficacy studyNCT01002547
Pioglitazone, PPARγ agonist + vitamin ENondiabetic patients with NASH3Efficacy studyNCT00063622
(PIVENS)
Pioglitazone, PPARγ agonistHepatic steatosis in HIV/HCV infections4Efficacy studyNCT00742326
Obeticholic acid, FXR agonistNASH fibrosis3Efficacy studyNCT02548351
Obeticholic acid, FXR agonistPrimary biliary cirrhosis3Safety/efficacy studyNCT02308111; NCT01473524
Obeticholic acid, FXR agonistNASH2Efficacy studyNCT01265498
Obeticholic acid, FXR agonistPrimary sclerosing cholangitis2Safety/efficacy studyNCT02177136
Obeticholic acid, FXR agonist + ursodeoxycholic acid (URSO)Primary biliary cirrhosis2Safety/efficacy studyNCT00550862
Losartan, angiotensin II type 1 receptor antagonistLiver fibrosis (F2-F3) with chronic HCV infection4Efficacy studyNCT00298714
Losartan, angiotensin II type 1 receptor antagonistNASH4Efficacy studyNCT01051219
Irbesartan, angiotensin II type 1 receptor antagonistLiver fibrosis with chronic HCV infection3Efficacy studyNCT00265642
Moexipril, angiotensin I converting enzymePrimary biliary cirrhosis2Safety/efficacy studyNCT00588302
Candesartan, angiotensin II type 1 receptor antagonistAlcoholic liver fibrosis1 + 2Safety/efficacy studyNCT00990639
Candesartan, angiotensin II type 1 receptor antagonistLiver fibrosis with chronic HCV infection2Safety/efficacy studyNCT00930995
Glycyrrhizin, antioxidantChronic hepatitis C and F2/F3 liver fibrosis3Efficacy studyNCT00686881
Warfarin, anticoagulantLiver fibrosis2Safety/efficacy studyNCT00180674
Galectin-3 inhibitor (GR-MD-02)NASH with advanced fibrosis2Safety/efficacy studyNCT02421094
Galectin-3 inhibitor (GR-MD-02)Portal hypertension in NASH with cirrhosis2Safety/efficacy studyNCT02462967
Pentoxifylline, TNFα suppressing phosphodiesterase inhibitorPrimary biliary cirrhosis2Safety/efficacy studyNCT01249092
Pentoxifylline, TNFα suppressing phosphodiesterase inhibitor + vitamin ELiver fibrosis with chronic HCV infection3Efficacy studyNCT00119119
Pentoxifylline, TNFα suppressing phosphodiesterase inhibitorNASH2/3Safety/efficacy studyNCT00267670
Pentoxifylline, TNFα suppressing phosphodiesterase inhibitorNASH2Efficacy studyNCT00590161
S-adenosyl methionine (SAMe) versus pentoxifyllineNASH2Efficacy studyNCT02231333
Cenicriviroc, CCR2 and CCR5 antagonistNASH2Safety/efficacy studyNCT02217475
Fuzheng Huayu, herbal medicineLiver fibrosis with chronic HCV infection2Efficacy studyNCT00854087
Sorafenib, tyrosine kinase inhibitorLiver cirrhosis with portal hypertension2Efficacy studyNCT01714609
Erlotinib, EGFR TK inhibitorLiver cirrhosis with HCC resection2Safety/efficacy studyNCT02273362
Everolimus, mammalian target of rapamycin inhibitorLiver fibrosis in posttransplant and recurrent HCV patients2/3Safety/efficacy studyNCT00582738, NCT01888432

Monoclonal antibodies
Simtuzumab, humanized monoclonal antibody against lysyl oxidase-like-2NASH with advanced liver fibrosis2Safety/efficacy studyNCT01672866
Simtuzumab, humanized monoclonal antibody against lysyl oxidase-like-2Liver fibrosis with hepatitis C, HIV, HIV/HCV coinfection2Safety/efficacy studyNCT01707472
Simtuzumab, humanized monoclonal antibody against lysyl oxidase-like-2Liver fibrosis with primary sclerosing cholangitis (PSC)2Safety/efficacy studyNCT01672853
Simtuzumab, humanized monoclonal antibody against lysyl oxidase-like-2 + Selonsertib (GS-4997)-apoptosis signal-regulating kinase 1 (ASK1) inhibitorNASH and fibrosis stages F2-F32Safety/efficacy studyNCT02466516
FG-3019, Human monoclonal antibody against connective tissue growth factorLiver fibrosis with chronic hepatitis B infection2Safety/efficacy studyNCT01217632

Targeted conjugate
Targeted liposome delivering siRNA against HSP47 (ND-L02-s0201)Healthy subjects1Safety studyNCT01858935
Targeted liposome delivering siRNA against HSP47 (ND-L02-s0201)Moderate to extensive hepatic fibrosis (F3-4)1/2Safety/efficacy studyNCT02227459