Target | Drug name (trade name/company) | Category | Highest completed trial | Current trials relevant to ECM stiffness | References |
miR-29 | MRG-201 (miRagen Therapeutics Inc.) | MicroRNA | Phase 1 | None | (26) NCT02603224 |
CTGF | FG-3019 (Fibrogen) | Monoclonal antibody | Phase 2 | Phase 2 | (33, 34) NCT01890265 NCT01262001 |
TGFβ signaling | Pirfenidone (Esbriet/Genentech) | Small molecule, mechanism unknown | Approved: Idiopathic lung fibrosis | Phase 1–3 | (36) NCT01872689 NCT02552849 NCT02408744 NCT03068234 NCT01872689 |
TGFβ | GC1008 (Fresolimumab/Genzyme) | Monoclonal antibody | Phase 2 | Phase 1–2 | (37) NCT01401062 NCT02581787 NCT01665391 |
VEGF, FGF, and PDGF receptors | Nintedanib (Ofev/Boehringer Ingelheim) | Small molecule, tyrosine kinase inhibitor | Approved: Idiopathic lung fibrosis | Phase 1–3 | NCT01284322 |
LOXL2 | GS-6624 (Simtuzumab/Gilead) | Monoclonal antibody | Phase 2 No efficacy in fibrosis or cancer | None | (56–58) NCT01472198 NCT01759511 NCT 01769196 |
LOX | Tetrathiomolybdate | Copper chelator | Phase 3 (Wilson’s disease) | Phase 2 | (60) NCT00805805 NCT00195091 NCT01837329 |
αvβ6 | BG00011/STX-100 (Biogen) | Monoclonal antibody | Phase 2 | None | (89) NCT01371305 |
FAK | VS-6063/PF-04554878 (Defactinib/Verastem) | Small molecule | Phase 2 | Phase 1–2 | (117) NCT02943317 NCT02758587 NCT02546531 NCT02465060 |
FAK | GSK-2256098 (GlaxoSmithKline) | Small molecule | Phase 1 | Phase 1–2 | (117) NCT02551653 NCT02428270 NCT02523014 |
NF-κB | Bortezomib (Velcade/Takeda) | Small molecule | Approved: Multiple myeloma | Phase 2 | (138, 139) NCT02370693 |