Table 1.
Drugs potentially targeting CAFs
| Target factor |
Expression cell | Function | Drug | Mechanism | Clinical Trial |
Reference |
|---|---|---|---|---|---|---|
| VEGF | tumor cells CAFs, TAMs. | Angiogenesis | Bevacizumab | Neutralization VEGF | Phase II | (119) |
| Adsflt | Interception of VEGF | Preclinical | (120) | |||
| IMC-1C11 | anit-VEGFR-2 antibody | Phase I | (121) | |||
| RPI.4610 | anti-VEGFR-1 ribozyme | Phase II | (122) | |||
| Tenascin-C | CAFs, cancer cells | cell adhesion | 81C6 | radioimmunotherapy | Phase II | (113) |
| ATN-RNA | siRNA | Phase I | (123) | |||
| FAP | CAFs, TECs, cancer cells | Serine protease | PT-100 | activity inhibitor | Phase I | (124) |
| Sibrotuzumab | anti-FAP antibody | Phase I | (125) | |||
| Sc40-FasL | induce apoptosis of FAP+
cells |
preclinical | (126) | |||
| Rebimastat | activity inhibitor | Phase III | (127) | |||
| CTGF | CAFs, TECs, cancer cell, neural |
Growth factor | FG-3019 | anti-CTGF antibody | preclinical | (128) |
| DN-9693 | degrade mRNA | preclinical | (129) | |||
| MMPs | CAFs, TECs, TAMs, cancer cells |
metalloproteinases | Marimastat | activity inhibitor | Phase III | (130) |
| Tanomastat | activity inhibitor | Phase III | (131) | |||
| Rebimastat | activity inhibitor | Phase III | (127) | |||
| uPA | CAFs, TAMs, cancer cells | Serine protease | PAI-2 | activity inhibitor | preclinical | (132) |
| uPA-UT1 | activity inhibitor | preclinical | (133) | |||
| CA IX | CAFs, cancer cells | Carbonic anhydrase | Rencarex WX-G250 | induce ADCC | Phase III | (134) |