Table 1 The clinical trials of drugs targeting CAFs, TGF-β, MMPs, LOX, TRP, Integrins, Rho/ROCK, FAK and YAP1/TAZ for cancer therapy
Target | Drug | Drug properties | Tumor type | Phase | enrollment | Status/results | Trial ID |
|---|---|---|---|---|---|---|---|
CAFs | Erdafitinib | Pan-FGFR inhibitor | Advanced solid tumors | Phase 2 | 316 | Recruiting | NCT04083976 |
| Â | Â | Â | Bladder cancer | Phase 2 | 25 | Recruiting | NCT04917809 |
| Â | Â | Â | Advanced solid tumors | Phase 2a | 35 | Recruiting | NCT02699606 |
| Â | Â | Â | Prostate cancer | Phase 2 | 9 | poorly tolerated | ACTRN12618001061224 |
| Â | Â | Â | Advanced NSCLC | Phase 2 | 22 | Completed | NCT03827850 |
TGF-β | Fresolimumab | Neutralizing antibody of TGF-β | Metastatic Breast Cancer | Phase 2 | 23 | Favorable prognosis | NCT01401062 |
| Â | Â | Â | Malignant pleural mesothelioma | Phase 2 | 13 | Favorable prognosis | NCT01112293 |
|  | Galunisertib | TGF-β receptor kinase inhibitor | Solid tumors | Phase 1b/2 | 170 | Favorable prognosis | NCT01373164 |
| Â | Â | Â | Solid tumors | Phase 1b/2 | 25 | Well tolerated | NCT02423343 |
| Â | Â | Â | Hepatocellular Carcinoma | Phase 2 | 47 | Favorable prognosis | NCT01246986 |
| Â | Â | Â | Solid tumors | Phase 1b | 26 | Recruiting | NCT03206177 |
|  | SHR-1701 | Anti-PD-L1/TGF-βRII | Advanced colorectal cancer | Phase 2/3 | NA | Recruiting | CTR20210880 |
MMPs | Prinomastat | Pan-MMPs inhibitor | Advanced NSCLC | Phase 3 | 362 | Failure | NCT00004199 |
| Â | Tanomastat | Biphenyl MMP inhibitor | Advanced ovarian cancer | Phase 3 | 243 | Failure | NCIC-CTG trial OV12 |
| Â | Marimastat | Pan-MMPs inhibitor | Metastatic breast cancer | Phase 3 | 179 | Failure | ECOG-E2196 |
LOX | Simtuzumab | Neutralizing antibody of LOXL2 | Pancreatic cancer | Phase 2 | 240 | Failure | NCT01472198 |
| Â | Â | Â | Colorectal Adenocarcinoma | Phase 2 | 249 | Failure | NCT01479465 |
| Â | Tetrathiomolybdate | LOX inhibitor | Prostate Cancer | Phase 2 | 19 | Failure | NCT00150995 |
| Â | Â | Â | Esophageal cancer | Phase 2 | 69 | Well tolerated | NCT00176800 |
TRP | EC D-3263 HCl | TRPM8 agonist | Advanced solid tumors | Phase 1 | 23 | Completed | NCT00839631 |
| Â | SOR-C13 | TRPV6 antagonist | Advanced solid tumors | Phase 1 | 23 | Well tolerated | NCT01578564 |
| Â | Nabiximols | TRPV2 agonists | Recurrent glioblastoma | Phase 1b | 12 | Favorable prognosis | NCT01812616 |
Integrins | Cilengitide | αvβ3 and αvβ5 integrin inhibitor | Glioblastoma | Phase 3 | 545 | Failure | NCT00689221 |
|  | Abituzumab | αv integrin inhibitor | Prostate cancer | Phase 2 | 180 | Failure | NCT01360840 |
|  | Etaracizumab | Neutralizing antibody of αvβ3 integrin | Metastatic melanoma | Phase 2 | 112 | Failure | NCT00066196 |
Rho/ROCK | AT13148 | ROCK-AKT inhibitor | Solid tumors | Phase 1 | 51 | Failure | NCT01585701 |
FAK | Defactinib | FAK inhibitor | Advanced NSCLC | Phase 2 | 55 | Well tolerated | NCT01951690 |
| Â | Â | Â | Pleural Mesothelioma | Phase 2 | 344 | Failure | NCT01870609 |
| Â | Conteltinib | FAK inhibitor | Advanced NSCLC | Phase 1 | 60 | Favorable prognosis | NCT02695550 |
YAP/TAZ | Liposomal Verteporfin | YAP1 inhibitor | Glioblastoma | Phase 1/2 | 24 | Recruiting | NCT04590664 |
| Â | IAG933 | TEAD inhibitor | Solid Tumors | Phase 1 | 156 | Recruiting | NCT04857372 |
| Â | BPI-460372 | TEAD inhibitor | Solid Tumors | Phase 1 | 82 | Recruiting | NCT05789602 |