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 |
| Bladder cancer | Phase 2 | 25 | Recruiting | NCT04917809 | |||
| Advanced solid tumors | Phase 2a | 35 | Recruiting | NCT02699606 | |||
| Prostate cancer | Phase 2 | 9 | poorly tolerated | ACTRN12618001061224 | |||
| Advanced NSCLC | Phase 2 | 22 | Completed | NCT03827850 | |||
| TGF-β | Fresolimumab | Neutralizing antibody of TGF-β | Metastatic Breast Cancer | Phase 2 | 23 | Favorable prognosis | NCT01401062 |
| Malignant pleural mesothelioma | Phase 2 | 13 | Favorable prognosis | NCT01112293 | |||
| Galunisertib | TGF-β receptor kinase inhibitor | Solid tumors | Phase 1b/2 | 170 | Favorable prognosis | NCT01373164 | |
| Solid tumors | Phase 1b/2 | 25 | Well tolerated | NCT02423343 | |||
| Hepatocellular Carcinoma | Phase 2 | 47 | Favorable prognosis | NCT01246986 | |||
| 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 |
| Tanomastat | Biphenyl MMP inhibitor | Advanced ovarian cancer | Phase 3 | 243 | Failure | NCIC-CTG trial OV12 | |
| 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 |
| Colorectal Adenocarcinoma | Phase 2 | 249 | Failure | NCT01479465 | |||
| Tetrathiomolybdate | LOX inhibitor | Prostate Cancer | Phase 2 | 19 | Failure | NCT00150995 | |
| Esophageal cancer | Phase 2 | 69 | Well tolerated | NCT00176800 | |||
| TRP | EC D-3263 HCl | TRPM8 agonist | Advanced solid tumors | Phase 1 | 23 | Completed | NCT00839631 |
| SOR-C13 | TRPV6 antagonist | Advanced solid tumors | Phase 1 | 23 | Well tolerated | NCT01578564 | |
| 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 |
| Pleural Mesothelioma | Phase 2 | 344 | Failure | NCT01870609 | |||
| Conteltinib | FAK inhibitor | Advanced NSCLC | Phase 1 | 60 | Favorable prognosis | NCT02695550 | |
| YAP/TAZ | Liposomal Verteporfin | YAP1 inhibitor | Glioblastoma | Phase 1/2 | 24 | Recruiting | NCT04590664 |
| IAG933 | TEAD inhibitor | Solid Tumors | Phase 1 | 156 | Recruiting | NCT04857372 | |
| BPI-460372 | TEAD inhibitor | Solid Tumors | Phase 1 | 82 | Recruiting | NCT05789602 |
NCIC-CTG trial Standard National Cancer Institute of Canada-Clinical Trials Group, ECOG-E2196 Eastern Cooperative Oncology Group trial E2196, ACTRN Australian New Zealand Clinical Trials Registry, CTR China drug trials