|
| Inhibitors/antibodies | Molecular targets | Phases of development | References |
|
| CAFs |
| PT630 (FAP inhibitor) | FAP-α | Preclinical | [5] |
| NK4 (anti-HGF monoclonal antibody) | HGF/MET | Preclinical | [6] |
| AMG337 (MET kinase inhibitor) | MET | Preclinical | [7] |
| Rebimastat (MMP inhibitor) | MMPs | Phase II clinical trial | NCT00040755 |
| AMD3100 (CXCR4 antagonist) | SDF-1/CXCR4 | Preclinical | [8] |
| GC1008 (anti-TGF-β monoclonal antibody) | TGF-β | Phase II clinical trial | NCT01401062 |
|
| Tumor vasculatures |
| Sorafenib (tyrosine kinase inhibitor) | VEGFRs, PDGFRs, KIT | FDA-approved | NDA021923 |
| Sunitinib (tyrosine kinase inhibitor) | VEGFRs, PDGFRs, KIT | FDA-approved | NDA021938 |
| MK0752 (γ-secretase inhibitor) | γ-secretase | Phase I clinical trial | NCT00106145 |
| OMP21M18 (anti-DLL4 monoclonal antibody) | DLL4 | Phase I clinical trial | NCT01189968 |
| OMP52M51 (anti-Notch1 monoclonal antibody) | Notch1 | Phase I clinical trial | NCT01778439 |
|
| TAMs |
| PLX3397 (CSF-1R inhibitor) | CSF-1R | Phase I/II clinical trial | NCT01596751 |
| AMG820 (anti-CSF-1R monoclonal antibody) | CSF-1R | Phase I/II clinical trial | NCT02713529 |
| Zoledronate, clodronate, ibandronate | Deplete macrophages | Phase III clinical trial | NCT00127205 |
| NCT00009945 |
| 852A (TLR7 agonist) | TLR7 | Phase II clinical trial | NCT00319748 |
| Imiquimod (TLR7 agonist) | TLR7 | Phase II clinical trial | NCT00899574 |
| NCT00821964 |
|
| MDSCs |
| Tadalafil (PDE-5 inhibitors) | PDE-5 | Pilot study | NCT00843635 |
| Phase II clinical trial | NCT00752115 |
| NCX4016 (Nitric oxide-releasing aspirin derivative) | iNOS and arginase | Phase I clinical trial | NCT00331786 |
| (Prevention purpose) |
| L-NAME (arginase inhibitor) | Arginase | Preclinical | [9] |
| All-trans retinoic acid | Inducing MDSC differentiation | Phase II clinical trial | NCT00617409 |
|
| Treg cells |
| MEDI6383 (OX40 agonist) | OX40 | Phase I clinical trial | NCT02221960 |
| Ipilimumab (anti-CTLA4 monoclonal antibody) | CTLA4 | FDA-approved | BLA125377 |
|
| Hypoxia |
| TH-302 (hypoxia-activated prodrug) | Hypoxia | Phase III clinical trial | NCT01746979 |
| AQ4N (hypoxia-activated prodrug) | Hypoxia | Phase I/II clinical trial | NCT00394628 |
|
| ECM |
| PEGPH20 (recombinant hyaluronidase) | Hyaluronan | Phase II clinical trial | NCT01839487 |
| Phase III clinical trial | NCT02715804 |
|
