Table 2.
Clinical trials with toll-like receptor (TLR) agonists for macrophages reprogramming.
| Target | Drugs | Inhibitor type | Clinical trial | Tumor type | Benefit |
|---|---|---|---|---|---|
| CD40 | APX005M | mAb |
NCT03502330 (2018) (Recruiting) NCT02482168 (2015) (Active, not recruiting) NCT03123783 (2017) (Recruiting)NCT03389802 (2018) (Recruiting) NCT03165994 (2017) (Recruiting) |
Non-small Cell Lung Cancer, Renal Cell Carcinoma Solid tumors Non-small Cell Lung Cancer or Metastatic Melanoma Pediatric CNS Tumors Resectable Esophageal and Gastroesophageal Junction Cancers |
Unknown |
| Selicrelumab | mAb | NCT02304393 (2014) (Recruiting) | Locally Advanced and/or Metastatic Solid Tumors | Unknown | |
| ChiLob 7/4 | mAb | NCT01561911 (2012) (Completed) | Non-Hodgkin Lymphoma | Unknown | |
| CP-870,893 | mAb | NCT00607048 (Completed) | Non-Hodgkin Lymphoma | Unknown | |
| CDX-1140 | Small molecule | NCT03329950 (Recruiting) | Advanced Malignancies | Unknown | |
| TLR7 | LHC165 | Small molecule | NCT03301896 (2017) (Recruiting) | Advanced Malignancies | Unknown |
| Imiquimod | Small molecule |
NCT01421017 (2011) (Completed) NCT00899574 (2009) (Completed with results) |
Breast Cancer With Skin Metastases Chest Wall Recurrence or Skin Metastases |
Well tolerated. Partial response: tumor regression and immune response | |
| NKTR-262 | Small molecule | NCT03435640 (2018) (Recruiting) | Locally Advanced or Metastatic Solid Tumor Malignancies | Unknown | |
| IMO-8400 | Small molecule | NCT02252146, (Completed with results) | Diffuse Large B Cell Lymphoma (DLBCL) | Lack of efficacy | |
| Resiquimod | Small molecule | NCT00821652 (2009) (Completed) | Surgically resected Stage IIB, IIC, Stage III or Stage IV (AJCC criteria) Melanoma | Unknown | |
| DSP-0509 | Small molecule | NCT03416335 (2018) (Recruiting) | Advanced Solid Tumors | Unknown | |
| TLR8 | VTX-2337 | Small molecule |
NCT02431559 (2015) (Completed) NCT01294293, (Completed) NCT01334177, (Completed) NCT02452697 (2015) (Recruiting) |
Platinum-Resistant Ovarian Cancer Ovarian Epithelial, Fallopian Tube, or Peritoneal Cavity Cancer Ovarian Epithelial, Fallopian Tube, or Peritoneal Cavity Cancer Myeloid and Lymphoid Malignancies |
Unknown |
| TLR9 | EMD 1201081 | Small molecule | NCT01040832 (2009) (Completed with results) | Recurrent or Metastatic Squamous Cell Carcinoma of the Head and Neck | EMD 1201081 was well tolerated in combination with cetuximab, but no clinical efficacy was observed Ruzsa et al., 2014 |
| DUK-CPG-001 | Small molecule | NCT02452697 (2015) (Recruiting) | Myeloid and Lymphoid Malignancies | Unknown | |
| IMO-2055 | Small molecule |
NCT00719199 (2008) (Completed) NCT00633529 (2008) (Completed) |
Colorectal Cancer NSCLC |
Unknown | |
| CMP-001 | Small molecule |
NCT03618641 (2018) (Recruiting) NCT03507699 (2018) (Recruiting) |
Stage IIIB/C/D Melanoma Patients With Clinically Apparent Lymph Node Disease Metastatic Colorectal Cancer |
Unknown | |
| SD-101 | Small molecule |
NCT03007732 (2017) (Recruiting) NCT03410901 (Recruiting) NCT02927964 (2016) (Recruiting) NCT02254772 (2014) (Completed with results) |
Hormone-Naïve Oligometastatic Prostate Cancer Low-Grade B-Cell Non-Hodgkin Lymphoma Refractory Grade 1-3A Follicular Lymphoma Recurrent Low-Grade B-Cell Lymphoma |
Well tolerated but progression of the tumor was observed |