Table 1.
Representative drugs approved by the US FDA and other checkpoint inhibitors
| (Generic/Brand name) | Target | Mainly indication (Approved time) | Status |
|---|---|---|---|
| Aldesleukin | IL-2 receptor | Metastatic Melanoma (1998.1) Metastatic Renal Cell Carcinoma (mRCC) (1992.5) |
Approved |
| Ipilimumab/ Yervoy |
CTLA-4 | Metastatic Colorectal Cancer (mCC) (2018.7) Advanced Renal Cell Carcinoma (aRCC) (2018.4) Metastatic Melanoma (2017.7) Late-Stage Melanoma (2011.5) |
Approved |
| Nivolumab/ Opdivo | PD-1 | Hepatocellular Carcinoma (HCC) (2017.9) Metastatic Urothelial Carcinoma (mUC) (2017.2) Head and Neck Cancer (HNC) (2016.11) Hodgkin Lymphoma (HL) (2016.5) mRCC (2015.11) Advanced Melanoma (2014.12) |
Approved |
| Pembrolizumab/Keytruda | PD-1 | mSCLC (2019.6); Squamous Cell HNC (2019.6); aRCC (2019.4); NSCLC (2019.4); Advanced or Metastatic Merkel Cell Carcinoma (a/mMCC) (2018.12); HCC (2018.11); mNSCLC (2018.10) Primary Mediastinal Large B-Cell Lymphoma (PMBCL) (2018.6) Metastatic Cervical Cancer (mCC) (2018.6) Advanced or Metastatic Gastric Cancer (2017.9) Advanced or Metastatic UC (2017.5); HL (2017.3); mNSCLC (2016.10) Advanced Melanoma (2014.9) |
Approved |
| Cemiplimab/ Libtayo | PD-1 | Squamous Cell Carcinoma (2018.9) | Approved |
| toripalimab | PD-1 | Advanced or Metastatic Melanoma | Phase 2 |
| Atezolizumab/ Tecentriq |
PD-L1 | Extensive-Stage SCLC (2019.3) Metastatic Triple-Negative Breast Cancer (mTNBC) (2019.3.) Metastatic Non-Squamous NSCLC (2018.12) Advanced Bladder Cancer (2017.4) Metastatic Lung Cancer (2016.10) Urothelial Carcinoma(2016.5) |
Approved |
| Avelumab/ Bavencio | PD-L1 | Advanced Renal Cell Carcinoma (2019.5) Urothelial Carcinoma (2017.5) Merkel Cell Carcinoma (2017.3) |
Approved |
| Durvalumab/ Imfinzi |
PD-L1 | Non-Small Cell Lung Cancer (2018.2) Urothelial Carcinoma (2017.3) |
Approved |
| MEDI4736 | PD-L1 | NSCLC | Phase 3a |
| Avelumab | PD-L1 | Ovarian Cancer | Phase 2 |
| Tisagenlecleucel/Kymriah | CD19 | Large B-Cell Lymphoma (2018.5) Acute Lymphoblastic Leukemia (2017.8) |
Approved |
| Axicabtagene ciloleucel/ Yescarta |
CD19 | Large B-Cell Lymphoma (2017.10) | Approved |
| Cyclophosphamide | CD19 | Lymphocytic Leukemia | Phase 1 |
| Sym023 | TIM-3 | Metastatic Cancer; Solid Tumor; Lymphoma | Phase 1 |
| TSR-022 | TIM-3 | Advanced or Metastatic Solid Tumors | Phase 1 |
| MEDI6469 | TNFRSF4 | Head and Neck Cancer; Progressive Metastatic Prostate Cancer | Phase 1 |
| KHK4083 | TNFRSF4 | B-Cell Non-Hodgkin Lymphoma | Phase 2 |
| PF-04518600 | TNFRSF4 | Metastatic Renal Cell Cancer | Phase 2 |
| Sym022 | LAG-3 | Advanced Solid Tumor Malignancies or Lymphomas | Phase 1 |
| BMS 986016 | LAG-3 | Gliosarcoma and Recurrent Brain Neoplasm | Phase 1 |