Table 1.
List of ICIs, approval year, mechanism of action and current clinical indications.
| Drug | Year approved | Mechanism of action | Target | Indications |
|---|---|---|---|---|
| Pembrolizumab (Keytruda) | 2014 | A mAb that binds to the PD-1 receptor and blocks its interaction with PD-L1 and PD-L2, releasing PD-1 pathway-mediated inhibition of the immune response leading to T cell proliferation and cytokine production. | PD-1 | Melanoma NSCLC HNSCC cHL PMBCL Urothelial carcinoma Microsatellite instability-high cancer Gastric cancer Cervical cancer HCC |
| Nivolumab (Opdiv) | 2014 | A mAb that binds to the PD-1 receptor and blocks its interaction with PD-L1 and PD-L2, releasing PD-1 pathway-mediated inhibition of the immune response leading to T cell proliferation and cytokine production. | PD-1 | Metastatic melanoma NSCLC Advanced RCC cHL HNSCC Urothelial carcinoma Metastatic colorectal cancer HCC |
| Atezolizumab (Tecentriq) | 2016 | A mAb that binds to PD-L1 and blocks its interaction with both PD1 and B7.1 receptors, which suppresses T-cell activity and cytokine production. | PD-L1 | Metastatic urothelial carcinoma NSCLC |
| Avelumab (Bavencio) | 2017 | A mAb that binds to PD-L1 and blocks its interaction with both PD1 and B7.1 receptors, which suppresses T-cell activity and cytokine production. | PD-L1 | Metastatic Merkel cell carcinoma Metastatic urothelial carcinoma |
| Durvalumab (Imfinzi) | 2017 | A mAb that binds to PD-L1 and blocks its interaction with both PD1 and B7.1 receptors, which suppresses T-cell activity and cytokine production. | PD-L1 | Metastatic urothelial carcinoma NSCLC |
| Ipilimumab (Yervoy) | 2011 | A mAb that binds to CTLA-4 and blocks interaction of CTLA-4 with its ligands CD80/CD86. Blockade of CTLA-4 has been shown to augment T-cell activation and proliferation, including the activation and proliferation of tumor infiltrating T-effector cells. | CTLA-4 | Metastatic melanoma |
ICIs: immune checkpoint inhibitors; mAb: monoclonal antibody; PD-1: programmed cell death 1; PD-L1: programmed cell death ligand 1; PD-L2: programmed cell death ligand 2; NSCLC: non-small-cell lung cancer; HNSCC: head and neck squamous cell carcinoma; cHL: classical Hodgkin lymphoma; PMBCL: primary mediastinal B-cell lymphoma; HCC: hepatocellular carcinoma; RCC: renal cell carcinoma; CTLA-4: cytotoxic T lymphocyte associated antigen 4; CD: cluster of differentiation.