PD-1 and PD-L1 Inhibitor Drugs in Cancer Treatment
The FDA-approved PD-1 inhibitors are pembrolizumab, nivolumab, cemiplimab, and dostarlimab; the PD-L1 inhibitors are atezolizumab, avelumab, and durvalumab. 1
PD-1 Inhibitors
Currently Approved Agents
- Pembrolizumab (Keytruda, Merck) - FDA-approved PD-1 inhibitor used across multiple cancer types including melanoma, NSCLC, urothelial carcinoma, and gastric cancer 1, 2
- Nivolumab (Opdivo, Bristol Myers Squibb) - FDA-approved PD-1 inhibitor indicated for melanoma, NSCLC, renal cell carcinoma, urothelial carcinoma, and other malignancies 1, 3
- Cemiplimab (Libtayo, Sanofi) - PD-1 inhibitor approved for cutaneous squamous cell carcinoma and other indications 1
- Dostarlimab (Jemperli, GSK) - PD-1 inhibitor with particular utility in MSI-H/dMMR tumors 1
Subcutaneous Formulation
- Nivolumab and hyaluronidase-nvhy is available as a subcutaneous injection that may substitute for IV nivolumab in monotherapy settings, but is not approved for concurrent use with ipilimumab 1
PD-L1 Inhibitors
Currently Approved Agents
- Atezolizumab (Tecentriq, Genentech) - FDA-approved PD-L1 inhibitor used in NSCLC, urothelial carcinoma, and other cancers 1
- Avelumab (Bavencio, Merck KGaA) - PD-L1 inhibitor approved for urothelial carcinoma and Merkel cell carcinoma 1
- Durvalumab (Imfinzi, AstraZeneca) - PD-L1 inhibitor indicated for NSCLC consolidation therapy and urothelial carcinoma 1
Additional Context on Mechanism
These agents work by blocking the PD-1/PD-L1 immune checkpoint axis. PD-1 is a cell surface receptor on activated T cells that negatively regulates immune function, while PD-L1 is expressed on tumor cells and antigen-presenting cells 4. The interaction between PD-1 and PD-L1 inhibits T-cell-mediated tumor cell death, allowing cancer cells to evade immune surveillance 4. Blocking this interaction with checkpoint inhibitor antibodies restores T cell activation and enables immune-mediated killing of cancer cells 5, 4.
CTLA-4 Inhibitor (For Combination Therapy)
- Ipilimumab (Yervoy, Bristol Myers Squibb) - CTLA-4 inhibitor that blocks a different immune checkpoint and is frequently used in combination with PD-1 inhibitors, particularly nivolumab, for enhanced efficacy in melanoma and other cancers 1, 3
Emerging Agent
- Tislelizumab-jsgr - A newer PD-1 inhibitor approved for gastric cancer with PD-L1 CPS ≥1 1