Principal LAG-3 checkpoint Inhibitors in clinical trials
| Drug | Description | Tumour type | Combination(s) with |
| Relatlimab (BMS-986016) | Human IgG4 | Melanoma, hepatocellular, sarcoma, chordoma, head and neck, mismatch repair deficiency and basal cell carcinoma | Nivolumab (anti-PDL1) and ipilimumab (anti-CTLA4) |
| Sym022 | Fc-inert monoclonal antibody | Solid tumours and lymphoma | Sym021* (anti-PD1) |
| Eftilagimod alpha (IMP-321) | LAG-3 fused to Fc region of IgG1 | Non-small cell lung cancer, head and neck, melanoma, renal, pancreas, breast and solid tumours | Pembrolizumab (anti-PDL1), avelumab (anti-PD1) and gemcitabine (cytotoxic chemotherapy) |
| Leramilimab (LAG 525/IMP-701) | Humanised IgG4 | Melanoma, breast cancer, haematological cancers and solid tumours | Spartalizumab* (anti-PD1), carboplatin (cytotoxic chemotherapy), NIR178* (AA2a inhibitor), capmatinib (MET inhibitor), lacnotuzumab* (CSF-1) and canakinumab (anti-IL1β) |
| Favezelimab (MK-4280) | Humanised IgG4 | Renal cell carcinoma, non-small cell lung cancer, lymphoma and solid tumours | Pembrolizumab (anti-PDL1), lenvatinib (anti-VEGF), irinotecan (cytotoxic chemotherapy), 5-flurouracil (cytotoxic chemotherapy) and oxaliplatin (cytotoxic chemotherapy |
| REGN-3767 | Humanised IgG4 | Breast cancer and solid tumours | Cemplimab (anti-PD1) |
| BI-754111 | Humanised IgG4 | Head and Neck cancer, non-small cell lung cancer and solid cancers | BI 754091* (anti-PD-1) |
| FS-118 | Tetravalent bispecific antibody (PD-L1 and LAG-3) IgG1 | Head and Neck cancer and solid cancers | None |
| Tebotelimab (MGD-013) | Bispecific antibody (PD-L1 and LAG-3) IgG4k | Hepatocellular carcinoma, melanoma, gastric cancer, gastro-oesophageal cancer, breast cancer, biliary tract cancer, head and neck cancer, endometrial and solid cancers | Brivanib alaninate* (anti-VEGF), niraparib (PARP inhibitor), margetuximab (anti-HER2), enobiltuzumab* (anti-B7H3) |
| TSR-033 | Humanised IgG4 | Colorectal cancer and solid cancers | Dostarlimab (anti-PDL1), bevacizumab (anti-VEGF), irinotecan (cytotoxic chemotherapy, 5-flurouracil (cytotoxic chemotherapy) and oxaliplatin (cytotoxic chemotherapy |
| INCAGN2385 | Fc-engineered IgG1κ | Solid cancers | None |
| XmAb22841 | Bispecific antibody (CTLA-4 and LAG-3) | Solid cancers | Pembrolizumab (anti-PDL1) |
| EMB-02 | Bispecific antibody (PD-1 and LAG-3) | Solid cancers | None |
| GSK2831781 | Humanised IgG1 | Ulcerative colitis and psoriasis | None |
*Investigational drug not approved by the United States Food and Drug Administration (FDA) or European Medicines Agency (EMA) at date of censoring.
AA2a, adenosine A2a receptor antagonist; anti-B7H3, humanised antibody targeting B7-H3; anti-IL1β, anti-interleukin 1β antibod; Anti-PDL1, anti-programmed cell death-ligand one antibody; CSF-1, colony-stimulating factor 1 antibody; CTLA4, cytotoxic T-lymphocyte-associated protein 4; HER2, human epidermal growth factor 2 antibody; LAG-3, lymphocyte-activation gene 3; MET inhibitor, c-MET tyrosine kinase inhibitor; PARP, Poly adenosine diphosphate ribose polymerase inhibitor; VEGF, vascular endothelial growth factor tyrosine kinase inhibitor.