Table 1

Principal LAG-3 checkpoint Inhibitors in clinical trials

DrugDescriptionTumour typeCombination(s) with
Human IgG4Melanoma, hepatocellular, sarcoma, chordoma, head and neck, mismatch repair deficiency and basal cell carcinomaNivolumab (anti-PDL1) and ipilimumab (anti-CTLA4)
Sym022Fc-inert monoclonal antibodySolid tumours and lymphomaSym021* (anti-PD1)
Eftilagimod alpha
LAG-3 fused to Fc region of IgG1Non-small cell lung cancer, head and neck, melanoma, renal, pancreas, breast and solid tumoursPembrolizumab (anti-PDL1), avelumab (anti-PD1) and gemcitabine (cytotoxic chemotherapy)
(LAG 525/IMP-701)
Humanised IgG4Melanoma, breast cancer, haematological cancers and solid tumoursSpartalizumab* (anti-PD1), carboplatin (cytotoxic chemotherapy), NIR178* (AA2a inhibitor), capmatinib (MET inhibitor), lacnotuzumab*
(CSF-1) and canakinumab (anti-IL1β)
Humanised IgG4Renal cell carcinoma, non-small cell lung cancer, lymphoma and solid tumoursPembrolizumab (anti-PDL1), lenvatinib (anti-VEGF), irinotecan (cytotoxic chemotherapy), 5-flurouracil (cytotoxic chemotherapy) and oxaliplatin (cytotoxic chemotherapy
REGN-3767Humanised IgG4Breast cancer and solid tumoursCemplimab (anti-PD1)
BI-754111Humanised IgG4Head and Neck cancer, non-small cell lung cancer and solid cancersBI 754091* (anti-PD-1)
FS-118Tetravalent bispecific antibody (PD-L1 and LAG-3) IgG1Head and Neck cancer and solid cancersNone
Bispecific antibody (PD-L1 and LAG-3) IgG4kHepatocellular carcinoma, melanoma, gastric cancer, gastro-oesophageal cancer, breast cancer, biliary tract cancer, head and neck cancer, endometrial and solid cancersBrivanib alaninate* (anti-VEGF), niraparib (PARP inhibitor), margetuximab (anti-HER2), enobiltuzumab* (anti-B7H3)
TSR-033Humanised IgG4Colorectal cancer and solid cancersDostarlimab (anti-PDL1), bevacizumab (anti-VEGF), irinotecan (cytotoxic chemotherapy, 5-flurouracil (cytotoxic chemotherapy) and oxaliplatin (cytotoxic chemotherapy
INCAGN2385Fc-engineered IgG1κSolid cancersNone
XmAb22841Bispecific antibody (CTLA-4 and LAG-3)Solid cancersPembrolizumab (anti-PDL1)
EMB-02Bispecific antibody (PD-1 and LAG-3)Solid cancersNone
GSK2831781Humanised IgG1Ulcerative colitis and psoriasisNone
  • *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.