Table 1.
Table summarizing the 15 compounds under development for blockade of LAG-3.
| Name (Code) | Company | Format | Tumor Type | Study Phase | National Clinical Trial nr. | Combined with |
|---|---|---|---|---|---|---|
| PRS-332 | Pieris Pharmaceuticals | LAG-3xPD-1 bispecific fusion protein | Solid | preclinical | / | / |
| P13B02-3 | Agenus | IgG1 | Solid | preclinical | / | (PD-1) |
| LBL-007 | Nanjing Leads Biolabs | scFv—IgG4 fusion | Solid | preclinical | / | (mouse PD-1) BE0146 BioXcell |
| Eftilagimod alpha (IMP321) | Immutep | LAG-3 IgG1 Fc fusion protein | Solid, NSCLC, HNSCC, Breast, Melanoma | I & II | 03252938, 00351949, 00349934, 02676869, 03625323, 02614833 | (PD-L1) Avelumab antibody, (PD-1) Pembrolizumab antibody |
| LAG525 (IMP701) | Novartis/Prima Biomed | Humanized IgG4 | Solid (advanced) | I/II & II | 02460224, 03365791 | (PD-1) Spartalizumab antibody |
| MK-4280 | Merck Sharp & Dohme | Humanized IgG4 | Hematological | I/II | 03598608 | (PD-1) pembrolizumab (MK-3475) antibody |
| REGN3767 | Regeneron Pharmaceuticals | hinge-stabilized IgG4 | Solid (advanced) | I | 03005782 | (PD-1) Cemiplimab (REGN2810) |
| Relatlimab (BMS-986016) | Bristol-Myers Squibb | Human IgG4 | Melanoma, Hematological, Glioblastoma, Kidney, Lungs, Colon | I, I/Iia, II & II/III | 02658981, 03335540, 02966548, 02061761, 01968109, 03459222, 02488759, 02996110, 02935634, 02750514, 02060188, 03470922 | (PD-1) Nivolumab (BMS-936558) antibody |
| BI 754111 | Boehringer Ingelheim | Humanized IgG4 | HN, NSCLC, Solid (metatstatic) |
I & II | 03964233, 03697304 | (PD-1) BI 754091 antibody, (VEGF/Ang2) BI 836880 bispecific nanobody |
| FS118 | F-star Therapeutics | LAG-3 x PD-L1 tetravalent bispecific IgG1 antibody | Solid (advanced & metatstatic) | I | 03440437 | / |
| Tebotelimab (MGD013) | MacroGenics | LAG-3 × PD-1 bispecific IgG4k antibody | Solid, Cholangiocarcinoma, Liver, Gastric (HER-2+), Breast (HER-2+), Oesophageal, Haematological | I | 03219268 | (HER2) Margetuximab |
| TSR-033 | Tesaro | Humanized IgG4 | Solid (advanced) | I | 03250832 | (Tim-3) TSR-022 antibody, (PD-1) dostarlimab (TSR-042) antibody, (VEGF-a) Bevacizumab antibody, mFOLFOX6, FOLFIRI |
| INCAGN2385 | Incyte | t.b.a. | Solid, Melanoma | I | 04370704 | / |
| Sym022 | Symphogen | Human Fc-inert | Solid, Lymphoma | I | 03311412, 03489369 | (PD-1) Sym021 antibody, (Tim-3) Sym023 antibody |
| XmAb22841 | Xencor | LAG-3 x CTLA-4 bispecific Fc-inert antibody | Solid | I | 03849469 | (PD-1) Pembrolizumab antibody |
Abbreviations: Ang2, angiotensin 2; CTLA-4, cytotoxic T lymphocyte-associated protein 4; Fc, fragment crystallizable; HER, human epidermal growth factor receptor; HN, head and neck cancer; Ig, immunoglobulin; NSCLC, non-small-cell lung cancer; PD-1, programmed death 1; PD-L1, programmed death-ligand 1; scFv, single-chain variable fragment; t.b.a., to be announced; TIM-3, T-cell immunoglobulin and mucin domain-3; VEGF, vascular endothelial growth factor; nr.; number.