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| Stem definition | Drug id | CAS RN |
|---|---|---|
| monoclonal antibodies | 5514 | 1673516-98-7 |
| Molecule | Description |
|---|---|
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Synonyms:
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Relatlimab is a human IgG4 monoclonal antibody that binds to the LAG-3 receptor, blocks interaction with its ligands, including MHC II, and reduces LAG-3 pathway-mediated inhibition of the immune response. Antagonism of this pathway promotes T cell proliferation and cytokine secretion. Binding of the PD-1 ligands, PD-L1 and PD-L2, to the PD-1 receptor found on T cells, inhibits T-cell proliferation and cytokine production. Upregulation of PD-1 ligands occurs in some tumors, and signaling through this pathway can contribute to inhibition of active T-cell immune surveillance of tumors. Nivolumab is a human IgG4 monoclonal antibody that binds to the PD-1 receptor, blocks interaction with its ligands PD-L1 and PD-L2, and reduces PD-1 pathwaymediated inhibition of the immune response, including the anti-tumor immune response. In syngeneic mouse tumor models, blocking PD-1 activity resulted in decreased tumor growth. The combination of nivolumab (anti-PD-1) and relatlimab (anti-LAG-3) results in increased T-cell activation compared to the activity of either antibody alone. In murine syngeneic tumor models, LAG-3 blockade potentiates the anti-tumor activity of PD-1 blockage, inhibiting tumor growth and promoting tumor regression.
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| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 18, 2022 | FDA | BRISTOL MYERS SQUIBB | |
| Sept. 15, 2022 | EMA | BRISTOL-MYERS SQUIBB PHARMA EEIG |
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| Source | Code | Description |
|---|---|---|
| ATC | L01FY02 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES Combinations of monoclonal antibodies and antibody drug conjugates |
| MeSH PA | D000074322 | Antineoplastic Agents, Immunological |
| MeSH PA | D000082082 | Immune Checkpoint Inhibitors |
| MeSH PA | D000970 | Antineoplastic Agents |
| FDA MoA | N0000194002 | Lymphocyte Activation Gene-3 Antagonists |
| FDA EPC | N0000194003 | Lymphocyte Activation Gene-3 Blocker |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Unresectable or metastatic melanoma | indication | 443493003 | |
| Advanced melanoma with tumour cell PD-L1 expression below 1% | indication | 443493003 |
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| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Lymphocyte activation gene 3 protein | Tumour-associated antigen | ANTAGONIST | Kd | 9.92 | DRUG LABEL | DRUG LABEL |
| ID | Source |
|---|---|
| CHEBI:756524 | CHEBI |
| CHEMBL3990044 | ChEMBL_ID |
| C000721227 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9536 | IUPHAR_LIGAND_ID |
| DB14851 | DRUGBANK_ID |
| 42656311000001103 | SNOMEDCT_US |
| 4041299 | VANDF |
| 4041300 | VANDF |
| C4724799 | UMLSCUI |
| D11350 | KEGG_DRUG |
| 10735 | INN_ID |
| 357919 | MMSL |
| 40561 | MMSL |
| d09869 | MMSL |
| 018998 | NDDF |
| AF75XOF6W3 | UNII |
| 2596772 | RXNORM |
| C000729737 | MESH_SUPPLEMENTAL_RECORD_UI |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| OPDUALAG | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0003-7125 | INJECTION | 4 mg | INTRAVENOUS | BLA | 28 sections |