efzofitimod

Home
Ligands
efzofitimod

GtoPdb Ligand ID: 13199

Synonyms: ATYR-1923 | ATYR1923 | KRP-R120

Compound class: Peptide or derivative

Comment: Efzofitimod (ATYR1923) is a Fc fusion protein [1]. The C-terminal 59 amino acids corresponds to the active N-terminal domain of histidyl-tRNA synthetase (HARS), an extracellular non-catalytic isoform that is upregulated by inflammatory cytokine stimulation in the lung. The IgG1 Fc domain extends the peptide's circulating half-life. The HARS domain binds selectively to the cell surface receptor neuropilin 2 (NRP2; O60462, which is an immunomodulatory protein and molecular target for inflammatory diseases [5]. In the airways, NRP2 plays an important role in activation of myeloid cells and their recruitment to inflammatory sites [3]. Efzofitimod was developed as a clinical candidate immunotherpy with potential for immune-mediated fibrotic lung conditions.

References
1. Baughman RP, Niranjan V, Walker G, Burkart C, Paz S, Chong Y, Siefker D, Sun E, Nangle L, Forster S et al.. (2023) Efzofitimod: a novel anti-inflammatory agent for sarcoidosis. Sarcoidosis Vasc Diffuse Lung Dis, 40 (1): e2023011. [PMID:36975051]
2. Culver DA, Aryal S, Barney J, Hsia CCW, James WE, Maier LA, Marts LT, Obi ON, Sporn PHS, Sweiss NJ et al.. (2023) Efzofitimod for the Treatment of Pulmonary Sarcoidosis. Chest, 163 (4): 881-890. [PMID:36356657]
3. Immormino RM, Lauzier DC, Nakano H, Hernandez ML, Alexis NE, Ghio AJ, Tilley SL, Doerschuk CM, Peden DB, Cook DN et al.. (2018) Neuropilin-2 regulates airway inflammatory responses to inhaled lipopolysaccharide. Am J Physiol Lung Cell Mol Physiol, 315 (2): L202-L211. [PMID:29671604]
4. Ishitoku M, Mokuda S, Araki K, Watanabe H, Kohno H, Sugimoto T, Yoshida Y, Sakaguchi T, Masumoto J, Hirata S et al.. (2023) Tumor Necrosis Factor and Interleukin-1β Upregulate NRP2 Expression and Promote SARS-CoV-2 Proliferation. Viruses, 15 (7). [PMID:37515185]
5. Roy S, Bag AK, Singh RK, Talmadge JE, Batra SK, Datta K. (2017) Multifaceted Role of Neuropilins in the Immune System: Potential Targets for Immunotherapy. Front Immunol, 8: 1228. [PMID:29067024]

References

1. Baughman RP, Niranjan V, Walker G, Burkart C, Paz S, Chong Y, Siefker D, Sun E, Nangle L, Forster S et al.. (2023)
Efzofitimod: a novel anti-inflammatory agent for sarcoidosis.
Sarcoidosis Vasc Diffuse Lung Dis, 40 (1): e2023011. [PMID:36975051]

2. Culver DA, Aryal S, Barney J, Hsia CCW, James WE, Maier LA, Marts LT, Obi ON, Sporn PHS, Sweiss NJ et al.. (2023)
Efzofitimod for the Treatment of Pulmonary Sarcoidosis.
Chest, 163 (4): 881-890. [PMID:36356657]

3. Immormino RM, Lauzier DC, Nakano H, Hernandez ML, Alexis NE, Ghio AJ, Tilley SL, Doerschuk CM, Peden DB, Cook DN et al.. (2018)
Neuropilin-2 regulates airway inflammatory responses to inhaled lipopolysaccharide.
Am J Physiol Lung Cell Mol Physiol, 315 (2): L202-L211. [PMID:29671604]

4. Ishitoku M, Mokuda S, Araki K, Watanabe H, Kohno H, Sugimoto T, Yoshida Y, Sakaguchi T, Masumoto J, Hirata S et al.. (2023)
Tumor Necrosis Factor and Interleukin-1β Upregulate NRP2 Expression and Promote SARS-CoV-2 Proliferation.
Viruses, 15 (7). [PMID:37515185]

5. Roy S, Bag AK, Singh RK, Talmadge JE, Batra SK, Datta K. (2017)
Multifaceted Role of Neuropilins in the Immune System: Potential Targets for Immunotherapy.
Front Immunol, 8: 1228. [PMID:29067024]