IAXO-101 (CD14/TLR4 Antagonist) (synthetic)

[1] Glycolipids and benzylammonium lipids as novel antisepsis agents: synthesis and biological characterization. Piazza M, et al. J. Med. Chem. (2009); 52:1209
[2] Glia TLR4 receptor as new target to treat neuropathic pain: efficacy of a new receptor antagonist in a model of peripheral nerve injury in mice. Bettoni I, et al. Glia (2008); 56:1312
[3] Inhibition of lipid a stimulated activation of human dendritic cells and macrophages by amino and hydroxylamino monosaccharides. 
Peri F, et al. Angew .Chem. (2007); 46:3308
[4] Evidence of a specific interaction between new synthetic antisepsis agents and CD14. Piazza M, et al. Biochemistry (2009); 48:12337
[5] Therapeutic targeting of innate immunity with Toll-like receptor 4 (TLR4) antagonists. Peri F, Piazza M. Biotechnol. Adv. (2012); 30:251 REVIEW
[6] Synthetic molecules and functionalized nanoparticles targeting the LPS-TLR4 signaling: A new generation of immunotherapeutics. Peri F, Calabrese V, Piazza M, Cighetti R.Pure Appl. Chem. (2012); 84:97 REVIEW
[7] Inhibition of the cluster of differentiation 14 innate immunity pathway with IAXO-101 improves chronic microelectrode performance. Hermann JK., et al. J Neural Eng (2017) [Epub ahead of print] PubMed Abstract
[8] A small-molecule TLR4 antagonist reduced neuroinflammation in female E4FAD mice. Balu, D., Valencia-Olvera, A.C., Nguyen, A. et al. Alz Res Therapy 15, 181 (2023). https://doi.org/10.1186/s13195-023-01330-6 Abstract
 

IAXO-102 (CD14/TLR4 Antagonist) (synthetic)

[1] TLR4 receptor as new target to treat neuropathic pain: efficacy of a new receptor antagonist in a model of peripheral nerve injury in mice. Bettoni I, et al. Glia (2008); 56:1312
[2] Exploring the LPS/TLR4 signal pathway with small molecules. Peri F, et al.; Biochem Soc Trans. (2010); 38:1390 REVIEW
[3] Toll like receptor 4 antagonist prevents acetaminophen induced acute liver failure in mice: a novel therapeutic strategy. Shah N, et al.; Gut (2012); 61:A28
[4] Multivalent glycoconjugates as anti-pathogenic agents. Bernardi A, et al.; Chem Soc Rev. (2013); 42:4709 REVIEW
[5] Toll-like receptor 4 (TLR4) modulation by synthetic and natural compounds: an update. Peri F, Calabrese V. Med Chem. (2014); 57:3612 REVIEW
[6] A novel small molecule TLR4 antagonist (IAXO-102) negatively regulates non-hematopoietic toll like receptor 4 signalling and inhibits aortic aneurysms development.. Huggins C, et al. Atherosclerosis. 242:563 (2015) Journal Article
[7] Synthetic and natural small molecule TLR4 antagonists inhibit motoneuron death in cultures from ALS mouse model. De Paola M, et al. Pharmacol Res. 103:180 (2016) Pubmed Abstract
[8] Effects of Toll-Like Receptor 4 Antagonists Against Cerebral Vasospasm After Experimental Subarachnoid Hemorrhage in Mice. Kawakita F., et al. Mol Neurobiol 54:6624-6633 (2017) Pubmed Abstract
[9] Protective effect of IAXO-102 on renal ischemia-reperfusion injury in rats. Yahiya YI, Hadi NR, Abu Raghif A, Al Habooby NGS. J Med Life. 2023 Apr;16(4):623-630. doi: 10.25122/jml-2022-0280. PMID: 37305825; PMCID: PMC10251395 Pubmed Abstract

IAXO-103 (CD14/TLR4 Antagonist) (synthetic)

[1] Glycolipids and benzylammonium lipids as novel antisepsis agents: synthesis and biological characterization.
Piazza M, et al. J. Med. Chem. (2009); 52:1209
[2] Evidence of a specific interaction between new synthetic antisepsis agents and CD14. Piazza M, et al. Biochemistry (2009); 48:12337
[3] Therapeutic targeting of innate immunity with Toll-like receptor 4 (TLR4) antagonists. Peri F, Piazza M. Biotechnol. Adv. (2012); 30:251 REVIEW
[4] Exploring the LPS/TLR4 signal pathway with small molecules. Peri F, et al.; Biochem Soc Trans. (2010); 38:1390 REVIEW
[5] Multivalent glycoconjugates as anti-pathogenic agents. Bernardi A, et al.; Chem Soc Rev. (2013); 42:4709 REVIEW
[6] Toll-like receptor 4 (TLR4) modulation by synthetic and natural compounds: an update. Peri F, Calabrese V. Med Chem. (2014); 57:3612 REVIEW
 

IAXO-201 (Control for IAXO-102) (synthetic)

[1] Glycolipids and benzylammonium lipids as novel antisepsis agents: synthesis and biological characterization. Piazza M, et al. J. Med. Chem. (2009); 52:1209
[2] Inhibition of lipid a stimulated activation of human dendritic cells and macrophages by amino and hydroxylamino monosaccharides. Peri F, et al. Angew .Chem. (2007); 46:3308
[3] Evidence of a specific interaction between new synthetic antisepsis agents and CD14. Piazza M, et al. Biochemistry (2009); 48:12337
[4] Therapeutic targeting of innate immunity with Toll-like receptor 4 (TLR4) antagonists. Peri F, Piazza M. Biotechnol. Adv. (2012); 30:251 REVIEW
[5] Synthetic molecules and functionalized nanoparticles targeting the LPS-TLR4 signaling: A new generation of immunotherapeutics. Peri F, Calabrese V, Piazza M, Cighetti R. Pure Appl. Chem. (2012); 84:97 REVIEW
 

IAXO-202 (Control for IAXO-101 / IAXO-103) (synthetic)

[1] Glycolipids and benzylammonium lipids as novel antisepsis agents: synthesis and biological characterization. Piazza M, et al. J. Med. Chem. (2009); 52:1209
[2] Inhibition of lipid a stimulated activation of human dendritic cells and macrophages by amino and hydroxylamino monosaccharides. 
Peri F, et al. Angew. Chem. (2007); 46:3308
[3] Evidence of a specific interaction between new synthetic antisepsis agents and CD14. Piazza M, et al. Biochemistry (2009); 48:12337
[4] Therapeutic targeting of innate immunity with Toll-like receptor 4 (TLR4) antagonists. Peri F, Piazza M. Biotechnol. Adv. (2012); 30:251 REVIEW
[5] Synthetic molecules and functionalized nanoparticles targeting the LPS-TLR4 signaling: A new generation of immunotherapeutics. Peri F, Calabrese V, Piazza M, Cighetti R.Pure Appl. Chem. (2012); 84:97 REVIEW
 

TLR4 antagonists

[1] Synthetic glycolipid-based TLR4 antagonists negatively regulate TRIF-dependent TLR4 signalling in human macrophages. Palmer C, Facchini FA, Jones RP, Neumann F, Peri F, Pirianov G. Innate Immunity. 2021;27(3):275-284. doi:10.1177/17534259211005840 Abstract

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