AMY109   Click here for help

GtoPdb Ligand ID: 12789

Synonyms: AMY-109 | H1009/L395-F1974m [2]
Immunopharmacology Ligand
Compound class: Antibody
Comment: AMY109 is a long-acting monoclonal antibody that blocks IL-8 recycling [4]. It was designed to reduce levels of IL-8 in endometriosis lesions, in which excessive IL-8 has been identified as a driving factor in promoting inflammation and fibrosis [1,3,5]. AMY109 is proposed as a potential disease-modifying treatment for endometriosis.
AMY109 is engineered to bind IL-8 in a pH-dependent manner. In the acidic conditions within the endosome, the antibody-IL-8 mmune complex dissociates; the free antibody is re-cycled and the IL-8 is trafficked to the lysosome for degradation.
Bioactivity Comments
AMY109 binds to cynoIL-8 with an affinity (Kd) of 0.38 nM (pKd 9.42) [4]. In vitro AMY109 inhibits both the recruitment of neutrophils to human endometriosis-derived cells, and neutrophil production of monocyte chemoattractant protein-1 [4].
Selectivity at ligand targets
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
CXCL8 Hs Antibody Binding 10.4 pKd - 4
pKd 10.4 (Kd 3.7x10-11 M) [4]