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To retrieve relevant published information, we used the keywords “small molecules,” “helminths small molecules,” “immunomodulatory,” “helminth-derived small molecules,” “host-parasite interaction,” “helminth metabolites,” “lipidomics,” “helminth therapy,” “metabolomics,” “targeted metabolomics,” “untargeted metabolomics,” “inflammation,” “inflammatory bowel diseases,” “autoimmune disease,” “inflammatory cytokines,” “anti-inflammatory,” “helminthiases,” “clinical trials,” “host-parasite interaction,” “biomarkers,” “down-regulation,” “up-regulation,” “excretory/secretory products,” and names of different helminth species.” We have conducted a narrative review of the available literature and presented SM identified from helminths and their reported biological activities, exploring their potential scope in diagnostics and therapeutics development