RTX-1738

RTX-1738 is a highly potent, selective, brain-penetrant, and orally bioavailable small molecule that acts as a negative allosteric modulator (NAM) of the AMPA receptor (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor), specifically targeting the transmembrane AMPA receptor regulatory protein gamma 8 (TARPγ8). By selectively inhibiting AMPARs associated with TARPγ8, which are enriched in brain regions involved in pain processing and seizure activity, RTX-1738 aims to provide neuroanatomical specificity for central nervous system disorders. Preclinical studies have demonstrated robust analgesic efficacy across acute, persistent, inflammatory, and neuropathic pain models as well as antiseizure effects in animal models. The compound is being developed by Rapport Therapeutics primarily for broad-spectrum analgesia and has also shown potential in preclinical epilepsy models[1][2][3][4][5][7][9].