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AGX323 is an orally available, S-adenosylmethionine (SAM)-competitive small molecule inhibitor of protein arginine methyltransferase 5 (PRMT5). Developed by Angex Pharmaceutical, it targets PRMT5, an enzyme involved in key oncogenic processes including epigenetic regulation, DNA damage response, and RNA processing. Overexpression of PRMT5 is associated with poor prognosis in several solid malignancies. AGX323 has demonstrated potent nanomolar antiproliferative activity in preclinical models of non-small cell lung cancer (NSCLC), breast, bladder, and pancreatic cancers. It exhibits favorable drug-like properties, including high oral bioavailability across multiple species and robust in vivo antitumor efficacy in xenograft models.
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