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BY101921 is a highly selective, orally administered small molecule inhibitor of PARP7 (ADP-ribosyltransferase diphtheria toxin-like 14, also known as ARTD14 or DDF1), developed by Chengdu Baiyu Pharmaceutical. It is designed to restore type I interferon signaling and enhance anti-tumor immunity in cancer. Preclinical studies have shown that BY101921 has potent anti-tumor activity both as monotherapy and in combination with anti-PD-1 therapy, with favorable pharmacokinetic properties and tolerability in animal models. Mechanistically, it upregulates pSTAT1 levels and promotes secretion of IFN-β and CXCL10, thereby restoring the type I interferon pathway. Clinical trials are ongoing to evaluate its safety, tolerability, pharmacokinetics, and preliminary efficacy in patients with advanced solid tumors[1][2][3].
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