BY101298

BY101298 is an innovative, highly selective small molecule inhibitor of DNA-dependent protein kinase (DNA-PK). DNA-PK plays a critical role in the non-homologous end joining (NHEJ) pathway, which repairs DNA double-strand breaks (DSBs). By inhibiting DNA-PK activity, BY101298 impairs DSB repair, thereby enhancing the cytotoxic effects of radiotherapy and chemotherapy on tumor cells. This mechanism may reduce local recurrence and metastasis in cancer patients. The drug is being developed primarily for use in advanced malignant solid tumors and is currently undergoing phase 1 clinical trials to assess its safety, tolerability, pharmacokinetics, and preliminary efficacy both as monotherapy and in combination with radiotherapy.