L-His-BPA is a prodrug of L-p-Boronophenylalanine (L-BPA) ( HY-W087830 ), formed by the peptide bond linkage of L-histidine (L-His) ( HY-N0832 ) and L-BPA. L-His-BPA is rapidly cleaved by endogenous proteases to de novo release L-BPA in the systemic circulation. When used in combination with neutron irradiation, L-His-BPA induces complete and durable tumor regression, elicits cancer vaccine responses, and produces abscopal inhibitory effects on unirradiated distant tumors. L-His-BPA can be used in studies of boron neutron capture therapy (BNCT) for relapsed/advanced solid tumors.
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