L-BPA dipeptide

L-BPA dipeptide refers to a class of highly soluble, ¹⁰B-enriched l-boronophenylalanine (l-BPA)-based dipeptide prodrugs developed for Boron Neutron Capture Therapy (BNCT). These agents are designed to overcome the poor aqueous solubility of native l-BPA, allowing for significantly higher intravenous dosing. The dipeptides target the Large Amino Acid Transporter 1 (LAT-1/SLC7A5), which is overexpressed in various solid tumors. Upon administration, endogenous proteases rapidly cleave the dipeptide to release l-BPA de novo within the tumor. Subsequent irradiation with epithermal neutrons triggers a nuclear capture reaction, producing high-linear energy transfer (LET) alpha particles and lithium nuclei that selectively destroy tumor cells while sparing healthy tissue. Research by TAE Life Sciences and Kyoto University has demonstrated that these prodrugs can induce complete tumor regression and a cancer vaccine effect in preclinical models.