Definition

A blood-brain-barrier (BBB) penetrative agent composed of a cytotoxic chemotherapeutic domain, tertiary N-bis(2-chloroethyl)amine, linked to the structural features of a selective large amino acid transporter 1 (LAT1) substrate, with potential antineoplastic activity. Upon administration of QBS10072S, the LAT1 substrate binds to LAT1 expressed on the BBB and in LAT1-expressing cancer cells, such as glioblastoma multiforme (GBM). After entering the brain and binding to LAT1-expressing tumor cells, the cytotoxic domain in turn binds to DNA, causing cell cycle arrest and induces apoptosis. LAT1 is expressed at much lower levels in normal brain tissue and QBS10072S may therefore potentially target brain tumors while avoiding uptake by healthy, normal tissue.