Central nervous system (CNS) is always an area of thrust where continuous efforts are required to achieve targeted drug delivery. The blood brain barrier (BBB) is the chief interfering element in the development of effective neurotherapeutics and efficient drug delivery to the CNS. Large neutral amino acid (LAT1) is the one which is the most promising gateway and belongs to the carrier-mediated transporters (CMTs), which is also called as Solute Carrier Family 7 Member 5 (SLC7A5). LAT1 is a sodium-and pH-independent transporter, which not only supplies essential amino acids to cells but also plays an important role in the facilitated transport of thyroid hormones, pharmaceuticals and metabolites into the brain by breaching the BBB. Levodopa, melphalan, gabapentin, brexpiprazole, valbenazine and α-methyldopa are already known drugs which cross the BBB via LAT1 mediated transport; therefore, the LAT1 is thought to be a potential target for piercing the BBB. This review is a combined effort to shed light on the pharmaceutical importance of this transporter and how this can be exploited further as a mediator for drugs to cross the BBB.
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