During the drug development, it has been very challenging to create potent compounds with perfect pharmacokinetic properties. Therefore, for example, the majority of central nervous system (CNS) drugs fail in clinical trials as they are not delivered to their site of actions, and thus, they lack efficacy and cause toxic side effects. The blood-brain barrier (BBB) prevents the uptake of numerous drug molecules into the brain, however, the cell membranes and the delivery to specific brain cell types may also create a secondary barrier for CNS-drugs. In this presentation, I will show how L-type amino acid transporter 1 (LAT1) can be utilized for brain-targeting purposes and what kind of methodology is required to develop transporter-utilizing brain-targeted prodrugs. The presentation will also cover the main challenges that can be faced when working with this approach.