The goal of the current work was to explore the human organic cation uptake transporter and its critical function in biological transportation. The hOCT is extensively articulated in the liver and has been found to have a broad range of substrate selectivity, which is encoded by the SLC22A1 gene. OCT1 promotes molecular diffusion, enabling nutrients to enter the cell. OCT1 can aid in the absorption of drugs used to treat illnesses like cancer, according to recent research. Functionally impaired OCT1, whose appearance levels are associated with responses to a variety of medications, is the root cause of drug resistance. One of the important pharmacological targets employed in pharmacogenomic studies has recently been proposed as OCT1. The entire OCT1 gene contains a few single nucleotide polymorphisms. Also unknown are the specific changes or interactions with other proteins required for OCT1 to recognize a range of ligands. The authors presented the most recent OCT1 findings in this review to stimulate further investigation into this crucial uptake transporter.