In the rapidly evolving field of pharmacokinetics, artificial intelligence (AI) is emerging as a game-changer, offering groundbreaking solutions to traditional challenges. AI is revolutionizing the way pharmacokinetic profiles are predicted from chemical structures, significantly enhancing aspects of pharmacology such as dosage customization and understanding drug interactions. This technological advancement also brings to the forefront the importance of ethical considerations and the need for transparency, particularly in dataset adaptation for pharmacokinetic predictions. Looking towards the future, the development of comprehensive AI-driven pharmacokinetics/pharmacometrics software holds the promise of transforming drug discovery and patient care into more individualized and effective healthcare solutions. This innovative approach not only streamlines processes like data cleaning and model selection but also prepares for regulatory report preparation, marking a significant leap in the pharmaceutical sciences.