Luteolin, a flavone abundant in various plant-based foods, presents a multifaceted pharmacological profile with promising therapeutic implications. This review provides a comprehensive analysis of the pharmacokinetics of luteolin, elucidating its absorption, distribution, metabolism, and excretion properties. Additionally, the protective mechanisms of luteolin are presented, encompassing its anti-inflammatory, antioxidant, and anti-apoptotic properties, which have been demonstrated in various in vitro and in vivo models. Furthermore, the review explores the impact of luteolin on diverse disorders, including cardiovascular diseases, neurodegenerative disorders, cancer, and liver and kidney diseases. In addition, synergistic effects of luteolin with conventional chemotherapeutic agents are discussed, shedding light on its potential in cancer therapy. Furthermore, we provide insights into ongoing clinical studies, emphasizing the need for more rigorous investigation to validate the therapeutic benefits of luteolin in human populations. Overall, luteolin emerges as a promising therapeutic candidate, warranting further research to unlock its full therapeutic potential and facilitate its clinical application in various disease contexts.