<p>Climate change profoundly affects the phytochemical profiles and therapeutic potentials of medicinal plants through environmental stressors such as rising temperatures, altered precipitation patterns, and increased atmospheric CO₂ levels. This review critically examines the mechanisms underlying these impacts, focusing on physiological plant responses, shifts in primary and secondary metabolite biosynthesis, and the consequent effects on medicinal efficacy and toxicity. Our findings indicate that elevated CO₂ often enhances biomass production but exerts variable effects on bioactive compound concentrations; temperature fluctuations disrupt phenological phases, thereby altering medicinal quality; and water stress significantly modulates secondary metabolite profiles. While these environmental challenges threaten plant-based healthcare, potential mitigation strategies—including sustainable agricultural practices, genetic engineering, and conservation approaches—are discussed as viable solutions. We recommend future research to emphasize metabolomics, interdisciplinary methodologies, and integration of traditional knowledge to bolster resilience and preserve the therapeutic efficacy of medicinal plants amid ongoing climatic uncertainties.</p> Graphical Abstract <p></p>