Terpenoids: A Comprehensive Review on Biosynthesis, Applications and Enhancement Strategies for Translational Research

There is growing interest in natural bioactive compounds as potentially safer and more sustainable sources of therapeutic agents. Terpenoids, one of the most structurally diverse and biologically active classes of natural products, are derived from repeating isoprene units and possess a broad range of pharmacological and industrial applications. This review provides a comprehensive overview of recent advances in terpenoid biosynthesis, structural classification, and therapeutic applications. It also discusses emerging approaches for enhancing large-scale production, improving functional efficacy, and overcoming pharmacokinetic limitations. Attention is given to terpenoids currently undergoing clinical evaluation, along with their progress toward commercial development. Despite substantial preclinical evidence supporting their therapeutic potential, the clinical translation of many terpenoids remains limited. Key challenges include poor aqueous solubility, low permeability, slow dissolution, and high lipophilicity, which can collectively restrict systemic bioavailability and therapeutic efficacy. Moreover, only a relatively small proportion of biologically active terpenoids have progressed to advanced stages of clinical development, highlighting a considerable gap between experimental findings and clinical application. This review integrates current knowledge of terpenoid biosynthesis, biological activities, production strategies, and translational development while highlighting sustainable and scientifically driven approaches that may facilitate their future therapeutic and commercial utilization.