Medicinal plants have served as the foundation of therapeutic interventions across diverse cultures for millennia, representing an invaluable repository of bioactive compounds with untapped pharmaceutical potential. Ethnopharmacology, the interdisciplinary science examining the cultural use of plants for medicinal purposes, provides a systematic framework for translating traditional knowledge into evidence-based drug discovery pipelines. This article examines the integration of ethnopharmacological approaches with contemporary pharmacological methodologies to accelerate the identification and development of plant-derived therapeutics. Key themes explored include the historical and cultural dimensions of medicinal plant use, systematic screening and selection strategies informed by ethnobotanical data, isolation and structural characterization of bioactive constituents, elucidation of molecular mechanisms and therapeutic targets, preclinical validation through in vitro and in vivo models, clinical translation and human safety assessment, and critical considerations regarding toxicity, herb-drug interactions, and regulatory standardization. The convergence of traditional wisdom with advanced analytical techniques, high-throughput screening platforms, genomics, and systems pharmacology has enabled the rational design of botanical therapeutics with improved efficacy and safety profiles. Despite significant progress, challenges persist in quality control, bioavailability enhancement, intellectual property rights, and sustainable sourcing. Future directions emphasize the application of artificial intelligence, network pharmacology, and precision medicine approaches to optimize ethnopharmacology-guided drug development, ensuring that traditional knowledge contributes meaningfully to global health solutions while respecting indigenous rights and biodiversity conservation.