Abstract: The research and development of innovative drugs has undergone significant changes from small molecule drugs to biopharmaceuticals, and then to cell and gene therapy products. Meanwhile, the demand for high-quality pharmaceutical products is no longer limited to the types of innovative drugs; more precise dosing regimens have also become an important aspect in improving patients’quality of life. In addition, the drug clinical trial failures due to insufficient dose exploration is also common, making dose exploration and optimization a crucial process in innovative drug development. Clinical pharmacology research spans the entire lifecycle from drug development to post-marketing surveillance. This article aims to establish a more refined, comprehensive, multidimensional, and mechanism-centered quantitative framework by delving into the clinical pharmacological characteristics of different types of drugs, along with scientific considerations in selecting critical metrics for exposure-response relationships, data analysis, and evidence evaluation, aiming to further elucidate the essential role of clinical pharmacological studies in exploring and optimizing innovative drug dosing to ensure safety and efficacy in patient care.