Compared with small‐molecule drugs (SMDs), the development of biologics has become one of the fastest growing areas in research and drug development owing to advancement in biotechnology sciences such as recombinant protein technology. This chapter focuses on the clinical pharmacology aspects of biologics, including their basic pharmacokinetic (PK)/pharmacodynamic (PD) characteristics, first‐in‐human dose selection, model‐based dose determination, and trial design. It also discusses monoclonal antibodies, proteins, and peptides. Compared to SMDs, biologics have unique characteristics in absorption, distribution, metabolism, and elimination, which play a role in their use as therapeutic interventions and lead to significant differences in their development. Quantitative methods, such as mechanism‐based PK, physiologically‐based PK, PK/PD, and exposure‐response models, offer great benefit for biologics development. With the advancement of new quantitative tools, drug developers and researchers can gain powerful insight into designing the most effective therapeutic regimens.