The cost of a new drug from discovery to launch is approaching $3B with the underlying time for development reaching up to 12 years. Given the costly and lengthy process, scientific and regulatory leaders in the pharmaceutical industry need to leverage all available tools to get drugs approved quickly and efficiently, bringing safe and efficacious medications for human needs. In recent years, pharmacometrics has emerged as an invaluable modeling and simulation tool that helps to de-risk and accelerate the drug development process. It facilitates the integration of preclinical/clinical development data and provides a scientifically based framework for designing a rationale dosage regimen and treatment optimization. There are several pharmacometrics techniques that can be elicited at various stages in the drug development pipeline to help make the approval process more efficient and get the most efficacious doses with increased safety for all patients, including special populations.