Recent technological advances have enabled precise quantitation of various bioanalytical measurements pertaining to antibody-drug conjugates (ADCs). However, availability of bioanalytical data alone cannot guarantee the provision of correct go/no-go decisions at different stages of ADC development. Integration and comprehension of all the available data at each stage of ADC development is necessary to make a well informed and objective decision about moving the ADC forward to the clinic. In this manuscript, we have reviewed the application of PK-PD modeling and simulation for quantitative integration of diverse bioanalytical data available from different stages of ADC development. We have also elaborated on how similar bioanalytical data can be characterized using different models to gain distinct insights into ADC development.