Purpose of review: To discuss the avenues that proteomic techniques are opening for the study of the chemical basis and cellular mechanisms of immunological reactions to drugs.
Recent findings: Technical developments in recent years are allowing a detailed characterization of drug–protein interactions. In addition, novel metabolic pathways for drug biotransformation are being uncovered and potential targets for protein haptenation are being proposed that may help in the understanding of these complex processes.
Summary: Immunological reactions to drugs pose important clinical problems. Since early works exploring drug–protein interactions, there has been steady progress in this field. However, the mechanisms involved remain incompletely understood. The availability of proteomic techniques with high resolution and sensitivity presents a unique opportunity to tackle this subject from a broad perspective, integrating work in model systems and in patients. Chemical and metabolic characterization of immunological reactions to drugs may also help in the prevention, diagnosis and/or treatment of these processes.