The receptor activity modifying proteins (RAMPs) are a family of membrane proteins that interact with some G protein-coupled receptors (GPCRs) to regulate their function. RAMPs can alter GPCR pharmacology and can regulate their signaling as well as trafficking to and from the cell surface. GPCRs have been successfully exploited as drug targets for many years. RAMPs therefore provide a new avenue for drug development, offering opportunities for regulating the function of therapeutically relevant RAMP-interacting GPCRs. RAMPs could be directly targeted themselves or advantage could be taken of the unique RAMP/GPCR interfaces for generating more selective drugs.