GPCRs constitute the largest receptor family in the human genome. Over the years they have proven themselves to be druggable targets accounting for about 1/3 of all drugs on the market today. Of these, approximately 15% have been approved by the US Food and Drug Administration (FDA) in the last 5 years. Recent GPCR drug discovery efforts are expanding the range of disease indications to include polycystic ovarian syndrome, gastroparesis, pulmonary fibrosis, and smoking cessation. This talk will cover some of the novel targets, such as the calcitonin gene-related peptide (CGRP) receptor, the bile acid receptor GPBAR, the hydroxycarboxylic acid (HCA2 and HCA3) receptors, and orphan GPCRs such as GPR119. Also covered will be the development of antibody-based therapeutics for GPCRs such as mogamulizumab for the chemokine receptor CCR4.