•An unprecedented number of peptide therapeutics have recently been approved.•Clinical pipeline analysis reveals an emphasis on peptides with enhanced properties.•Development of innovative glucagon-like peptide (GLP)-1 receptor agonists is a strong growth area.•Peptide–drug conjugates and constrained peptides hold promise as new therapeutics. The notable expansion of peptide therapeutics development in the late 1990s and the 2000s led to an unprecedented number of marketing approvals in 2012 and has provided a robust pipeline that should deliver numerous approvals during the remainder of the 2010s. To document the current status of the pipeline, we collected data for peptide therapeutics in clinical studies and regulatory review, as well as those recently approved. In this Foundation review, we provide an overview of the pipeline, including therapeutic area and molecular targets, with a focus on glucagon-like peptide 1 receptor agonists. Areas for potential expansion, for example constrained peptides and peptide–drug conjugates, are profiled. The unprecedented number of marketing approvals in 2012 for peptide therapeutics could be a harbinger for the innovative peptide-based drugs in the clinical pipeline.