As our understanding of biological systems is increasing, a range of exciting novel biological targets are being discovered where modulation may enable new therapeutic options for many diseases. These targets include growth factor receptors, protein-protein and protein nucleic acid interactions, which are often refractory to classical small molecule approaches. Other types of molecules, or modalities, can therefore be used to address these targets. One class of these molecules are peptides. Peptides are often highly selective and potent signalling molecules and this class of molecules have contributed towards many drugs which are used to treat disease. However, the inherent instability of peptides in plasma leading to a short half life after dosing has limited the broader application of peptide-based drugs. A range of approaches are now being explored and applied to extend the half life of bioactive peptides including the use of more stable, natural peptidic frameworks and utilising other modalities, such as small molecules, conjugated to peptides to enhance their properties. In addition to acting as therapeutic agents themselves, the exquisite selectivity of peptides is also now being used to target other agents to specific tissues. Once a bioactive peptide with the desired biological properties has been discovered, many challenges remain including optimising the physicochemical and biophysical properties of the peptide-based molecules to allow effective development, ultimately allowing future treatment options for patients. All of these perspectives will be discussed with examples during this presentation.