The primary aim of this review article is to highlight current exciting and future looking areas of research in peptide science as applied to the discovery and development of novel therapeutics. Among the strengths of peptides as drug candidates are their high potency, specificity, and good safety profile. These positive attributes of peptides along with advances in drug delivery technologies have generated renewed interest in the discovery, optimization, and development of peptides as therapeutics. The intent of this review is to demonstrate that peptides have broad applicability in many therapeutic areas by examining some of the most compelling indications and targets for peptide therapeutics. For example, target selection for peptide therapeutics is challenging due to the inherent properties of peptides; therefore, identifying a clear differentiation strategy for a new peptide program over a small molecule or antibody program from the outset is critical for successful navigation of drug development hurdles. In this review, some of the latest techniques that accentuate the advantages and overcome the druggability limitations of peptides will be covered. Emerging technologies for enhancing the pharmacokinetics of peptides to achieve sufficient in vivo half-lives will be described and evaluated, as well as novel technologies for getting peptides across cell membranes to reach intracellular targets and across the blood-brain-barrier to reach central nervous system targets.