Review of Clinical Pharmacology Information for Peptides Found in US FDA Drug Labeling

Abstract Peptides are oligomers with ≤40 amino acids and are regulated as small molecule drugs. Peptides can exhibit certain clinical pharmacology features characteristic of small molecule drugs and others characteristic of biologics. To inform best practices in clinical pharmacology, we reviewed general characteristics of peptides approved by US Food and Drug Administration before July 2022 and how often clinical pharmacology information, and corresponding recommendations were discussed in drug labeling. For peptides, clinical pharmacology information was available in the labeling related to renal impairment for 57% (30/53), drug–drug interactions for 49% (26/53), immunogenicity for 40% (21/53), hepatic impairment for 38% (20/53), QT interval assessment for 34% (18/53), and mass balance for 17% (9/53). Actionable clinical pharmacology recommendations found in labeling related to each survey topic were catalogued and included dose adjustments and risk mitigation strategies.