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The late‐stage modification of structurally complex peptides bears great potential for drug discovery, crop protection, and the pharmaceutical industry, among others. Whereas traditional approaches largely rely on prefunctionalizations, C−H activation catalysis has in recent years emerged as an increasingly powerful tool for post‐translational peptide modifications in a step‐economic manner. Herein, we summarize recent progress in organometallic C−H activation on peptides until June 2018, including position‐ and chemoselective palladium‐, ruthenium‐, and manganese‐catalyzed processes.