Porphyrins are crucial photosensitizers (PS) in photodynamic therapy (PDT) due to their ability to generate singlet oxygen (¹O₂), which makes them instrumental in tumor treatment. PDT functions through a combination of light, PS, and oxygen, triggering oxidative stress that selectively destroys tumor cells. Current research is increasingly focused on conjugating porphyrins with peptides to improve their solubility, stability, and tumor-specific targeting. Peptide conjugates enhance the selectivity and effectiveness of PS while reducing harmful effects on healthy tissues. However, a persistent challenge is the aggregation of porphyrins, which diminishes their solubility, biodistribution, and photophysical properties, thereby reducing PDT's therapeutic efficiency. Porphyrins can bind to peptides through covalent, coordinative, or non-covalent interactions, with each approach offering specific advantages in creating stable, functional conjugates. Different synthetic methods, such as solid-phase peptide synthesis (SPPS) and solution-phase conjugation, have been developed to create these conjugates. SPPS enables efficient peptide synthesis followed by subsequent attachment to porphyrins, while solution-phase synthesis leverages the inherent functional groups of peptides for direct conjugation to porphyrin derivatives. These porphyrin-peptide conjugates are integral to PDT and other biomedical applications by facilitating precise tumor targeting, thereby enhancing therapeutic outcomes and reducing toxicity. Recent progress in the synthesis of porphyrin-peptide conjugates is opening new avenues in photodynamic therapy, diagnostics, and drug delivery, with great potential to further improve cancer treatment and other therapeutic interventions.