The review discusses the potential of BODIPY dyes in photodynamic therapy (PDT), a clinical modality for treating neoplastic and non-malignant lesions. BODIPY dyes, known for their high fluorescence, can be modified to enhance singlet-to-triplet intersystem crossing, generating singlet oxygen upon photoexcitation. This singlet oxygen causes cell damage in illuminated regions, leading to PDT. The review highlights the advantages of BODIPY-based PDT agents, including their low toxicity, cellular uptake, and high extinction coefficients. It also explores various modifications to BODIPY cores, such as halogenation and aza-borylation, to improve their PDT properties. Aza-BODIPY compounds, in particular, show promise due to their red-shifted absorption maxima and high singlet oxygen generation efficiency. The review further discusses the application of BODIPY dyes in observing reactive oxygen species and their use in chromophore-assisted light inactivation (CALI) for molecular-level targeting. Overall, the review emphasizes the potential of BODIPY-based PDT agents for clinical development and active targeting strategies.The review discusses the potential of BODIPY dyes in photodynamic therapy (PDT), a clinical modality for treating neoplastic and non-malignant lesions. BODIPY dyes, known for their high fluorescence, can be modified to enhance singlet-to-triplet intersystem crossing, generating singlet oxygen upon photoexcitation. This singlet oxygen causes cell damage in illuminated regions, leading to PDT. The review highlights the advantages of BODIPY-based PDT agents, including their low toxicity, cellular uptake, and high extinction coefficients. It also explores various modifications to BODIPY cores, such as halogenation and aza-borylation, to improve their PDT properties. Aza-BODIPY compounds, in particular, show promise due to their red-shifted absorption maxima and high singlet oxygen generation efficiency. The review further discusses the application of BODIPY dyes in observing reactive oxygen species and their use in chromophore-assisted light inactivation (CALI) for molecular-level targeting. Overall, the review emphasizes the potential of BODIPY-based PDT agents for clinical development and active targeting strategies.