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Photodynamic sensitizers are drugs activated by light of a specific wavelength and are used in the photodynamic therapy (PDT) of certain diseases. Second- and third-generation photosensitizers with improved PDT properties are now under investigation. In this issue of the British Journal of Pharmacology, Leung et al. have described the synthesis and investigation of a second-generation photosensitizer (BAM-SiPc) targeted towards the cells of HepG2 and HT29 tumours. BAM-SiPc is selectively functionalized with bis-amino groups and has demonstrated potent PDT activity in a small animal model. However, it also exhibited non-selective distribution and accumulation in multiple animal (small mouse) organs and tissue. These issues highlight the importance and need for good biodistribution and localization properties for an efficacious photosensitizer. The lack of tumour specificity may have a significant impact on the potential BAM-SiPc has in clinical PDT. [ABSTRACT FROM AUTHOR]