Photodynamic therapy (PDT) is a relatively new cytotoxic treatment, predominantly used in anticancer approaches, that depends on the retention of photosensitizers in tumor and their activation after light exposure. This technology is based on the light excitation of a photosensitizer which induces very localized oxidative damages within the cells by formation of highly reactive oxygen species, the most important being singlet oxygen. Many photo-activable molecules have been synthesized such as porphyrins, chlorins and more recently phthalocyanines which present a strong light absorption at wavelengths around 670 nm and are therefore well-adapted to the optical window required for PDT application. However, the lack of selective accumulation of these photo-activable molecules within tumor tissue is a major problem in PDT, and one research area of importance is developing targeted photosensitizers. Indeed, targeted photodynamic therapy offers the advantage to enhance photodynamic efficiency by directly targeting diseased cells or tissues. Many attempts have been made to either increase the uptake of the dye by the target cells and tissues or to improve subcellular localization so as to deliver the dye to photosensitive sites within the cells. The aim of this review is to present the actual state of the development of phthalocyanines covalently conjugated with biomolecules that possess a marked selectivity towards cancer cells; for some of them their photophysical properties and photodynamic activity will be presented.