This review article briefly describes: (a) the advantages in developing multifunctional nanoparticles for cancerimaging and therapy, (b) the advantages and limitations of most of the porphyrinbased compounds in fluorescence imaging and photodynamic therapy (PDT), (c) problems associated with current Food and Drug Administration (FDA) approved photosensitizers, (d) challenges in developing in vivo targetspecific PDT agents, (e) development of porphyrinbased nuclearimaging agents (PET, SPECT) with an option of PDT, (f) the importance of light dosimetry in PDT, (g) the role of whole body or local hyperthermia in enhancing tumoruptake, tumorimaging and phototherapy and finally, (h) the advantages of photosensitizergold nanocages (PsAu NC) in photoacoustic and PDT.