Internal radiation using radiopharmaceuticals promises efficient cancer therapeutics. The specificity and selectivity required for screening and pinpointing tumor cells for cell-kill has been made possible by targeted ligands based on 'magic bullet' and tracer principle- theories nearing a century. Overexpression of certain receptors has been exploited using biomolecules for targeting. The pragmatic analysis, however, is not as promising compared with the theoretical knowledge of available gamut of vectors and targets. The complex interplay of in vitro and in vivo parameters, and the effect of radionuclides involve a systematic assessment of radiopharmaceuticals as diagnostic and therapeutic agent. This review presents different vectors with their pros and cons, present status and recent design variations followed by a future perspective based on novel approaches.