Hybrid drugs, also termed “single molecule multiple targets” or “multiple ligands”, can be referred to as the most sophisticated form of combination therapy. They are designed utilizing molecular hybridization—a strategy of rational drug design which enables the fusing of one or more bioactive compounds or their pharmacophoric subunits into one molecule, which represents the preselected, desired features of original drugs. Obviously, connected entities should retain affinity to their specific targets and provide a superior therapeutic effect by amplification or exerting multifactorial biological activity. Such a single hybrid agent can modulate multiple targets involved in proliferation and efficiently destroy cancer cells.