Calixdrugs are calix[4]arene-based clusters (chaliced shapes) of established therapeutic drugs (e.g., penicillin, cephalosporin, tyrosol, and carboplatin) that are innovatively named calixpenam, calixcephem, calixtyrosol, and calixplatin, respectively. Going over the structures of cluster compounds, the calixarene scaffold lies at the heart of the structure (chaliced shape of drug), and it is an integral part of the cluster. In fact, the monomer drugs contribute as 1/4 of the corresponding cluster. In addition, probably because of the multivalency, spatial preorganization, and synergistic effect of four impacted drug units in the structures of calixdrugs, they are more effective in interactions with the target sites over their corresponding monomers.