Calixarene nano-baskets enable to encapsulate the guest drugs and show different biological activities. This review deals with the behavior of calixarene-based drugs and illustrates their potentials in the pharmacological sciences. The role of calixarene's scaffolds and substitutions in aspects of anti-cancer, anti-mycobacterial, antiproliferativity, catalytic and inhibitory activities as well as solubility control, drug analysis, drug purification, drug supports and structural studies is reviewed.