Abstract: In accordance with the present invention, it has been discovered that certain synthetic steroid compounds are capable of inhibiting the efflux pump which is believed to be responsible for multidrug resistance, while at the same time activating glucocorticoid-induced response. Thus, chemotherapy of glucocorticoid sensitive tumors can be enhanced by use of a compound having the dual ability to activate glucocorticoid-induced response and facilitate the accumulation of drug at the target site, with reduced or eliminated competition by the drug efflux system.