Human colon adenocarcinoma cells (LoVo) resistant to the new antitumor agent FCE 24517 [benzoyl-mustard derivative of distamycin A] (LoVo/24517) are resistant to the selecting agent and related molecules as well as to vinblastine, with marginal or no resistance to other antitumour drugs. Treatment with verapamil, tamoxifen, nicergoline or cyclosporin A only partially restores the activity of FCE 24517 against LoVo/24517 cells. Such results suggest that resistance mechanisms possible specific for this class of compounds are operating.