This review, as its title indicates, views acivicin at a particular point in the ongoing process of its development. There is a large body of biochemical information which permits the formulation of a number of hypotheses regarding the drug's optimal regimen, mechanism of CNS toxicity, and potential role in combination chemotherapy. We have attempted to survey those data and to project some avenues of future research which may circumvent the drug's limitations. Current deficits exist in our information, particularly in the area of the clinical activity spectrum of acivicin. Yet the final definition of the set of human tumors in which acivicin may find clinical utility will probably not occur until we have defined the optimal regimen for the drug, both as a single agent and in combination, and have identified and addressed the toxic effects which limit its use. A coordinated effort between the preclinical pharmacologists and clinicians will be necessary in the next few years, if acivicin is to play an important role in the treatment of human malignancies.