Although there has been a rapid expansion of the number of classes of compounds with antineoplastic activity, few have played a more vital role in the curative and palliative treatment of cancers than the antimicrotubule agents. Although the vinca alkaloids have been the only subclass of antimicrotubule agents that have had broad experimental and clinical applications in oncologic therapeutics over the last several decades, the taxanes, led by the prototypic agent taxol, are emerging as another very active class of antimicrotubule agents. After briefly reviewing the mechanisms of antineoplastic action and resistance, this article comprehensively reviews the clinical pharmacology, therapeutic applications, and clinical toxicities of selected antimicrotubule agents.