Taxol is the first novel antimicrotubule agent approved for clinical use since the vinca alkaloids in the 1960s and may be one of the most important antineoplastic agents to emerge over the last two decades. Significant antitumor activity has been noted in ovarian, breast, lung, and head and neck cancers. This report reviews the clinical pharmacology of Taxol based on early developmental trials of the agent administered on various intravenous schedules as a single agent and in combination with other antineoplastic agents, as well as via the intraperitoneal route. In addition, available information pertaining to the pharmaco-dynamic and metabolic profiles of Taxol are discussed. Such information may be useful in designing rational treatment approaches with Taxol either as monotherapy or in chemotherapy combinations, potentially resulting in the optimal use of this important agent in cancer chemotherapeutics.