Metabolism of Taxoid Drugs

Abstract: The metabolism of the two most promising anti-cancer taxoid drugs - docetaxel (Taxotere) and paclitaxel (Taxol) - is fully reported. Complete in-vitro and in-vivo results in animals and humans are described while structures of the observed metabolites are identified. The chemical synthesis of the major metabolites of docetaxel as well as their biological activities are reported. Furthermore, in accordance with the chemical reactivity observed for some of the synthetic intermediates, a metabolic pathway is proposed.