The chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of vinorelbine are reviewed. Vinorelbine is a semisynthetic vinca alkaloid with a broader spectrum of antitumor activity in vitro than naturally occurring vinca alkaloids have. Vinorelbine shows selective activity against mitotic microtubules. Higher concentrations of vinorelbine relative to vinblastine and vincristine are required to affect axonal microtubules; presumably this accounts for the decreased neurotoxicity of vinorelbine. Vinorelbine is lipophilic and is rapidly distributed into peripheral tissues. It is highly bound to blood components. Vinorelbine is excreted slowly by the fecal route and rapidly by the urinary route. Disposition is characterized by a three-compartment model, high systemic clearance, and a long terminal-phase elimination half-life. In clinical studies, vinorelbine has shown antitumor activity both as a single agent and in combination with cisplatin in patients with non-small-cell lung cancer (NSCLC). Vinorelbine plus cisplatin produces a higher response rate and longer survival than vindesine plus cisplatin, a combination previously found to be superior to best supportive care. Encouraging results for vinorelbine in the treatment of advanced breast cancer, advanced ovarian epithelial cancer, and other tumors have also been observed. The dose-limiting adverse effect of vinorelbine is myelosuppression. Vinorelbine has FDA-approved labeling for use alone or in combination with cisplatin for the first-line treatment of unresectable, advanced NSCLC. The recommended dosage is 30 mg/sq m i.v. weekly administered by either slow i.v. push or i.v. infusion. Vinorelbine alone or in combination with other antineoplastics has shown activity against NSCLC, advanced breast cancer, and other malignancies. More study is needed to determine whether vinorelbine is superior to best supportive care in patients with NSCLC.