Brands, Medical Use, Clinical Data
- Radiation-Sensitizing Agents
- Antineoplastic Agents
Brands / Synonyms
Navelbine; Navelbine Base; Vinorelbin; Vinorelbina [Spanish]; Vinorelbine; Vinorelbine Bitartrate; Vinorelbine Ditartarate; Vinorelbine Ditartrate; Vinorelbine Tartrate; Vinorelbinum [Latin]
For the treatment of non-small-cell lung carcinoma
Vinorelbine is a vinca alkaloid antineoplastic agent used as a treatment for various cancers including breast cancer, Hodgkin's disease, Kaposi's sarcoma, and testicular cancer. The vinca alkaloids are structurally similar compounds comprised of 2 multiringed units, vindoline and catharanthine. The vinca alkaloids have become clinically useful since the discovery of their antitumour properties in 1959. Initially, extracts of the periwinkle plant (Catharanthus roseus) were investigated because of putative hypoglycemic properties, but were noted to cause marrow suppression in rats and antileukemic effects in vitro. Vinorelbine binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death. Vinorelbine has some immunosuppressant effect. The vinca alkaloids are considered to be cell cycle phase-specific.
Mechanism of Action
The antitumor activity of vinorelbine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin. Like other vinca alkaloids, vinorelbine may also interfere with: 1) amino acid, cyclic AMP, and glutathione metabolism, 2) calmodulin-dependent Ca2+-transport ATPase activity, 3) cellular respiration, and 4) nucleic acid and lipid biosynthesis.
Biotrnasformation / Drug Metabolism
Administration of NAVELBINE is contraindicated in patients with pretreatment granulocyte counts
Acute pulmonary reactions have been reported with NAVELBINE and other anticancer vinca alkaloids used
in conjunction with mitomycin. Although the pharmacokinetics of vinorelbine are not influenced by the concurrent
administration of cisplatin, the incidence of granulocytopenia with NAVELBINE used in combination with cisplatin is
significantly higher than with single-agent NAVELBINE. Patients who receive NAVELBINE and paclitaxel, either
concomitantly or sequentially, should be monitored for signs and symptoms of neuropathy. Administration of NAVELBINE
to patients with prior or concomitant radiation therapy may result in radiosensitizing effects.
Caution should be exercised in patients concurrently taking drugs known to inhibit drug metabolism by
hepatic cytochrome P450 isoenzymes in the CYP3A subfamily, or in patients with hepatic dysfunction. Concurrent
administration of vinorelbine tartrate with an inhibitor of this metabolic pathway may cause an earlier onset and/or
an increased severity of side effects.