Skip to content
Bending the Curve Trial by Trial
?

Microtubule-targeting agentsIn useDerivative of an earlier drug

Vinorelbine

Also known as Navelbine, 5'-noranhydrovinblastine, NVB, vinorelbine tartrate

A semisynthetic vinca alkaloid given by injection. Its 2024 US generic label lists first-line treatment of non-small cell lung cancer, in combination with cisplatin or as a single agent.

From discovery to approval

  1. 1979 · Earliest report found

    Vinorelbine is 5'-noranhydrovinblastine, a vinblastine derivative modified on the catharanthine part of the molecule. The earliest papers found are two 1979 chemistry reports by Mangeney, Potier and colleagues, cited by title only.[2][3][4][5][6][7][8]

  2. 1994-12-23 · FDA regular

    Vinorelbine (Navelbine), NDA 020388, original approval, classed as a new molecular entity with priority review in the Drugs@FDA history. The original label and letter are not available there, so the indication at approval is not stated here; a 2024 generic label gives 1994 as the year of initial US approval and lists non-small cell lung cancer. The type regular is an inference: no accelerated-approval wording was found.[9]

How it works

The label describes a vinca alkaloid that interferes with microtubule assembly; antitumour activity is thought to come mainly from inhibition of mitosis at metaphase through interaction with tubulin. In the label's mouse-embryo experiment it was modestly more selective for mitotic than for axonal microtubules.[1]

Where it came from and why

A 1997 review says it reached clinical trial because preclinical work suggested less toxicity to neuronal tissue and greater cytotoxic activity than the older vinca alkaloids. A 1991 review says it affects axonal microtubules less than mitotic ones, and describes it as developed by Pierre Fabre Médicament.

Cancers

Family and partners

Derived from: Vinblastine

Drugs derived from it: Vinflunine

Worth knowing

  • The 2024 US generic label lists only non-small cell lung cancer indications, although earlier reviews of the development programme describe activity in breast cancer, ovarian cancer and Hodgkin disease.[1]
  • The authors of a 1989 study of its effects on tubulin say it showed for the first time that an anticancer drug can discriminate between the various types of microtubules; with vinorelbine only certain tau isoforms induced paracrystals, whereas all isoforms could contribute with vincristine or vinblastine.[4]
  • A 1991 review reports that the phase I trial of weekly intravenous vinorelbine found a maximum tolerated dose of 27.5 to 35.4 mg/m2 and set the recommended dose at 30 mg/m2 weekly.[6]
  • In the ANITA trial of 840 patients with completely resected stage IB to IIIA NSCLC, adjuvant vinorelbine plus cisplatin gave a median survival of 65.7 months against 43.7 months with observation (hazard ratio for death 0.80, 95% CI 0.66 to 0.96).[11]

References

  1. Sagent Pharmaceuticals. Vinorelbine injection: prescribing information. DailyMed, set ID 10a70995-e04d-4044-b1dc-c9aa27460397, published 18 September 2024. Source
  2. Mangeney P, Andriamialisoa RZ, Lallemand JY, Langlois N, Langlois Y, Potier P. 5'-Nor anhydrovinblastine. Tetrahedron. 1979;35(18):2175-2179. DOI
  3. Mangeney P, Andriamialisoa RZ, Langlois N, Langlois Y, Potier P. A new class of antitumor compounds: 5'-nor and 5',6'-seco derivatives of vinblastine-type alkaloids. The Journal of Organic Chemistry. 1979;44(22):3765-3768. DOI
  4. Fellous A, Ohayon R, Vacassin T, Binet S, Lataste H, Krikorian A, et al. Biochemical effects of Navelbine on tubulin and associated proteins. Semin Oncol. 1989;16(2 Suppl 4):9-14. PubMed
  5. Marty M, Extra JM, Espie M, Leandri S, Besenval M, Krikorian A. Advances in vinca-alkaloids: Navelbine. Nouv Rev Fr Hematol (1978). 1989;31(2):77-84. PubMed
  6. Krikorian A, Breillout F. Vinorelbine (Navelbine). A new semisynthetic vinca alkaloid. Onkologie. 1991;14(1):7-12. PubMed
  7. Budman DR. Vinorelbine (Navelbine): a third-generation vinca alkaloid. Cancer Invest. 1997;15(5):475-90. PubMedDOI
  8. Le Roux M, Guéritte F. From Catharanthus roseus Alkaloids to the Discovery of Vinorelbine (Navelbine®). Navelbine® and Taxotère®. 2017;:87-149. DOI
  9. U.S. Food and Drug Administration. Drugs@FDA: Approval date(s) and history, letters, labels, reviews for NDA 020388 (vinorelbine; Navelbine). Page read 2026-10-29. Source
  10. Winton T, Livingston R, Johnson D, Rigas J, Johnston M, Butts C, et al. Vinorelbine plus cisplatin vs. observation in resected non-small-cell lung cancer. N Engl J Med. 2005;352(25):2589-97. PubMedDOI
  11. Douillard JY, Rosell R, De Lena M, Carpagnano F, Ramlau R, Gonzáles-Larriba JL, et al. Adjuvant vinorelbine plus cisplatin versus observation in patients with completely resected stage IB-IIIA non-small-cell lung cancer (Adjuvant Navelbine International Trialist Association [ANITA]): a randomised controlled trial. Lancet Oncol. 2006;7(9):719-27. PubMedDOI