Description

Simple

A cancer chemotherapy medication used to treat a specific type of lung cancer that has spread in the body.

Clinical

A vinca alkaloid used in the treatment of metastatic non-small cell lung carcinoma (NSLC) and in conjunction with other drugs in locally advanced NSCLC.

Overview

Vinorelbine is an anti-mitotic chemotherapy drug that is used in the treatment of several types of malignancies, including breast cancer and non-small cell lung cancer (NSCLC) [5]. It was initially approved in the USA in 1990's for the treatment of NSCLC [13].

It is a third-generation vinca alkaloid. The introduction of third-generation drugs (vinorelbine, gemcitabine, taxanes) in platinum combination improved survival of patients with advanced NSCLC, with very similar results from the various drugs. Treatment toxicities are considerable in the combination treatment setting [2].

A study was done on the clearance rate of vinorelbine on individuals with various single polymorphonuclear mutations. It was found that there was 4.3-fold variation in vinorelbine clearance across the cohort, suggesting a strong influence of genetics on the clearance of this drug [7].

Pharmacology

Indication


Vinorelbine tartrate is indicated for adults in the treatment of advanced non-small cell lung cancer (NSCLC), as a single therapy or in combination with other chemotherapeutic drugs [5].

Used in relapsed or refra... Read more

Pharmacodynamic


Vinorelbine is a semi-synthetic vinca-alkaloid with a wide spectrum of anti-tumor activity. The vinca-alkaloids are considered spindle poisons. They work by interfering with the polymerization of tubulin, a protein responsible for building the microtubule system which appears during cell division... Read more

Mechanism of action

Vinca alkaloids are structurally similar compounds composed of two multi-ringed units, _vindoline_, and _catharanthine_. _Vinorelbine tartrate_ is a vinca alkaloid in which the catharanthine component is the target of structural modification [ Read more

Absorption

Vinorelbine is rapidly absorbed with peak serum concentration reached within 2 hours [5].

Vinorelbine is highly bound to platelets and lymphocytes and is also bound to alpha 1-acid glycoprotein, albumin, and lipopro... Read more

Protein binding

80-90% [6]

Volume of distribution

The volume of distribution is large, indicating extensive extravascular distribution [4].The steady-state volume of... Read more

Clearance

The plasma clearance of vinorelbine is high, approaching the same as hepatic blood flow in humans, and its volume of distribution is large, indicating extensive extravascular distribution. In comparison to vinblastine or vincristine [ Read more

Half life

The terminal phase half-life averaged 27.7 to 43.6 hours; the mean plasma clearances ranged from 0.97 to 1.26 L/hr/kg [4... Read more

Route of elimination

Vinorelbine undergoes substantial hepatic elimination in humans, with large amounts recovered in feces after intravenous administration to humans [5].

Urinary excretion of unchanged drug accounts for less than 20% o... Read more

Toxicity

Due to the wide array of adverse effects of this drug, the toxicity of is categorized into organ systems [5].

**Hematologic:** Granulocytopenia was the primary dose-limiting toxicity with vinorelbine tartrate therap... Read more

Adverse Effects

Contraindications

  • Route:
    • Intravenous
  • Hypersensitivity:
    • false
  • Regions: US

Food Interactions

    Information currently not available.

Interactions

Type in a drug name to check for interaction with Vinorelbine
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The risk or severity of bleeding can be increased when (R)-warfarin is combined with Vinorelbine.
(S)-Warfarin
The risk or severity of bleeding can be increased when (S)-Warfarin is combined with Vinorelbine.
2-Methoxyethanol
The risk or severity of adverse effects can be increased when Vinorelbine is combined with 2-Methoxyethanol.
4-hydroxycoumarin
The risk or severity of bleeding can be increased when 4-hydroxycoumarin is combined with Vinorelbine.
4-Methoxyamphetamine
The metabolism of 4-Methoxyamphetamine can be decreased when combined with Vinorelbine.
5-methoxy-N,N-dimethyltryptamine
The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Vinorelbine.
6-Deoxyerythronolide B
The serum concentration of Vinorelbine can be increased when it is combined with 6-Deoxyerythronolide B.
9-(N-methyl-L-isoleucine)-cyclosporin A
The risk or severity of adverse effects can be increased when Vinorelbine is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
Abatacept
The risk or severity of adverse effects can be increased when Vinorelbine is combined with Abatacept.
Abciximab
The risk or severity of bleeding can be increased when Abciximab is combined with Vinorelbine.
Abetimus
The risk or severity of adverse effects can be increased when Vinorelbine is combined with Abetimus.
Acebutolol
The metabolism of Acebutolol can be decreased when combined with Vinorelbine.
Acenocoumarol
The risk or severity of bleeding can be increased when Acenocoumarol is combined with Vinorelbine.
Acepromazine
Vinorelbine may increase the neurotoxic activities of Acepromazine.
Aceprometazine
Vinorelbine may increase the neurotoxic activities of Aceprometazine.
Acetaminophen
The metabolism of Acetaminophen can be decreased when combined with Vinorelbine.
Acetophenazine
Vinorelbine may increase the neurotoxic activities of Acetophenazine.
Acetyldigitoxin
Acetyldigitoxin may decrease the cardiotoxic activities of Vinorelbine.
Acetyldigoxin
Acetyldigoxin may decrease the cardiotoxic activities of Vinorelbine.
Acteoside
The risk or severity of adverse effects can be increased when Vinorelbine is combined with Acteoside.
14 References
  1. 1 . Marty M, Fumoleau P, Adenis A, Rousseau Y, Merrouche Y, Robinet G, Senac I, Puozzo C: Oral vinorelbine pharmacokinetics and absolute bioavailability study in patients with solid tumors. Ann Oncol. 2001 Nov;12(11):1643-9.PubMed: 11822766
  2. 2 . Piccirillo MC, Daniele G, Di Maio M, Bryce J, De Feo G, Del Giudice A, Perrone F, Morabito A: Vinorelbine for non-small cell lung cancer. Expert Opin Drug Saf. 2010 May;9(3):493-510. doi: 10.1517/14740331003774078.PubMed: 20350282
  3. 3 . Bahadori F, Topcu G, Eroglu MS, Onyuksel H: A new lipid-based nano formulation of vinorelbine. AAPS PharmSciTech. 2014 Oct;15(5):1138-48. doi: 10.1208/s12249-014-0146-3. Epub 2014 May 29.PubMed: 24871553
  4. 4 . Wargin WA, Lucas VS: The clinical pharmacokinetics of vinorelbine (Navelbine). Semin Oncol. 1994 Oct;21(5 Suppl 10):21-7.PubMed: 7973765
  5. 5 . Vinorelbine Tartrate Link
  6. 6 . Vinorelbine, Ontario Cancer Care Link
  7. 7 . Predictors of Vinorelbine Pharmacokinetics and Pharmacodynamics in Patients With Cancer Link
  8. 8 . Vinorelbine injection, Daily Med Link
  9. 9 . Metabolism pathway of vinorelbine (Navelbine®) in human: Characterisation of the metabolites by HPLC–MS/MS Link
  10. 10 . Vinca Alkaloid Pharmacokinetics Link
  11. 11 . Vinorelbine, a clinical review Link
  12. 12 . Vinorelbine FDA pharmacology review Link
  13. 13 . Drug Approval Package Link
  14. 14 . Navelbine, PDR Link