Substance

ID:245

Names and Identifiers
Brand Name
Navelbine BaseNavelbine
IUPAC name
methyl (1R,9R,10S,11R,12R,19R)-11-(acetyloxy)-12-ethyl-4-[(12S)-16-ethyl-12-(methoxycarbonyl)-1,10-diazatetracyclo[12.3.1.0^{3,11}.0^{4,9}]octadeca-3(11),4,6,8,15-pentaen-12-yl]-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.0^{1,9}.0^{2,7}.0^{16,19}]nonadeca-2(7),3,5,13-tetraene-10-carboxylate
Synonyms
Vinorelbinum [Latin]Vinorelbine TartrateVinorelbine DitartaratevinorelbineVinorelbina [Spanish]Vinorelbine BitartrateVinorelbine DitartrateVinorelbineVinorelbin
IUPAC Traditional name
NVB
Registration numbers
CAS Number
71486-22-1
Properties
Physical Property
Hydrophobicity(logP)
4
Molecule Details
Drug Groups
approved; investigational
Description
Vinorelbine (Navelbine®) is an anti-mitotic chemotherapy drug that is given as a treatment for some types of cancer, including breast cancer and non-small cell lung cancer. [Wikipedia]
Indication
For the treatment of non-small-cell lung carcinoma.
Pharmacology
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.
Affected Organisms
Humans and other mammals
Half Life
27.7-43.6 hours
Protein Binding
~27%
Elimination
Vinorelbine undergoes substantial hepatic elimination in humans, with large amounts recovered in feces after intravenous administration to humans.
Distribution
* 25.4 to 40.1 L/kg
Clearance
* 0.97 - 1.26 L/hr/kg
References
• 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]
External Links
• [Wikipedia]
• [RxList]
• [Drugs.com]
Molecular Spectra
No Data Available
Click here to submit data
References
• 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
Navigation