Vinorelbine Tartrate
Medicinal Chemistry
Pharmacognosy
Biological Source
Semi-synthetic from Catharanthus roseus (Madagascar Periwinkle)
Active Constituents
Anhydrovinblastine (Precursor)
Pharmacology & Synthesis
Mechanism of Action
Binds specifically to tubulin, inhibiting assembly of microtubules and arresting cells in metaphase (shows high affinity for mitotic microtubules over axonal microtubules).
Pharmacokinetics (ADME)
A: Incomplete oral absorption; typically administered IV.
D: High binding to platelets and lymphocytes, extensive tissue Vd.
M: Hepatic via CYP3A4.
E: Biliary and fecal.
Pharmacodynamics
Cytotoxic to rapidly dividing cells; particularly active against non-small cell lung cancer (NSCLC).
Synthesis Pathway
Semi-synthetic modification involving the structural dehydration of the catharanthine moiety.
Safety, Warnings & Interactions
Adverse Effects
Granulocytopenia (dose-limiting), mild peripheral neuropathy, nausea, vomiting, injection site reactions.
Contraindications
Severe baseline granulocytopenia, severe hepatic impairment, current infection.
Drug Interactions
CYP3A4 inhibitors, prior extensive radiation therapy.