Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

4.1    Pharmacodynamic properties

Pharmacotherapeutic group: Vinca alkaloids and analogues - ATC code: L01 C A04 
Vinorelbine is an antineoplastic drug of the vinca alkaloid family but unlike all the other vinca alkaloids, the catharanthine moiety of vinorelbine has been structurally modified. At molecular level, it acts on the dynamic equilibrium of tubulin in the microtubular apparatus of the cell. It inhibits tubulin polymerization and binds preferentially to mitotic microtubules, affecting axonal microtubules at high concentrations only. The strength of tubulin spiralization is less than that produced by vincristine.
Vinorelbine blocks mitosis in G2-M, causing cell death in interphase or in the following mitosis.

The safety and efficacy of Vinorelbine in paediatric patients have not been established.
Clinical data from two single arm Phase II studies using intravenous vinorelbine in 33 and 46 paediatric patients with recurrent solid tumours, including rhabdomyosarcoma, other soft tissue sarcoma, Ewing sarcoma, liposarcoma, synovial sarcoma, fibrosarcoma, central nervous system cancer, osteosarcoma, neuroblastoma at doses of 30 to 33.75 mg/m² D1 and D8 every 3 weeks or once a week for 6 weeks every 8 weeks, showed no meaningful clinical activity.
The toxicity profile was similar to that reported in adult patients (see section 4.2).

Pharmacokinetic Properties