Brands, Medical Use, Clinical Data
Brands / Synonyms
EPT; Etoposide; Etoposide Usp26; PTG; Teniposide [Usan:Ban:Inn]; Teniposido [Inn-Spanish]; Teniposidum [Inn-Latin]; Vee M-26; Veham-Sandoz; Vehem; Vumon; Vumon
Treatment of refractory acute lymphoblastic leukaemia
Teniposide is a phase-specific cytotoxic drug, acting in the late S or early G 2 phase of the cell cycle, thus preventing cells from entering mitosis. Teniposide causes dose-dependent single- and double-stranded breaks in DNA and DNA: protein cross-links. The mechanism of action appears to be related to the inhibition of type II topoisomerase activity since teniposide does not intercalate into DNA or bind strongly to DNA.
Mechanism of Action
Binds to and inhibits DNA topoisomerase II. The cytotoxic effects of teniposide are related to the relative number of double-stranded DNA breaks produced in cells, which are a reflection of the stabilization of a topoisomerase II-DNA intermediate.
Biotrnasformation / Drug Metabolism
VUMON is generally contraindicated in patients who have demonstrated a previous hypersensitivity to teniposide
and/or Cremophor® EL (polyoxyethylated castor oil).
Drug Interactions: In a study in which 34 different drugs were tested, therapeutically relevant
concentrations of tolbutamide, sodium salicylate and sulfamethizole displaced protein-bound teniposide in fresh human
serum to a small but significant extent. Because of the extremely high binding of teniposide to plasma proteins,
these small decreases in binding could cause substantial increases in free drug levels in plasma which could result
in potentiation of drug toxicity. Therefore, caution should be used in administering VUMON (teniposide injection) to
patients receiving these other agents. There was no change in the plasma kinetics of teniposide when coadministered
with methotrexate. However, the plasma clearance of methotrexate was slightly increased. An increase in intracellular
levels of methotrexate was observed in vitro in the presence of teniposide.