Pharmacokinetics of VP16-213 given by different administration methods

M. D'Incalci, P. Farina, C. Sessa, C. Mangioni, V. Conter, G. Masera, M. Rocchetti, M. Brambilla Pisoni, E. Piazza, M. Beer, F. Cavalli

Research output: Contribution to journalArticle

Abstract

Plasma pharmacokinetics of VP16-213 were investigated after a 30-60 min infusion in 14 adult patients and six children. In adults the elimination half-life (T1/2 β), plasma clearance (Clp) and volume of distribution (Vd) were respectively 7.05±0.67 h, 26.8±2.4 ml/min/m2, and 15.7±1.8 l/m2; in children 3.37±0.5 h, 39.34±6.6 ml/min/m2, and 9.97±3.7 l/m2. After repeated daily doses no accumulation of VP16-213 was found in plasma. The unchanged drug found in the 24 h urine after administration amounted to 20-30% of the dose. In eight choriocarcinoma patients plasma levels of VP16-213 were measured after oral capsules and drinkable ampoules. The bioavailability compared to the i.v. route was variable, mean values being 57% for capsules and 91% for ampoules. In one further patient, with abnormal d-Xylose absorption results, VP16-213 was not detectable in plasma after the oral ampoule dose. Steady state levels investigated in three patients after 72 h continuous VP16-213 infusion (100 mg/m2/24 h) were around 2-5 μg/ml. Levels of VP16-213 were undetectable in CSF after i.v. or oral administration.

Original languageEnglish
Pages (from-to)141-145
Number of pages5
JournalCancer Chemotherapy and Pharmacology
Volume7
Issue number2-3
DOIs
Publication statusPublished - 1982

ASJC Scopus subject areas

  • Cancer Research
  • Oncology
  • Pharmacology

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    D'Incalci, M., Farina, P., Sessa, C., Mangioni, C., Conter, V., Masera, G., Rocchetti, M., Pisoni, M. B., Piazza, E., Beer, M., & Cavalli, F. (1982). Pharmacokinetics of VP16-213 given by different administration methods. Cancer Chemotherapy and Pharmacology, 7(2-3), 141-145. https://doi.org/10.1007/BF00254536