Variability in Teniposide Plasma Protein Binding Is Correlated With Serum Albumin Concentrations

William P. Petros, Mary V. Relling, Michael Christensen, Ching‐Hon ‐H Pui, Gaston K. Rivera, William E. Evans

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Abstract

Teniposide is a widely used anticancer drug that is extensively bound to plasma proteins (> 95%). We evaluated the drug's plasma protein binding in nine patients with acute lymphocytic leukemia who were in their first complete remission, and in a second group of nine patients at the time of relapse and subsequently after achieving another complete remission. Plasma protein binding was assessed by equilibrium dialysis, with direct high‐performance liquid chromatographic measurement of total and free teniposide. The mean unbound fraction was 0.44% (0.21–0.88%) in the plasma of patients in first remission. It was significantly higher in patients at the time of relapse (mean = 0.86%; range 0.68–1.08%) and after achieving another complete remission (mean = 1.25%; range 0.51–2.11%). Serum albumin values were significantly lower at the time of relapse (mean = 4.6 vs 4.0 mg/dl; p<0.014), and decreased further during intensive postremission therapy containing l‐asparaginase (mean = 3.2; p<0.05). For all 18 patients, a significant negative correlation (r2=0.667; p<0.001) was found between serum albumin and unbound teniposide, with low albumin being associated with higher unbound fraction. Such patients have higher systemic exposure to unbound (presumably active) teniposide at any given total plasma concentration of the agent. 1992 Pharmacotherapy Publications Inc.

Original languageEnglish (US)
Pages (from-to)273-277
Number of pages5
JournalPharmacotherapy: The Journal of Human Pharmacology and Drug Therapy
Volume12
Issue number4
DOIs
StatePublished - Jan 1 1992

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Teniposide
Protein Binding
Serum Albumin
Blood Proteins
Recurrence
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Pharmaceutical Preparations
Publications
Dialysis
Albumins
Drug Therapy

All Science Journal Classification (ASJC) codes

  • Pharmacology (medical)

Cite this

Variability in Teniposide Plasma Protein Binding Is Correlated With Serum Albumin Concentrations. / Petros, William P.; Relling, Mary V.; Christensen, Michael; Pui, Ching‐Hon ‐H; Rivera, Gaston K.; Evans, William E.

In: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, Vol. 12, No. 4, 01.01.1992, p. 273-277.

Research output: Contribution to journalArticle

Petros, William P. ; Relling, Mary V. ; Christensen, Michael ; Pui, Ching‐Hon ‐H ; Rivera, Gaston K. ; Evans, William E. / Variability in Teniposide Plasma Protein Binding Is Correlated With Serum Albumin Concentrations. In: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy. 1992 ; Vol. 12, No. 4. pp. 273-277.
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