Pharmacokinetics of glucarpidase in subjects with normal and impaired renal function

Marc Phillips, William Smith, Guhan Balan, Suzanne Ward

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

Glucarpidase (formerly known as carboxypeptidase G2 or CPG2) is being evaluated for the adjunctive treatment of patients experiencing, or at risk of, methotrexate toxicity attributable to its delayed elimination. Delayed elimination of methotrexate can occur in patients with methotrexate-induced renal toxicity. In this study, glucarpidase pharmacokinetics were assessed in volunteer subjects with normal (n = 8) and severely impaired (n = 4) renal function. Each subject received a single intravenous dose of glucarpidase 50 U/kg (equivalent to 114.5 μg/kg) infused over 5 minutes. The mean maximum serum concentration (Cmax) for glucarpidase in renally impaired subjects was 2.9 μ g/mL, the mean half-life (t1/2) was 10.0 hours, and the mean area under the serum concentration- time curve from time zero to infinity (AUC0-∞) was 24.5 μgxh/mL. Similar values were found in subjects with normal renal function (mean Cmax 3.1 μg/mL, mean t1/2 9.0 hours, and mean AUC0-∞ 23.4 μgxh/mL). The results indicated little effect of renal impairment on the serum pharmacokinetics of glucarpidase.

Original languageEnglish (US)
Pages (from-to)279-284
Number of pages6
JournalJournal of clinical pharmacology
Volume48
Issue number3
DOIs
StatePublished - Mar 1 2008

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Pharmacokinetics
Methotrexate
Kidney
gamma-Glutamyl Hydrolase
Serum
Half-Life
Volunteers
Therapeutics

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmacology (medical)

Cite this

Pharmacokinetics of glucarpidase in subjects with normal and impaired renal function. / Phillips, Marc; Smith, William; Balan, Guhan; Ward, Suzanne.

In: Journal of clinical pharmacology, Vol. 48, No. 3, 01.03.2008, p. 279-284.

Research output: Contribution to journalArticle

Phillips, Marc ; Smith, William ; Balan, Guhan ; Ward, Suzanne. / Pharmacokinetics of glucarpidase in subjects with normal and impaired renal function. In: Journal of clinical pharmacology. 2008 ; Vol. 48, No. 3. pp. 279-284.
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