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Pharmacokinetics of (-)-(S)-bromofosfamide after intravenous and oral administration in mice.

Abstract
(-)-(S)-Bromofosfamide ((2S)-(2-chloroethylamino)-3-(2-bromoethyl)-1,3,2-oxazaphosphorinane 2-oxide, CAS 146452-37-1, CBM-11) is a new potential anti-cancer drug, currently under investigation. Its pharmacokinetics and bioavailability were studied in female mice following intravenous and oral administration of the dose of 50 mg/kg. The compound was extracted from plasma samples using chloroform and analyzed by high-performance liquid chromatography with UV detection at 200 nm. Orally administered (-)-(S)-bromofosfamide was absorbed quickly, attaining a maximum level of 33.9 micrograms/ml at 5 min, and was eliminated with a half-life (t1/2) of about 0.9 h. The average half-life of intravenously administered (-)-(S)-bromofosfamide was about 0.7 h. The total plasma clearance (CL) and volume of distribution (Vd) were found to be 0.14 l/h and 4.92 l/kg, respectively. The absolute bioavailability of (-)-(S)-bromofosfamide after oral administration was 105%.
AuthorsK Kobylińska, M Kobylińska, B Sobik
JournalArzneimittel-Forschung (Arzneimittelforschung) Vol. 51 Issue 7 Pg. 596-9 ( 2001) ISSN: 0004-4172 [Print] Germany
PMID11505792 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Antineoplastic Agents, Alkylating
  • bromofosfamide
  • Ifosfamide
Topics
  • Administration, Oral
  • Animals
  • Antineoplastic Agents, Alkylating (administration & dosage, pharmacokinetics)
  • Area Under Curve
  • Biological Availability
  • Chromatography, High Pressure Liquid
  • Female
  • Half-Life
  • Ifosfamide (administration & dosage, analogs & derivatives, pharmacokinetics)
  • Injections, Intravenous
  • Mice
  • Spectrophotometry, Ultraviolet

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