Article

Long-term pharmacokinetics of thio-TEPA, TEPA and total alkylating activity following i. v. bolus administration of thio-TEPA in ovarian cancer patients

University of Trondheim
Cancer Chemotherapy and Pharmacology (impact factor: 2.83). 06/1990; 25(4):257-262. DOI:10.1007/BF00684882 pp.257-262

ABSTRACT The serum pharmacokinetics of unchanged thio-TEPA and the active metabolite TEPA and the urinary excretion of thio-TEPA, TEPA and total alkylating activity were studied after a single i. v. bolus injection of thio-TEPA in six ovarian cancer patients. TEPA was present in serum as of 5 min after drug administration, and its concentration rapidly reached a plateau in the range of 50–100 ng/ml. After about 3 h the serum concentration of TEPA exceeded that of thio-TEPA, and in five of the six patients the metabolite persisted longer than the parent drug in serum. AUCs of thio-TEPA and TEPA were 82283 and 1,084234 ng h/ml, respectively. The great interindividual variation encountered in the serum pharmacokinetics of TEPA may be of clinical importance and represents a further indication that pharmacokinetically guided dosing of thio-TEPA could be valuable. Urinary recoveries of both thio-TEPA and TEPA were low, together consituting

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Keywords

5 min
 
active metabolite TEPA
 
bolus injection
 
clinical importance
 
drug administration
 
great interindividual variation
 
metabolite
 
ovarian cancer patients
 
parent drug
 
pharmacokinetically
 
serum concentration
 
serum pharmacokinetics
 
single i
 
six patients
 
TEPA
 
thio-TEPA
 
total alkylating activity
 
unchanged thio-TEPA
 
urinary excretion
 
Urinary recoveries
 

Bjørn Hagen