Human pharmacokinetics of WR-2721.
The pharmacokinetic properties of WR-2721 were investigated in 13 cancer patients given a 150 mg/M2 intravenous bolus dose of the drug. An average plasma clearance value of 2.17 L/min was obtained. Very little of the drug or the two metabolites, WR-1065 and WR-33278, were excreted in urine obtained after the blood collection schedule. Plasma concentrations of WR-2721 decreased by 94% within 6 minutes of drug administration. The mean value of 6.44 L obtained for the steady-state volume of distribution indicates that the extravascular space occupied by the drug is small. These observations suggest that in human cancer patients, WR-2721 is rapidly taken up by tissues and converted to metabolites.
D004999:Amifostine / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D008624:Mercaptoethylamines / Q000378:metabolism; D009369:Neoplasms / Q000378:metabolism*; D009946:Organothiophosphorus Compounds / Q000378:metabolism*; D011837:Radiation-Protective Agents / Q000378:metabolism*; D014018:Tissue Distribution
D008624:Mercaptoethylamines; D009946:Organothiophosphorus Compounds; D011837:Radiation-Protective Agents; C020174:N-(2-mercaptoethyl)-1,3-diaminopropane; D004999:Amifostine; C045611:WR 33278