Pharmacokinetics of gallium nitrate in man.
Gallium nitrate is a new antineoplastic agent that has shown activity in a number of in vitro tumor systems. During a Phase I clinical trial, the pharmacokinetics of two methods of administration of gallium nitrate were studied: a seven-day continuous intravenous infusion, and a weekly rapid intravenous infusion. During the continuous infusion of 200 mg/M2 of gallium nitrate, plasma gallium concentrations of 0.9 +/- 0.2 microgram/ml in one patient, and 1.9 +/- 0.4 microgram/ml in a second were noted. Urine excretion of gallium approximated the daily administered dose by day 2-3. Overall, 68-107% of the total administered dose was recovered in the urine. Following a rapid intravenous infusion, a biphasic curve was generated. The T1/2 alpha ranged from 8.3-26 minutes; the T1/2 beta from 6.3-196 hours. From 69-91% of the administered dose was recovered in the urine. The effects of gallium nitrate on tissue localization and body retention of 67Ga are also presented.
D000293:Adolescent; D000368:Aged; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D004341:Drug Evaluation; D005260:Female; D005708:Gallium / Q000008:administration & dosage / Q000378:metabolism*; D006207:Half-Life; D006801:Humans; D007263:Infusions, Parenteral; D007700:Kinetics; D009369:Neoplasms / Q000378:metabolism*; D014018:Tissue Distribution
D000970:Antineoplastic Agents; D005708:Gallium; C027235:gallium nitrate