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Kinetics of gallium nitrate, a new anticancer agent
Author(s) -
Hall Stephen W.,
Yeung Katherine,
Benjamin Robert S.,
Stewart David,
Valdivieso Manuel,
Bedikian Agop Y.,
Loo Ti Li
Publication year - 1979
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt197925182
Subject(s) - pharmacokinetics , gallium , chemotherapy , volume of distribution , renal function , urology , medicine , excretion , chemistry , urine , pharmacology , gastroenterology , surgery , organic chemistry
Pharmacokinetic studies were conducted in 8 patients with disseminated neoplasms refractory to conventional chemotherapy, who received gallium nitrate at doses of 300 to 600 mg/m 2 intravenously in a phase I clinical trial. Gallium concentrations in biological fluids were determined colorimetrically. In patients with normal renal function, gallium showed a biphasic plasma disappearance with an initial half‐life (t½) of 0.5 to 1.8 hr (mean 1.0) and a terminal t½ of 10.5 to 50.4 hr (mean 25.1). Gallium was distributed in total body water and often localized in some body compartment as evidenced by a volume of distribution ranging from 0.25 to 2.53 L/kg (mean 1.19). The total drug clearance from the plasma was 0.13 to 1.00 ml/kg/min (mean 0.65) in patients with normal renal function. Cumulative urinary excretion of gallium was 15% to 12% (mean 35%) of the administered dose in 24 hr (it fell to 23% in 8 days in a patient with acute oliguric renal failure). Gallium kinetics are altered in patients with acute renal dysfunction and in patients who have received multiple doses of gallium or other metal chemotherapy.