TECHNETIUM-99M-LABELED N-(2,6-DIMETHYLPHENYLCARBAMOYLMETHYL) IMINODIACETIC ACID (TC-99M HIDA) - NEW RADIOPHARMACEUTICAL FOR HEPATOBILIARY IMAGING STUDIES

Abstract

An easily formulated, stable kit preparation of technetium-99m HIDA suitable for use in humans, was developed and tested in mice and dogs. The tracer was cleared rapidly from the blood and excreted predominantly by the liver in both species. In dogs, hepatobiliary clearance of Tc-99m HIDA was significantly greater than that of 14C HIDA and 113Sn HIDA. The LD50 for HIDA in mice, 168 mg/kg, exceeded the average human dose by a factor of 1000 on a per-weight basis. Blood clearance curves for Tc-99m HIDA in 12 normal subjects were biexponential with half-times of 4.6 .+-. 1.0 min and 31.5 .+-. 7.0 min, and cumulative 90-min urine samples contained 14.2 .+-. 1.8% of the injected dose. Images in normal subjects and nonjaundiced patients showed rapid concentration of tracer by the liver, and activity was present within the biliary system in 10-20 min. In jaundiced patients, the tracer blood clearance was delayed and urinary excretion increased, but intestinal activity, indicating biliary patency, was imaged in those patients without complete focal obstruction of the common duct. Technetium-99m HIDA is a nontoxic radiopharmaceutical useful for clinical evaluation of hepatobiliary disorders in humans.