[Clinical evaluation of safety, pharmacokinetics and dosimetry of the somatostatin analog 111In-DTPA-D-Phe-octreotide--report of the phase 1 study].

The safety, pharmacokinetics and dosimetry of the somatostatin analog 111In-DTPA-D-Phe-octreotide (111In-octreotide) were investigated in four young normal volunteers as phase 1 study in Japan. Neither adverse reactions nor significant changes of vital signs and clinical laboratory data were observed after intravenous injection of 111 MBq of 111In octreotide. The plasma clearance curve consisted of fast and slow exponential components with mean half life of 9.2 minutes and 2.2 hours, respectively. Seventy three percent of the injected dose were excreted in the urine by 24 hours after the injection of 111In-octreotide. With respect to the radiation dose to normal tissue, the most important organs were the urinary bladder, the kidney, the spleen and the liver. The effective dose equivalent was calculated as 3.26 +/- 0.43 mSv/37 MBq (mean +/- s.d.). This phase 1 study demonstrated the safety of scintigraphy with 111In-octreotide.