This study was performed to demonstrate the quantitative in vivo assessment of human pharmacokinetics of 90Y-radiotherapeutics using the positron-emitting substitute 86Y and PET. This technique is illustrated in a patient with disseminated bone metastases from breast cancer who was injected with 100 MBq of 86Y-citrate as an analog of the commercially available radiotherapeutic 90Y-citrate. Whole-body distribution was measured with a PET camera 4, 10, 21, 28 and 45 hr postinjection. Uptake data were determined from reconstructed transverse PET images by regions of interest placed in normal bone tissue, liver and metastases. Images of coronal and sagittal whole-body sections were obtained by reformatting the transverse PET images. The ratio of activity concentration in metastases to that in normal bone ranged from 1.5:1 to 3.5:1. Of the injected tracer, 13.4% was found in the skeleton and 0.43% in the metastasis with the highest 86Y concentration. Radiation doses per 1 MBq of injected 90Y-citrate were calculated from 86Y-citrate data and data from MIRD pamphlets 5 and 11. The doses were 1.01 MGy/MBq for red marrow, 593 microGy/MBq for the liver and approximately 3.5 MGy/MBq for the most conspicuous metastases. This study demonstrates that the use of PET via 86Y allows an individual in vivo quantification of activity uptake and radiation dose of both normal tissue and tumor in pain treatment with 90Y-labeled radiotherapeutics.