Pharmacokinetic, Dosimetry and Toxicity Study of ¹⁷⁷Lu-EDTMP in Patients: Phase 0/I study

Current Radiopharmaceuticals
Chandrasekhar BalM R A Pillai

Abstract

177Lu-EDTMP has been proposed as a potent bone pain palliation agent owing to theoretical advantage of reduced bone marrow suppression resulting from the low β(-) energy and a suitably long half-life facilitating its wider distribution with less loss from radioactive decay. Herein, we report the pharmacokinetics, dosimetry and toxicity analysis of 177Lu-EDTMP in patients (phase-0/I study). In a phase-0 study, the biokinetics of skeletal and non-skeletal uptake of 177Lu-EDTMP was assessed in 6 patients with metastatic prostate cancer using tracer doses (172.7-206.9MBq). Data of whole skeletal uptake, blood and fractionated urine samples were obtained and dosimetric calculations were performed using the OLINDA/EXM 1.0 software. Prolonged bone retention was observed in all patients. Excretion was mainly via the renal route and blood clearance was rapid and biphasic. Mean estimated red marrow dose was 0.80±0.15mGy/MBq while mean total-body dose was 0.16±0.04mGy/MBq. A maximum tolerated dose (MTD) of 2000-3250MBqfor 177Lu-EDTMP was calculated. For the phase-I study, 21 patients with metastatic prostate cancer were given a therapeutic dose of 177Lu- EDTMP (692-5550MBq). Toxiciy (WHO), evaluated by assessment of hemoglobin levels, pla...Continue Reading

Citations

Jul 25, 2018·Minerva urologica e nefrologica = The Italian journal of urology and nephrology·Wei M OngHomayoun Zargar
Jul 5, 2019·The Quarterly Journal of Nuclear Medicine and Molecular Imaging : Official Publication of the Italian Association of Nuclear Medicine (AIMN) [and] the International Association of Radiopharmacology (IAR), [and] Section of the Society of Radiopharmaceutica·Pradeep Thapa, Sandip Basu
Sep 10, 2020·Nature Reviews. Drug Discovery·Tal BurtYuichi Sugiyama
Feb 12, 2020·International Journal of Radiation Biology·Hesham M H ZakalyMichael Zhukovsky
Dec 2, 2020·Cancer Biotherapy & Radiopharmaceuticals·Emran AskariRamin Sadeghi
Jul 3, 2021·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Mostafa Y A MostafaM Zhukovsky

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