Eva M. Molina Trinidad, Consuelo Arteaga de Murphy, Helgi Jung-Cook Eduardo Murphy-Stack, Martha Pedraza-López, José Luis Morales-Márquez, Guadalupe Vertiz Serrano. Therapeutic 188Re-lanreotide: Determination of Radiopharmacokinetics Parameters in rats. Journal Pharmacy and Pharmacology. 2010, 62:1-6. DOI: 10.1211/jpp.62.04.0007
Objectives The radiopharmacokinetic parameters of the therapeutic radiopharmaceutical 188Re-lanreotide were compared in rats implanted with hepatocarcinoma tumours (n= 18) and healthy rats (n= 18).Methods Rats were injected with approximately 1.8 MBq 188Re-lanreotide (0.1 ml) via the tail vein and blood samples were obtained. The activity per gram of tissue (%IA/g) was calculated and the radiopharmacokinetic parameters determined. Data were fitted using a two-compartment model.Key findings Significant differences were found between healthy and hepatoma rats for beta elimination half-life (22.56 vs 48.14 h); transference constants K10 (ke) (6.44 vs 3.05 h-1) and K12 (2.76 vs 7.09 h-1); volume of distribution (2.06 vs 5.45 ml); mean residence time (66.58 vs 95.50 h) and apparent volume of distribution at steady state (131.30 vs 810.37 ml). The tumour/organ ratios after 24 h were 11.20 for tumour/muscle, 8.00 for tumour/liver and 7.72 for tumour/bone. The scintigraphic images obtained therefore had high resolution.Conclusions188Re-lanreotide had a prolonged beta elimination half-life and increased volume of distribution in rats with hepatocellular carcinoma. This may be beneficial in the diagnosis and therapy of metastatic lesions in patients with cancer.