213Bi-[DOTA0, Tyr3]Octreotide Peptide Receptor Radionuclide Therapy of Pancreatic Tumors in a Preclinical Animal Model

Abstract

Bi-DOTATOC (specific activity 7.4 MBq/Ag) were investigated. Biodistribution studies to determine somatostatin receptor specificity were done in Lewis rats at 1and 3 hours postinjection. Histopathology of various organs was used to evaluated toxicity and safety. Therapeutic efficacy of 4 to 22 MBq Bi-DOTATOC showed significantly greater tumor reduction when compared with animals receiving <11MBq (P < 0.02). Conclusions:213 Bi-DOTATOC showed dose-related antitumor effects with minimal treatmentrelated organ toxicity. No acute or chronic hematologic toxicities were observed. Mild, acute nephrotoxicity was observed without evidence of chronic toxicity. 213Bi-DOTATOC is a promising therapeutic radiopharmaceutical for further evaluation.

Preclinical Evaluation of the α-Particle Generator Nuclide 225Ac for Somatostatin Receptor Radiotherapy of Neuroendocrine Tumors

“…Mild interstitial nephritis at 26 weeks after the application of 11 to 13 MBq of 213 Bi-DOTATOC was noted as a sign of chronic toxicity (15). Just like 225 Ac-DOTATOC, 213 Bi-DOTATOC compared favorably with 177 Lu-DOTATOC in vitro and displayed a higher therapeutic efficacy at the same absorbed dose (16), supporting the idea that a-emitting isotopes may help to improve the efficacy of PRRT in neuroendocrine tumors.…”

Pharmacokinetics and toxicity of 213Bi-labeled PAI2 in preclinical targeted alpha therapy for cancer

“…Some mild chronic nephropathy was observed for 11.4 MBq of 213 Bi-DOTATOC. 15 Radiation nephropathy is a process of necrosis, atrophy and sclerosis that follows exposure of the kidney to ionizing radiation. 16 A cell with sufficient DNA injury eventually dies after mitosis.…”

Radionuclide Therapy via SSTR: Future Aspects from Experimental Animal Studies

“…Glycosylated octreotide analogues have been labelled with 211 At, or 125 I, with maintained SSTR2 affinity and improved pharmacokinetics in AR42J-bearing rats [66,67]. 213 Bi-labelled DOTATOC has been produced and given promising therapeutic results in one animal model [68]. …”