Chelators and metal complex stability for radiopharmaceutical applications

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Abstract

Diagnostic and therapeutic nuclear medicine relies heavily on radiometal nuclides. The most widely used and well-known radionuclide is technetium-99m ( ^99mTc), which has dominated diagnostic nuclear medicine since the advent of the ⁹⁹Mo/ ^99mTc generator in the 1960s. Since that time, many more radiometals have been developed and incorporated into potential radiopharmaceuticals. One critical aspect of radiometal-containing radiopharmaceuticals is their stability under in vivo conditions. The chelator that is coordinated to the radiometal is a key factor in determining radiometal complex stability. The chelators that have shown the most promise and are under investigation in the development of diagnostic and therapeutic radiopharmaceuticals over the last 5 years are discussed in this review.

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Most cited references 196

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Click Chemistry: Diverse Chemical Function from a Few Good Reactions

Hartmuth Kolb, M G Finn, K. Barry Sharpless … (2001)

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Phase 3 Trial of (177)Lu-Dotatate for Midgut Neuroendocrine Tumors.

Jonathan Strosberg, Ghassan El-Haddad, Edward Wolin … (2017)

Background Patients with advanced midgut neuroendocrine tumors who have had disease progression during first-line somatostatin analogue therapy have limited therapeutic options. This randomized, controlled trial evaluated the efficacy and safety of lutetium-177 ((177)Lu)-Dotatate in patients with advanced, progressive, somatostatin-receptor-positive midgut neuroendocrine tumors. Methods We randomly assigned 229 patients who had well-differentiated, metastatic midgut neuroendocrine tumors to receive either (177)Lu-Dotatate (116 patients) at a dose of 7.4 GBq every 8 weeks (four intravenous infusions, plus best supportive care including octreotide long-acting repeatable [LAR] administered intramuscularly at a dose of 30 mg) ((177)Lu-Dotatate group) or octreotide LAR alone (113 patients) administered intramuscularly at a dose of 60 mg every 4 weeks (control group). The primary end point was progression-free survival. Secondary end points included the objective response rate, overall survival, safety, and the side-effect profile. The final analysis of overall survival will be conducted in the future as specified in the protocol; a prespecified interim analysis of overall survival was conducted and is reported here. Results At the data-cutoff date for the primary analysis, the estimated rate of progression-free survival at month 20 was 65.2% (95% confidence interval [CI], 50.0 to 76.8) in the (177)Lu-Dotatate group and 10.8% (95% CI, 3.5 to 23.0) in the control group. The response rate was 18% in the (177)Lu-Dotatate group versus 3% in the control group (P<0.001). In the planned interim analysis of overall survival, 14 deaths occurred in the (177)Lu-Dotatate group and 26 in the control group (P=0.004). Grade 3 or 4 neutropenia, thrombocytopenia, and lymphopenia occurred in 1%, 2%, and 9%, respectively, of patients in the (177)Lu-Dotatate group as compared with no patients in the control group, with no evidence of renal toxic effects during the observed time frame. Conclusions Treatment with (177)Lu-Dotatate resulted in markedly longer progression-free survival and a significantly higher response rate than high-dose octreotide LAR among patients with advanced midgut neuroendocrine tumors. Preliminary evidence of an overall survival benefit was seen in an interim analysis; confirmation will be required in the planned final analysis. Clinically significant myelosuppression occurred in less than 10% of patients in the (177)Lu-Dotatate group. (Funded by Advanced Accelerator Applications; NETTER-1 ClinicalTrials.gov number, NCT01578239 ; EudraCT number 2011-005049-11 .).

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N-heterocyclic carbenes in late transition metal catalysis.

Silvia Díez-González, Steven P. Nolan, Nicolas Marion (2009)

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Author and article information

Journal

Title: Radiochimica Acta

Publisher: Walter de Gruyter GmbH

ISSN (Electronic): 2193-3405

ISSN (Print): 0033-8230

Publication date Created: September 25 2019

Publication date Created: September 01 2019

Publication date (Print): September 25 2019

Publication date (Electronic): July 20 2019

Publication date (Print): September 01 2019

Volume: 107

Issue: 9-11

Pages: 1087-1120

Affiliations

[1 ]Department of Chemistry , University of Missouri , Columbia, MO 65211 , USA

[2 ]University of Missouri Research Reactor Center , Columbia, MO 65211 , USA

Article

DOI: 10.1515/ract-2018-3090

SO-VID: 9c17a372-a738-4342-ac99-0fd8977c9dea

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