Identification of the soluble in vivo metabolites of indium-111-diethylenetriaminepentaacetic acid-D-Phe1-octreotide

Bioconjugate Chemistry
L A BassC J Anderson

Abstract

Indium-111-diethylenetriaminepentaacetic Acid-D-phenylalanine-octreotide ([111]In-DTPA-octreotide) is a cyclic eight amino acid somatostatin analogue which is approved for gamma scintigraphy of neuroendocrine tumors. To address the factors that contribute to liver and kidney retention of this radiopharmaceutical, its metabolism was evaluated in normal and tumor-bearing rats. The soluble fractions from nontarget (liver and kidney) and target (tumor, pancreas, adrenals) organ homogenates were analyzed out to 21 h postinjection, and urine was analyzed out to 12 h postinjection. The blood was analyzed at shorter time intervals due to the rapid clearance of (111)In-DTPA-octreotide. Radio-TLC and HPLC were used to analyze organ homogenates, blood, and urine. By TLC, intact (111)In-DTPA-octreotide was resolved from the soluble metabolites, and a similar apparent rate of metabolism was observed in the liver, kidney, tumor, and pancreas with approximately 30% intact (111)In-DTPA-octreotide at 4 h postinjection. In the adrenals, metabolism occurred more slowly with approximately 60% intact (111)In-DTPAoctreotide at 4 h postinjection. At 4 h postinjection, the activity excreted in the urine consisted of 85% intact (111)In-DTPA-octreotide....Continue Reading

References

Feb 15, 1990·International Journal of Cancer. Journal International Du Cancer·J C ReubiV Macaulay
Sep 15, 1990·International Journal of Cancer. Journal International Du Cancer·J C ReubiJ Laissue
Aug 1, 1986·The Journal of Clinical Endocrinology and Metabolism·J C ReubiS W Lamberts
Dec 22, 1983·The New England Journal of Medicine·S Reichlin
Sep 15, 1994·Annals of the New York Academy of Sciences·E P KrenningA E Reijs
Jan 17, 1996·International Journal of Cancer. Journal International Du Cancer·P O ZamoraF F Knapp

❮ Previous
Next ❯

Citations

Sep 7, 2002·International Journal of Cancer. Journal International Du Cancer·Yubin MiaoThomas P Quinn
Jun 10, 2008·European Journal of Nuclear Medicine and Molecular Imaging·Georgios S LimourisLambros Vlahos
Jan 25, 2014·Bioorganic & Medicinal Chemistry·Nobuhiro OshimaKazue Ohkura
Oct 2, 2001·Nuclear Medicine and Biology·H AkizawaH Saji
Jan 23, 2014·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Lina Y HuJulie L Sutcliffe
Aug 29, 2006·Nuclear Medicine and Biology·Yubin MiaoThomas P Quinn
Feb 6, 2017·Nuclear Medicine and Biology·Nobuhiro OshimaKazue Ohkura
Jun 20, 2017·Natural Product Reports·Francesc Rabanal, Yolanda Cajal
Jan 15, 2005·Journal of Receptor and Signal Transduction Research·Alex N EberleSylvie Froidevaux
Apr 24, 2007·Der Orthopäde·G Delling
Feb 18, 2003·Endocrine Reviews·Leo J Hofland, Steven W J Lamberts
Dec 30, 2004·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Jennifer E SpragueCarolyn J Anderson
Feb 2, 2020·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Mark LubberinkAnders Sundin

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.