The phase I/II trial assess the safety and efficacy of a new positron emission tomography (PET) test for early diagnosis of lung cancer. This study uses PET and Me-4FDG new glucose tracer (alpha-methyl-4-deoxy-4-[(18)F]fluoro-D-glucopyranoside) designed specifically to determine glucose update into cells in the body. PET is a non-invasive imaging method used to detect cancer in patient. Me4FDG is a radioactive glucose tracer used in PET to locate cells in the body taking up glucose by SGLT2. SLGT2 is a sodium glucose transport protein that accumulates glucose in some cells, e.g. kidney cells and tumors. This study may help researcher determine how effective PET with ME4FDG tracer works in detecting lung cancer.

Start Date19 Jan 2023

Sponsor / Collaborator

Jonsson Comprehensive Cancer Center

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100 Clinical Results associated with Alpha-methyl-4-deoxy-4-[(18)F]fluoro-D-glucopyranoside

100 Translational Medicine associated with Alpha-methyl-4-deoxy-4-[(18)F]fluoro-D-glucopyranoside

100 Patents (Medical) associated with Alpha-methyl-4-deoxy-4-[(18)F]fluoro-D-glucopyranoside

Literatures (Medical) associated with Alpha-methyl-4-deoxy-4-[(18)F]fluoro-D-glucopyranoside

01 Mar 2024·Journal of Nuclear Medicine

It’s a Trap! Aldolase-Prescribed C₄Deoxyradiofluorination Affords Intracellular Trapping and the Tracing of Fructose Metabolism by PET

Article

Author: Shuhendler, Adam ; Addison, Christina L ; Kirby, Alexia ; Charlton, Thomas A ; Calvert, Nicholas D ; Graf, Dominic ; Suchý, Mojmír ; Ben, Robert N

Fructose metabolism has been implicated in various diseases, including metabolic disorders, neurodegenerative disorders, cardiac disorders, and cancer. However, the limited availability of a quantitative imaging radiotracer has hindered its exploration in pathology and diagnostic imaging. Methods: We adopted a molecular design strategy based on the catalytic mechanism of aldolase, a key enzyme in fructolysis. We successfully synthesized a radiodeoxyfluorinated fructose analog, [¹⁸F]4-fluoro-4-deoxyfructose ([¹⁸F]4-FDF), in high molar activity. Results: Through heavy isotope tracing by mass spectrometry, we demonstrated that C₄-deoxyfluorination of fructose led to effective trapping as fluorodeoxysorbitol and fluorodeoxyfructose-1-phosphate in vitro, unlike C₁- and C₆-fluorinated analogs that resulted in fluorolactate accumulation. This observation was consistent in vivo, where [¹⁸F]6-fluoro-6-deoxyfructose displayed substantial bone uptake due to metabolic processing whereas [¹⁸F]4-FDF did not. Importantly, [¹⁸F]4-FDF exhibited low uptake in healthy brain and heart tissues, known for their high glycolytic activity and background levels of [¹⁸F]FDG uptake. [¹⁸F]4-FDF PET/CT allowed for sensitive mapping of neuro- and cardioinflammatory responses to systemic lipopolysaccharide administration. Conclusion: Our study highlights the significance of aldolase-guided C₄ radiodeoxyfluorination of fructose in enabling effective radiotracer trapping, overcoming limitations of C₁ and C₆ radioanalogs toward a clinically viable tool for imaging fructolysis in highly glycolytic tissues.

01 Aug 2023·European journal of nuclear medicine and molecular imaging

Excretion of glucose analogue with SGLT2 affinity predicts response effectiveness to sodium glucose transporter 2 inhibitors in patients with type 2 diabetes mellitus.

Article

Author: Geist, Barbara Katharina ; Kautzky-Willer, Alexandra ; Brath, Helmut ; Yu, Josef ; Hacker, Marcus ; Rasul, Sazan ; Nics, Lukas ; Zisser, Lucia ; Patronas, Eva Maria ; Fueger, Barbara

PURPOSESodium-glucose cotransporter 2 inhibitor (SGLT2i) regulation, developed as treatment for patients with type 2 diabetes, can be imaged with the glucose analogue alpha-methyl-4-deoxy-4-[¹⁸F]fluoro-D-glucopyranoside (Me4FDG), a positron emission tomography (PET) tracer with a high affinity for SGLT1 and SGLT2 proteins. With regard to therapy effectiveness, we aimed to investigate whether clinical parameters or Me4FDG excretion could predict response to SGLT2i in patients with type 2 diabetes.METHODSIn a longitudinal, prospective study, 19 patients with type 2 diabetes underwent Me4FDG combined PET and magnetic resonance imaging (PET/MRI) scans at baseline and 2 weeks after initiation of therapy with SGLT2i, accompanied by the collection of blood and urine samples. Me4FDG-excretion was determined from the Me4FDG uptake in the bladder. Long-term response was determined by HbA1c level after 3 months; a strong response to the therapy was defined as a reduction of HbA1c by at least 10% from baseline.RESULTSSGLT2i resulted in significantly increased Me4FDG excretion (4.8 vs. 45.0, P < 0.001) and urine glucose (56 vs. 2806 mg/dl, P < 0.001). Baseline urine glucose and baseline Me4FDG excretion correlated both with long-term decline in HbA1c with r = 0.55 (P < 0.05). However, only Me4FDG excretion was a predictor of a strong response to SGLT2i (P = 0.005, OR 1.9).CONCLUSIONSUsing Me4FDG-PET, we demonstrated for the first time renal SGLT2-related excretion before and after short-term SGLT2i treatment. In contrary to other clinical parameters, SGLT2-related excretion before treatment was a robust predictor of long-term HbA1c response in patients with type 2 diabetes, suggesting that therapy effectiveness is only dependent of endogenous SGLT2 processes.

01 Jan 2022·Molecular Imaging

In Vivo Functional Assessment of Sodium-Glucose Cotransporters (SGLTs) Using [¹⁸F]Me4FDG PET in Rats

Article

Author: Lapa, Constantin ; Chen, Xinyu ; Pomper, Martin G. ; Sasaki, Takanori ; Nose, Naoko ; Werner, Rudolf A. ; Rowe, Steven P. ; Arias-Loza, Paula ; Matsusaka, Yohji ; Higuchi, Takahiro

Background. Mediating glucose absorption in the small intestine and renal clearance, sodium glucose cotransporters (SGLTs) have emerged as an attractive therapeutic target in diabetic patients. A substantial fraction of patients, however, only achieve inadequate glycemic control. Thus, we aimed to assess the potential of the SGLT-targeting PET radiotracer alpha-methyl-4-deoxy-4-[18F]fluoro-D-glucopyranoside ([18F]Me4FDG) as a noninvasive intestinal and renal biomarker of SGLT-mediated glucose transport. Methods. We investigated healthy rats using a dedicated small animal PET system. Dynamic imaging was conducted after administration of the reference radiotracer 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG), or the SGLT-targeting agent, [18F]Me4FDG either directly into the digestive tract (for assessing intestinal absorption) or via the tail vein (for evaluating kidney excretion). To confirm the specificity of [18F]Me4FDG and responsiveness to treatment, a subset of animals was also pretreated with the SGLT inhibitor phlorizin. In this regard, an intraintestinal route of administration was used to assess tracer absorption in the digestive tract, while for renal assessment, phlorizin was injected intravenously (IV). Results. Serving as reference, intestinal administration of [18F]FDG led to slow absorption with retention of [Formula: see text]% of administered radioactivity at 15 min. [18F]Me4FDG, however, was rapidly absorbed into the blood and cleared from the intestine within 15 min, leading to markedly lower tracer retention of [Formula: see text]% ([Formula: see text]). Intraintestinal phlorizin led to marked increase of [18F]Me4FDG uptake (15 min, [Formula: see text]%; [Formula: see text] vs. untreated controls), supporting the notion that this PET agent can measure adequate SGLT inhibition in the digestive tract. In the kidneys, radiotracer was also sensitive to SGLT inhibition. After IV injection, [18F]Me4FDG reabsorption in the renal cortex was significantly suppressed by phlorizin when compared to untreated animals (%ID/g at 60 min, [Formula: see text] vs. untreated controls, [Formula: see text]; [Formula: see text]). Conclusion. As a noninvasive read-out of the concurrent SGLT expression in both the digestive tract and the renal cortex, [18F]Me4FDG PET may serve as a surrogate marker for treatment response to SGLT inhibition. As such, [18F]Me4FDG may enable improvement in glycemic control in diabetes by PET-based monitoring strategies.

100 Deals associated with Alpha-methyl-4-deoxy-4-[(18)F]fluoro-D-glucopyranoside

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Indication	Highest Phase	Country/Location	Organization	Date
Adenocarcinoma of Lung	Phase 2	US	Jonsson Comprehensive Cancer Center	19 Jan 2023
Lung Cancer	Phase 2	US	Jonsson Comprehensive Cancer Center	19 Jan 2023

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