A Clinical PET Imaging Tracer ([18F]DASA-23) to Monitor Pyruvate Kinase M2–Induced Glycolytic Reprogramming in Glioblastoma

Pyruvate kinase M2 (PKM2) catalyzes the final step in glycolysis, a key process of cancer metabolism. PKM2 is preferentially expressed by glioblastoma (GBM) cells with minimal expression in healthy brain. We describe the development, validation, and translation of a novel PET tracer to study PKM2 in...

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Published inClinical cancer research Vol. 27; no. 23; pp. 6467 - 6478
Main Authors Beinat, Corinne, Patel, Chirag B., Haywood, Tom, Murty, Surya, Naya, Lewis, Castillo, Jessa B., Reyes, Samantha T., Phillips, Megan, Buccino, Pablo, Shen, Bin, Park, Jun Hyung, Koran, Mary Ellen I., Alam, Israt S., James, Michelle L., Holley, Dawn, Halbert, Kim, Gandhi, Harsh, He, Joy Q., Granucci, Monica, Johnson, Eli, Liu, Daniel Dan, Uchida, Nobuko, Sinha, Rahul, Chu, Pauline, Born, Donald E., Warnock, Geoffrey I., Weissman, Irving, Hayden-Gephart, Melanie, Khalighi, Mehdi, Massoud, Tarik F., Iagaru, Andrei, Davidzon, Guido, Thomas, Reena, Nagpal, Seema, Recht, Lawrence D., Gambhir, Sanjiv Sam
Format Journal Article
LanguageEnglish
Published United States 01.12.2021
Subjects
Animals
Brain Neoplasms - pathology
Diazonium Compounds
Glioblastoma - pathology
Glycolysis
Humans
Mice
Positron-Emission Tomography - methods
Pyruvate Kinase - metabolism
Sulfanilic Acids
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Abstract Pyruvate kinase M2 (PKM2) catalyzes the final step in glycolysis, a key process of cancer metabolism. PKM2 is preferentially expressed by glioblastoma (GBM) cells with minimal expression in healthy brain. We describe the development, validation, and translation of a novel PET tracer to study PKM2 in GBM. We evaluated 1-((2-fluoro-6-[ F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([ F]DASA-23) in cell culture, mouse models of GBM, healthy human volunteers, and patients with GBM. [ F]DASA-23 was synthesized with a molar activity of 100.47 ± 29.58 GBq/μmol and radiochemical purity >95%. We performed initial testing of [ F]DASA-23 in GBM cell culture and human GBM xenografts implanted orthotopically into mice. Next, we produced [ F]DASA-23 under FDA oversight, and evaluated it in healthy volunteers and a pilot cohort of patients with glioma. In mouse imaging studies, [ F]DASA-23 clearly delineated the U87 GBM from surrounding healthy brain tissue and had a tumor-to-brain ratio of 3.6 ± 0.5. In human volunteers, [ F]DASA-23 crossed the intact blood-brain barrier and was rapidly cleared. In patients with GBM, [ F]DASA-23 successfully outlined tumors visible on contrast-enhanced MRI. The uptake of [ F]DASA-23 was markedly elevated in GBMs compared with normal brain, and it identified a metabolic nonresponder within 1 week of treatment initiation. We developed and translated [ F]DASA-23 as a new tracer that demonstrated the visualization of aberrantly expressed PKM2 for the first time in human subjects. These results warrant further clinical evaluation of [ F]DASA-23 to assess its utility for imaging therapy-induced normalization of aberrant cancer metabolism.
AbstractList Pyruvate kinase M2 (PKM2) catalyzes the final step in glycolysis, a key process of cancer metabolism. PKM2 is preferentially expressed by glioblastoma (GBM) cells with minimal expression in healthy brain. We describe the development, validation, and translation of a novel PET tracer to study PKM2 in GBM. We evaluated 1-((2-fluoro-6-[18F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([18F]DASA-23) in cell culture, mouse models of GBM, healthy human volunteers, and patients with GBM.PURPOSEPyruvate kinase M2 (PKM2) catalyzes the final step in glycolysis, a key process of cancer metabolism. PKM2 is preferentially expressed by glioblastoma (GBM) cells with minimal expression in healthy brain. We describe the development, validation, and translation of a novel PET tracer to study PKM2 in GBM. We evaluated 1-((2-fluoro-6-[18F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([18F]DASA-23) in cell culture, mouse models of GBM, healthy human volunteers, and patients with GBM.[18F]DASA-23 was synthesized with a molar activity of 100.47 ± 29.58 GBq/μmol and radiochemical purity >95%. We performed initial testing of [18F]DASA-23 in GBM cell culture and human GBM xenografts implanted orthotopically into mice. Next, we produced [18F]DASA-23 under FDA oversight, and evaluated it in healthy volunteers and a pilot cohort of patients with glioma.EXPERIMENTAL DESIGN[18F]DASA-23 was synthesized with a molar activity of 100.47 ± 29.58 GBq/μmol and radiochemical purity >95%. We performed initial testing of [18F]DASA-23 in GBM cell culture and human GBM xenografts implanted orthotopically into mice. Next, we produced [18F]DASA-23 under FDA oversight, and evaluated it in healthy volunteers and a pilot cohort of patients with glioma.In mouse imaging studies, [18F]DASA-23 clearly delineated the U87 GBM from surrounding healthy brain tissue and had a tumor-to-brain ratio of 3.6 ± 0.5. In human volunteers, [18F]DASA-23 crossed the intact blood-brain barrier and was rapidly cleared. In patients with GBM, [18F]DASA-23 successfully outlined tumors visible on contrast-enhanced MRI. The uptake of [18F]DASA-23 was markedly elevated in GBMs compared with normal brain, and it identified a metabolic nonresponder within 1 week of treatment initiation.RESULTSIn mouse imaging studies, [18F]DASA-23 clearly delineated the U87 GBM from surrounding healthy brain tissue and had a tumor-to-brain ratio of 3.6 ± 0.5. In human volunteers, [18F]DASA-23 crossed the intact blood-brain barrier and was rapidly cleared. In patients with GBM, [18F]DASA-23 successfully outlined tumors visible on contrast-enhanced MRI. The uptake of [18F]DASA-23 was markedly elevated in GBMs compared with normal brain, and it identified a metabolic nonresponder within 1 week of treatment initiation.We developed and translated [18F]DASA-23 as a new tracer that demonstrated the visualization of aberrantly expressed PKM2 for the first time in human subjects. These results warrant further clinical evaluation of [18F]DASA-23 to assess its utility for imaging therapy-induced normalization of aberrant cancer metabolism.CONCLUSIONSWe developed and translated [18F]DASA-23 as a new tracer that demonstrated the visualization of aberrantly expressed PKM2 for the first time in human subjects. These results warrant further clinical evaluation of [18F]DASA-23 to assess its utility for imaging therapy-induced normalization of aberrant cancer metabolism.
Pyruvate kinase M2 (PKM2) catalyzes the final step in glycolysis, a key process of cancer metabolism. PKM2 is preferentially expressed by glioblastoma (GBM) cells with minimal expression in healthy brain. We describe the development, validation, and translation of a novel PET tracer to study PKM2 in GBM. We evaluated 1-((2-fluoro-6-[ F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([ F]DASA-23) in cell culture, mouse models of GBM, healthy human volunteers, and patients with GBM. [ F]DASA-23 was synthesized with a molar activity of 100.47 ± 29.58 GBq/μmol and radiochemical purity >95%. We performed initial testing of [ F]DASA-23 in GBM cell culture and human GBM xenografts implanted orthotopically into mice. Next, we produced [ F]DASA-23 under FDA oversight, and evaluated it in healthy volunteers and a pilot cohort of patients with glioma. In mouse imaging studies, [ F]DASA-23 clearly delineated the U87 GBM from surrounding healthy brain tissue and had a tumor-to-brain ratio of 3.6 ± 0.5. In human volunteers, [ F]DASA-23 crossed the intact blood-brain barrier and was rapidly cleared. In patients with GBM, [ F]DASA-23 successfully outlined tumors visible on contrast-enhanced MRI. The uptake of [ F]DASA-23 was markedly elevated in GBMs compared with normal brain, and it identified a metabolic nonresponder within 1 week of treatment initiation. We developed and translated [ F]DASA-23 as a new tracer that demonstrated the visualization of aberrantly expressed PKM2 for the first time in human subjects. These results warrant further clinical evaluation of [ F]DASA-23 to assess its utility for imaging therapy-induced normalization of aberrant cancer metabolism.
Author Thomas, Reena
Naya, Lewis
Recht, Lawrence D.
Hayden-Gephart, Melanie
He, Joy Q.
Chu, Pauline
Haywood, Tom
Johnson, Eli
Khalighi, Mehdi
Castillo, Jessa B.
Halbert, Kim
Holley, Dawn
Gandhi, Harsh
Born, Donald E.
Gambhir, Sanjiv Sam
Alam, Israt S.
Patel, Chirag B.
James, Michelle L.
Weissman, Irving
Reyes, Samantha T.
Koran, Mary Ellen I.
Shen, Bin
Liu, Daniel Dan
Phillips, Megan
Iagaru, Andrei
Beinat, Corinne
Massoud, Tarik F.
Davidzon, Guido
Nagpal, Seema
Granucci, Monica
Warnock, Geoffrey I.
Buccino, Pablo
Sinha, Rahul
Murty, Surya
Park, Jun Hyung
Uchida, Nobuko
AuthorAffiliation 3 Division of Nuclear Medicine and Molecular Imaging, Department of Radiology, Stanford University, Stanford, CA 94305, USA
7 Department of Pathology, Neuropathology, Stanford University School of Medicine, Stanford, CA, 94305, USA
10 Departments of Bioengineering and Materials Science & Engineering, Stanford University, Stanford, CA 94305, USA
4 Stanford Institute for Stem Cell Biology and Regenerative Medicine, Department of Pathology, Stanford University School of Medicine, Stanford, CA, 94305, USA
1 Department of Radiology, Molecular Imaging Program at Stanford, Stanford University School of Medicine, Stanford, CA 94305, USA
5 Department of Neurosurgery, Stanford University School of Medicine, Stanford, CA, 94305, USA
8 PMOD Technologies Ltd, Zurich, Switzerland
2 Department of Neurology and Neurological Sciences, Stanford University School of Medicine, Stanford, CA 94305, USA
6 Stanford Human Research Histology Core, Stanford University School of Medicine, Stanford, CA, 94305, USA
9 Divisi
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Snippet Pyruvate kinase M2 (PKM2) catalyzes the final step in glycolysis, a key process of cancer metabolism. PKM2 is preferentially expressed by glioblastoma (GBM)...
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SubjectTerms Animals
Brain Neoplasms - pathology
Diazonium Compounds
Glioblastoma - pathology
Glycolysis
Humans
Mice
Positron-Emission Tomography - methods
Pyruvate Kinase - metabolism
Sulfanilic Acids
Title A Clinical PET Imaging Tracer ([18F]DASA-23) to Monitor Pyruvate Kinase M2–Induced Glycolytic Reprogramming in Glioblastoma
URI https://www.ncbi.nlm.nih.gov/pubmed/34475101
https://www.proquest.com/docview/2569383697
https://pubmed.ncbi.nlm.nih.gov/PMC8639752
Volume 27
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