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We propose a focused, prospective pilot clinical imaging trial to evaluate 11C-Gln PET/CT followed by 18F-FSPG PET/CT in 20 HNSCC patients. Imaging metrics that are common to PET (e.g. SUVmax, peak or mean) will be determined.
This study will also allow the acquisition of additional safety and biodistribution data, as, to date, only a limited number of patients have been evaluated with 11C-Gln as a direct PET imaging biomarker of Gln uptake. To date, no adverse side effects have been observed. We do not anticipate any toxicity since this tracer is a naturally-occurring essential amino acid in high abundance and is administered at sub-pharmacologic doses.
A long-term goal of these preliminary studies is to validate the utility of Gln PET imaging metrics for HNSCC and to expand this imaging technique to additional patients in prospective cohorts of patients with HNSCC.

Start Date14 Sep 2022

Sponsor / Collaborator

The University of Texas MD Anderson Cancer Center

NCT02379377

/ RecruitingPhase 1IIT

PET Imaging of Hepatocellular Carcinoma With 18F-FSPG

This clinical trial studies fluorine F 18 L-glutamate derivative BAY94-9392 (18F-FSPG) positron emission tomography (PET) in imaging patients with liver cancer before undergoing surgery or transplant. Diagnostic procedures, such as 18F-FSPG PET, may help find and diagnose liver cancer and find out how far the disease has spread.

Start Date15 Feb 2022

Sponsor / Collaborator

The University of Texas MD Anderson Cancer Center

[+1]

NCT03275974

/ Active, not recruitingPhase 1IIT

Glutamine PET Imaging of Colorectal Cancer

The clinical trial studies how well 11C-glutamine and 18F-FSPG positron emission tomography (PET) imaging works in detecting tumors in patients with metastatic colorectal cancer compared to standard imaging methods such as magnetic resonance imaging (MRI) or computed tomography (CT) scanning.

Start Date27 Apr 2021

Sponsor / Collaborator

The University of Texas MD Anderson Cancer Center

100 Clinical Results associated with BAY-94-9392

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100 Translational Medicine associated with BAY-94-9392

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100 Patents (Medical) associated with BAY-94-9392

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5

Literatures (Medical) associated with BAY-94-9392

01 Jun 2013·Journal of Nuclear MedicineQ1 · MEDICINE

(S)-4-(3-¹⁸F-Fluoropropyl)-l-Glutamic Acid: An ¹⁸F-Labeled Tumor-Specific Probe for PET/CT Imaging—Dosimetry

Q1 · MEDICINE

Article

Author: Wagner, Franziska Martina ; Krause, Bernd Joachim ; Hultsch, Christina ; Smolarz, Kamilla ; Sparks, Richard B. ; Bacher-Stier, Claudia ; Graner, Frank-Philipp ; Dinkelborg, Ludger M. ; Fels, Lueder ; Ramsay, Susan ; Schwaiger, Markus

The glutamic acid derivative (S)-4-(3-(18)F-Fluoropropyl)-l-glutamic acid ((18)F-FSPG, alias BAY 94-9392), a new PET tracer for the detection of malignant diseases, displayed promising results in non-small cell lung cancer patients. The aim of this study was to provide dosimetry estimates for (18)F-FSPG based on human whole-body PET/CT measurements.METHODS(18)F-FSPG was prepared by a fully automated 2-step procedure and purified by a solid-phase extraction method. PET/CT scans were obtained for 5 healthy volunteers (mean age, 59 y; age range, 51-64 y; 2 men, 3 women). Human subjects were imaged for up to 240 min using a PET/CT scanner after intravenous injection of 299 ± 22.5 MBq of (18)F-FSPG. Image quantification, time-activity data modeling, estimation of normalized number of disintegrations, and production of dosimetry estimates were performed using the RADAR (RAdiation Dose Assessment Resource) method for internal dosimetry and in general concordance with the methodology and principles as presented in the MIRD 16 document.RESULTSBecause of the renal excretion of the tracer, the absorbed dose was highest in the urinary bladder wall and kidneys, followed by the pancreas and uterus. The individual organ doses (mSv/MBq) were 0.40 ± 0.058 for the urinary bladder wall, 0.11 ± 0.011 for the kidneys, 0.077 ± 0.020 for the pancreas, and 0.030 ± 0.0034 for the uterus. The calculated effective dose was 0.032 ± 0.0034 mSv/MBq. Absorbed dose to the bladder and the effective dose can be reduced significantly by frequent bladder-voiding intervals. For a 0.75-h voiding interval, the bladder dose was reduced to 0.10 ± 0.012 mSv/MBq, and the effective dose was reduced to 0.015 ± 0.0010 mSv/MBq.CONCLUSIONOn the basis of the distribution and biokinetic data, the determined radiation dose for (18)F-FSPG was calculated to be 9.5 ± 1.0 mSv at a patient dose of 300 MBq, which is of similar magnitude to that of (18)F-FDG (5.7 mSv). The effective dose can be reduced to 4.5 ± 0.30 mSv (at 300 MBq), with a bladder-voiding interval of 0.75 h.

01 Jan 2013·Journal of Nuclear MedicineQ1 · MEDICINE

(4S)-4-(3-¹⁸F-Fluoropropyl)-l-Glutamate for Imaging of x_C^¯ Transporter Activity in Hepatocellular Carcinoma Using PET: Preclinical and Exploratory Clinical Studies

Q1 · MEDICINE

Article

Author: Baek, Sora ; Mueller, Andre ; Gong, Gyungyub ; Kim, Jae Seung ; Lee, Seung Jin ; Ryu, Jin-Sook ; Lim, Young-Suk ; Lee, Han Chu ; Moon, Dae Hyuk ; Lee, Young-Joo ; Bacher-Stier, Claudia ; Koglin, Norman ; Fels, Luder ; Schatz, Christoph A. ; Oh, Seung Jun ; Dinkelborg, Ludger M.

(4S)-4-(3-(18)F-fluoropropyl)-l-glutamate ((18)F-FSPG, or BAY 94-9392) is a new tracer to assess system x(C)(¯) transporter activity with PET. The aim of this study was to explore the tumor detection rate of (18)F-FSPG, compared with that of (18)F-FDG, in patients with hepatocellular carcinoma (HCC).METHODSPreclinically, in vivo HCC models of orthotopically implanted Huh7 and MH3924a cancer cells were studied with (18)F-FSPG in Naval Medical Research Institute nude mice (n = 3) and August-Copenhagen Irish rats (n = 4), respectively. Clinically, 5 patients with HCC who had hyper- or isometabolic lesions on (18)F-FDG PET were enrolled for evaluation of the tracer. Dynamic whole-body PET images with (18)F-FSPG were acquired for up to 120 min after injection of approximately 300 MBq of (18)F-FSPG. Immunohistochemical expression levels of the xCT subunit of the system x(C)(¯) and CD44 of HCC were studied in 4 patients with HCC.RESULTSStrong tumor uptake and low background from nontarget tissue allowed excellent tumor visualization in animal models with orthotopically implanted liver tumors. (18)F-FSPG PET procedures were well tolerated in all patients. (18)F-FSPG PET and (18)F-FDG detected lesions in 5 of 5 and 3 of 5 patients, respectively. The maximal standardized uptake values (SUV) were comparable ((18)F-FSPG, 4.7 ± 3.2; (18)F-FDG, 6.1 ± 2.9). The ratios of maximal SUV of the tumor to mean SUV of normal liver were also comparable ((18)F-FSPG, 3.6 ± 2.2; (18)F-FDG, 2.7 ± 1.3), but the mean SUV of normal liver of (18)F-FSPG was significantly lower than that of (18)F-FDG (P < 0.05). Two patients with HCC who showed both xCT and CD44 expression had moderate or intense accumulation of (18)F-FSPG, but the remaining 2 patients with negative CD44 expression showed mild uptake.CONCLUSION(18)F-FSPG was successfully translated from preclinical evaluation into patients with HCC. (18)F-FSPG may be a promising tumor PET agent with a high cancer detection rate in patients with HCC.

01 Oct 2012·Clinical Cancer ResearchQ1 · MEDICINE

Exploratory Clinical Trial of (4S)-4-(3-[18F]fluoropropyl)-l-glutamate for Imaging xC− Transporter Using Positron Emission Tomography in Patients with Non–Small Cell Lung or Breast Cancer

Q1 · MEDICINE

Article

Author: Lee, Jong Won ; Gong, Gyungyub ; Gambhir, Sanjiv S. ; Dinkelborg, Ludger M. ; Choi, Chang-Min ; Hultsch, Christina ; Baek, Sora ; Bacher-Stier, Claudia ; Fels, Lüder ; Oh, Seung Jun ; Koglin, Norman ; Ryu, Jin-Sook ; Schatz, Christoph A. ; Mittra, Erik S. ; Moon, Dae Hyuk ; Ahn, Sei Hyun

AbstractPurpose: (4S)-4-(3-[18F]fluoropropyl)-l-glutamate (BAY 94-9392, alias [18F]FSPG) is a new tracer to image xC− transporter activity with positron emission tomography (PET). We aimed to explore the tumor detection rate of [18F]FSPG in patients relative to 2-[18F]fluoro-2-deoxyglucose ([18F]FDG). The correlation of [18F]FSPG uptake with immunohistochemical expression of xC− transporter and CD44, which stabilizes the xCT subunit of system xC−, was also analyzed.Experimental Design: Patients with non–small cell lung cancer (NSCLC, n = 10) or breast cancer (n = 5) who had a positive [18F]FDG uptake were included in this exploratory study. PET images were acquired following injection of approximately 300 MBq [18F]FSPG. Immunohistochemistry was done using xCT- and CD44-specific antibody.Results: [18F]FSPG PET showed high uptake in the kidney and pancreas with rapid blood clearance. [18F]FSPG identified all 10 NSCLC and three of the five breast cancer lesions that were confirmed by pathology. [18F]FSPG detected 59 of 67 (88%) [18F]FDG lesions in NSCLC, and 30 of 73 (41%) in breast cancer. Seven lesions were additionally detected only on [18F]FSPG in NSCLC. The tumor-to-blood pool standardized uptake value (SUV) ratio was not significantly different from that of [18F]FDG in NSCLC; however, in breast cancer, it was significantly lower (P < 0.05). The maximum SUV of [18F]FSPG correlated significantly with the intensity of immunohistochemical staining of xC− transporter and CD44 (P < 0.01).Conclusions: [18F]FSPG seems to be a promising tracer with a relatively high cancer detection rate in patients with NSCLC. [18F]FSPG PET may assess xC− transporter activity in patients with cancer. Clin Cancer Res; 18(19); 5427–37. ©2012 AACR.

100 Deals associated with BAY-94-9392

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Advanced Triple-Negative Breast Carcinoma	Discovery	US	National Cancer Institute	01 Jul 2015
B-Cell Lymphoma	Discovery	US	National Cancer Institute	01 Jul 2015
Breast Cancer 3	Discovery	US	National Cancer Institute	01 Jul 2015
Metastatic breast cancer	Discovery	US	National Cancer Institute	01 Jul 2015
metastatic non-small cell lung cancer	Discovery	US	National Cancer Institute	01 Jul 2015
Metastatic Renal Cell Carcinoma	Discovery	US	National Cancer Institute	01 Jul 2015
Non-small cell lung cancer stage IIIA	Discovery	US	National Cancer Institute	01 Jul 2015
Multiple Pulmonary Nodules	Discovery	US	National Cancer Institute	16 Jun 2015
Smoking Cessation	Discovery	US	National Cancer Institute	16 Jun 2015
Solitary Pulmonary Nodule	Discovery	US	National Cancer Institute	16 Jun 2015

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Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02448225 (CTgov)	Phase 2	Lung Cancer \| Smoking Cessation \| Solitary Pulmonary Nodule \| Multiple Pulmonary Nodules	46	fluorodeoxyglucose F-18+Fluorine F 18 L-glutamate Derivative BAY94-9392	opypruvrdi(grdemlzkvd) = fzshxrwrxq cjpokvcxsq (icuqfnxysk, jkykeauqxq - mijkivowvd) View more	-	10 May 2022
NCT01103310 \| NCT01186601 (Pubmed \| Clin Cancer Res)	Phase 1	Recurrent Prostate Carcinoma xCT \| CD44	20	18F-FSPG3-[18F]Fluoropropyl)-L-glutamate (18F-FSPG) (18F-FSPG PET)	lwpmqoqrnz(mreqzyctld) = vvzxfgkfen zisyplkptz (ktxgnfmvqb )	Positive	15 Oct 2020
NCT02599194 (CTgov)	Phase 2	Metastatic Renal Cell Carcinoma \| Non-small cell lung cancer stage IIIA \| Mesothelioma \| B-Cell Lymphoma \| Non-small cell lung cancer stage IIIB \| Metastatic breast cancer \| metastatic non-small cell lung cancer \| Advanced Triple-Negative Breast Carcinoma \| Breast Cancer 3	7	18F-FDG+18F-FSPG	edjsqitmao(nufbxmsmvm) = qysbbdbhuh talyzwtflb (yttfrmcmfb, cdxcjnyywn - gouutaecat) View more	-	03 Jan 2019
AACR2012	Not Applicable	Neoplasms	-	FSPG (BAY 94-9392)	wlmrdklqer(lbgbengxlv) = significant correlation between FSPG uptake and protein expression of both the xCT subunit and CD44 ssdfrleenz (vpwzlzmjhf )	-	15 Apr 2012