Delving into the Latest Updates on 18F-FMAU with Synapse

Overview

Basic Info

Drug Type

Small molecule drug, Diagnostic radiopharmaceuticals

Synonyms

Target-

Action-

Mechanism-

Therapeutic Areas

NeoplasmsUrogenital DiseasesNervous System Diseases+ [3]

Active Indication

Prostatic CancerBrain metastasesColonic Cancer+ [7]

Inactive Indication-

Originator Organization

The University of Texas at Austin

Active Organization

National Cancer Institute

The University of Texas at Austin

Inactive Organization

National Institute For Biomedical Imaging And Bioengineering (Nibib)

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC10H13FN2O5

InChIKeyGBBJCSTXCAQSSJ-MSYRQUNGSA-N

CAS Registry241144-93-4

This early phase I trial tests the use of a radioactive tracer (a drug that is visible during an imaging test) known as 18F-FMAU, for imaging with positron emission tomography/computed tomography (PET/CT) in patients with brain cancer or cancer that has spread to the brain (brain metastases). A PET/CT scan is an imaging test that uses a small amount of radioactive tracer (given through the vein) to take detailed pictures of areas inside the body where the tracer is taken up. 18F-FMAU may also help find the cancer and how far the disease has spread. Magnetic resonance imaging (MRI) is a type of imaging test used to diagnose brain tumors. 18F-FMAU PET/CT in addition to MRI may make the finding and diagnosing of brain tumor easier.

Start Date15 Feb 2021

Sponsor / Collaborator

University of Southern California

[+1]

NCT02809690

/ TerminatedPhase 1IIT

Pilot Feasibility Study of 18F-FMAU PET for Diagnosing and Characterizing Prostate Cancer

This pilot clinical trial studies how well fluorine F 18 d-FMAU (18F-FMAU) positron emission tomography (PET)/computed tomography (CT) works in diagnosing and characterizing prostate cancer. A PET/CT scan is an imaging test that uses a small amount of radioactive tracer that is given through the vein to take detailed pictures of areas inside the body where the tracer is taken up. Radiotracers such as 18F-FMAU may help to find the cancer and see how far the disease has spread.

Start Date12 Sep 2016

Sponsor / Collaborator

University of Southern California

[+2]

100 Clinical Results associated with 18F-FMAU

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100 Translational Medicine associated with 18F-FMAU

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100 Patents (Medical) associated with 18F-FMAU

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30

Literatures (Medical) associated with 18F-FMAU

12 Feb 2021·ACS Pharmacology & Translational Science

Exploring Solvent Effects in the Radiosynthesis of ¹⁸F-Labeled Thymidine Analogues toward Clinical Translation for Positron Emission Tomography Imaging

Article

Author: Van Valkenburgh, Juno ; Li, Jindian ; Chen, Kai ; Conti, Peter S.

Thymidine analogues, 5-substituted 2'-deoxy-2'-[¹⁸F]fluoro-arabinofuranosyluracil derivatives, are promising positron emission tomography (PET) tracers being evaluated for noninvasive imaging of cancer cell proliferation and/or reporter gene expression. We report the radiosynthesis of 2'-deoxy-2'-[¹⁸F]fluoro-5-methyl-1-β-d-arabinofuranosyluracil ([¹⁸F]FMAU) and other 2'-deoxy-2'-[¹⁸F]fluoro-5-substituted-1-β-d-arabinofuranosyluracil analogues using 1,4-dioxane to replace the currently used 1,2-dichloroethane. Compared to 1,2-dichloroethane, 1,4-dioxane is analyzed as a better solvent in terms of radiochemical yield and toxicity concern. The use of a less toxic solvent allows for the translation of the improved approach to clinical production. The new radiolabeling method can be applied to an extensive range of uses for ¹⁸F-labeling of other nucleoside analogues.

15 Jan 2019·Clinical Cancer ResearchQ1 · MEDICINE

Biomarkers and Bone Imaging Dynamics Associated with Clinical Outcomes of Oral Cabozantinib Therapy in Metastatic Castrate-Resistant Prostate Cancer

Q1 · MEDICINE

Article

Author: Podgorski, Izabela ; Heath, Elisabeth I. ; Stark, Karri ; Smith, Daryn W. ; Lawhorn-Crews, Jawana M. ; Boerner, Julie ; Heilbrun, Lance K. ; Shields, Anthony F. ; Vaishampayan, Ulka N. ; Dobson, Kimberlee C. ; Fontana, Joseph A.

AbstractPurpose:Cabozantinib is a multitargeted tyrosine kinase inhibitor that demonstrated remarkable responses on bone scan in metastatic prostate cancer. Randomized trials failed to demonstrate statistically significant overall survival (OS). We studied the dynamics of biomarker changes with imaging and biopsies pretherapy and posttherapy to explore factors that are likely to be predictive of efficacy with cabozantinib.Experimental Design: Eligibility included patients with metastatic castrate-resistant prostate cancer with normal organ function and performance status 0–2. Cabozantinib 60 mg orally was administered daily. Pretherapy and 2 weeks post, 99mTc-labeled bone scans, positron emission tomography with 18F-sodium fluoride (NaF-PET) and 18F-(1-(2′-deoxy-2′-fluoro-β-D-arabinofuranosyl) thymine (FMAU PET) scans were conducted. Pretherapy and posttherapy tumor biopsies were conducted, and serum and urine bone markers were measured.Results:Twenty evaluable patients were treated. Eight patients had a PSA decline, of which 2 had a decline of ≥50%. Median progression-free survival (PFS) and OS were 4.1 and 11.2 months, respectively, and 3 patients were on therapy for 8, 10, and 13 months. The NaF-PET demonstrated a median decline in SUVmax of −56% (range, −85 to −5%, n = 11) and −41% (range, −60 to −25%, n = 9) for patients who were clinically stable and remained on therapy for ≥4 or <4 cycles, respectively. The FMAU PET demonstrated a median decline in SUVmax of −44% (−60 to −14%) and −42% (−63% to −23%) for these groups. The changes in bone markers and mesenchymal epithelial transition/MET testing did not correlate with clinical benefit.Conclusions:Early changes in imaging and tissue or serum/urine biomarkers did not demonstrate utility in predicting clinical benefit with cabozantinib therapy.

01 Nov 2018·Pharmaceutical Patent Analyst

Therapeutic Use of Fluorinated Nucleosides – Progress in Patents

Review

Author: Slusarczyk, Magdalena ; Bassetto, Marcella

Fluorinated nucleosides constitute a large class of chemotherapeutics approved for clinical use. The pharmacokinetic and pharmacodynamic properties of a drug can be affected, as a consequence of modulation of electronic, lipophilic and steric parameters, by the introduction of fluorine into the structure of drug-like molecule. Herein, we focus on fluorinated-nucleoside analogs, their therapeutic use and applications based on the patent literature from 2014 to 2018. We briefly discuss the clinical properties of anticancer and antiviral fluorine-containing nucleos(t)ides US FDA-approved or in development, and highlight their resistance mechanisms and limitations in the clinic. We emphasize patent inventions related to improved synthetic methods toward selected nucleos(t)ide analogs including the phosphoramidate sofosbuvir and 18F-labeled nucleosides FLT and FMAU, used as a 18F-PET tracers.

100 Deals associated with 18F-FMAU

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB14913

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Brain metastases	Phase 1	United States	National Cancer Institute	15 Feb 2021
Colonic Cancer	Phase 1	United States	National Cancer Institute	15 Feb 2021
Glioma	Phase 1	United States	National Cancer Institute	15 Feb 2021
Melanoma, Cutaneous Malignant	Phase 1	United States	National Cancer Institute	15 Feb 2021
Metastatic breast cancer	Phase 1	United States	National Cancer Institute	15 Feb 2021
Metastatic Colorectal Carcinoma	Phase 1	United States	National Cancer Institute	15 Feb 2021
Metastatic Lung Cancer	Phase 1	United States	National Cancer Institute	15 Feb 2021
Metastatic melanoma	Phase 1	United States	National Cancer Institute	15 Feb 2021
Renal Cell Carcinoma	Phase 1	United States	National Cancer Institute	15 Feb 2021
Prostatic Cancer	Phase 1	-	The University of Texas at Austin	-