Delving into the Latest Updates on Fluorine-18-ML-10 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug, Diagnostic radiopharmaceuticals

Synonyms

ApoSense-PET

+ [1]

Target-

Mechanism

PET imaging(Positron-emission tomography enhancers)

Therapeutic Areas

NeoplasmsImmune System DiseasesNervous System Diseases+ [2]

Active Indication-

Inactive Indication

Brain metastasesNon-Hodgkin LymphomaStroke+ [1]

Originator Organization

Aposense Ltd.

Active Organization-

Inactive Organization

Aposense Ltd.

Centres de Médecine Nucléaire

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Background:
The new drug 18F-PF-06445974 has a little radioactivity. This can be seen by a positron emission tomography (PET) scan. The drug helps researchers see a protein, PDE4B, in the brain. Looking at PDE4B in the living brain might show how it is involved in psychiatric and neurological disorders. One part of the study will look at how the study drug is distributed in the brain. Another part will study how brain measures vary.
Objectives:
To measure the protein PDE4B in the brain. To test how a new radioactive chemical, 18F-PF-06445974, is distributed in the body.
Eligibility:
Healthy adults ages 18 and older
Design:
Participants will have 1-3 visits over a year. Each will be 2-5 hours.
Women will have a pregnancy test each time.

Start Date10 Jan 2017

Sponsor / Collaborator

National Institute of Mental Health

NCT01651520 / Unknown statusNot ApplicableIIT

Prognosis Value of the Neuronal Damage Detected by Positrons Emission Tomography (PET) With 11C-Flumazenil in Early Multiple Sclerosis.

In this study the investigators will use PET and 11C-Flumazenil to visualize and quantify neuronal injury in the cortex and the deep gray matter of Multiple Sclerosis patients at an early stage. The investigators will follow up patients to determine the prognostic value of this neuronal injury.

Start Date01 Jun 2013

Sponsor / Collaborator

Assistance Publique des Hôpitaux de Paris SA

EUCTR2010-019832-11-GB / Not yet recruitingNot Applicable

An open-label study to evaluate the utility of the apoptosis imaging biomarker [18F]ML-10 to assess the response to chemotherapy in patients with non Hodgkin's lymphoma. - Utility of ML10-PET imaging for Apoptosis Evaluation

Start Date13 Jul 2010

Sponsor / Collaborator

GlaxoSmithKline Research & Development Ltd.

100 Clinical Results associated with Fluorine-18-ML-10

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100 Translational Medicine associated with Fluorine-18-ML-10

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100 Patents (Medical) associated with Fluorine-18-ML-10

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27

Literatures (Medical) associated with Fluorine-18-ML-10

17 May 2023·Antimicrobial agents and chemotherapy

Modified Plasmodium falciparum Ring-Stage Survival Assay with ML10 Kinase Inhibitor.

Article

Author: Platon, Lucien ; Baker, David A ; Ménard, Didier

The ring-stage survival assay is the reference assay to measure in vitro Plasmodium falciparum artemisinin partial resistance. The main challenge of the standard protocol is to generate 0-to-3-h postinvasion ring stages (the stage least susceptible to artemisinin) from schizonts obtained by sorbitol treatment and Percoll gradient. We report here a modified protocol facilitating the production of synchronized schizonts when multiple strains are tested simultaneously, by using ML10, a protein kinase inhibitor, that reversibly blocks merozoite egress.

01 Jan 2022·Methods in Molecular Biology

Synchronisation of Plasmodium falciparum and P. knowlesi In Vitro Cultures Using a Highly Specific Protein Kinase Inhibitor

Article

Author: van Ooij, Christiaan ; Moon, Robert William ; Baker, David Andrew ; Ressurreição, Margarida

Synchronisation of Plasmodium cultures is essential to investigate the complexities of time-dependent events associated with the asexual blood stage of the malaria parasite life cycle. Here we describe a procedure using ML10, a highly specific inhibitor of the parasite cyclic GMP-dependent protein kinase (PKG), to attain high synchronicity of Plasmodium falciparum and P. knowlesi asexual blood-stage cultures and to obtain high levels of arrested mature schizonts as well as viable released merozoites. Additionally, we describe how to use ML10 to improve the transfection efficiency of P. falciparum parasites and also how to derive the half maximal effective concentration (EC₅₀) of ML10 in other P. falciparum laboratory lines and clinical isolates.

01 Feb 2016·Molecular Imaging and BiologyQ3 · MEDICINE

In Vivo Evaluation of Radiofluorinated Caspase-3/7 Inhibitors as Radiotracers for Apoptosis Imaging and Comparison with [18F]ML-10 in a Stroke Model in the Rat

Q3 · MEDICINE

Article

Author: Krause-Heuer, Anwen M ; Fraser, Benjamin H ; Matesic, Lidia ; Greguric, Ivan ; Touzani, Omar ; Dhilly, Martine ; Sobrio, Franck ; Barré, Louisa ; Delamare, Jérôme ; Médoc, Marie ; Toutain, Jérôme

PURPOSEThe first biological evaluation of two potent fluorine-18 radiolabelled inhibitors of caspase-3/7 was achieved in a cerebral stroke rat model to visualize apoptosis.PROCEDURESIn vivo characteristics of isatins [(18)F]-2 and [(18)F]-3 were studied and compared by μPET to previously described 1-[4-(2-[(18)F]fluoroethyl)benzyl]-5-(2-methoxymethylpyrrolidin-1-ylsulfonyl)isatin ([(18)F]-1) and to 2-(5-[(18)F]fluoropentyl)-2-methyl-malonic acid ([(18)F]ML-10) used as a reference radiotracer in a rat stroke model.RESULTS[(18)F]-2 and [(18)F]-3 were radiolabelled with high radiochemical purity and high specific radioactivity. Radioactivity uptakes in ischemic and contralateral brain regions were weak for the three radiolabelled isatins and lower for [(18)F]ML-10. In μPET, time activity curves showed significant uptake differences between both regions of interest for [(18)F]-1 after 45 min. No differences were observed for [(18)F]ML-10.CONCLUSIONSRadiolabelled isatins are more promising radiotracers to image apoptosis than [(18)F]ML-10 in this stroke animal model without craniectomy. In particular, [(18)F]-1 presented significant uptake in apoptotic area 45 min after administration.

100 Deals associated with Fluorine-18-ML-10

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Non-Hodgkin Lymphoma	Phase 2	GB	Centres de Médecine Nucléaire	20 Dec 2021
Stroke	Phase 2	GB	Centres de Médecine Nucléaire	20 Dec 2021
Brain metastases	Phase 2	-	Aposense Ltd.	01 Jul 2008
Brain metastases	Phase 2	-	Aposense Ltd.	01 Jul 2008
Unknown Primary Neoplasms	Phase 2	-	Aposense Ltd.	01 Jul 2008