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

Overview

Basic Info

Drug Type

Small molecule drug, Diagnostic radiopharmaceuticals

Synonyms-

Target

tissue factor

Action

inhibitors

Mechanism

tissue factor inhibitors(Tissue factor inhibitors)

Therapeutic Areas

Neoplasms

Active Indication

Neoplasms

Inactive Indication-

Originator Organization

Rigshospitalet

Active Organization

Rigshospitalet

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Activated factor VII blocked in the active site with Phe–Phe–Arg–chloromethyl ketone (active site inhibited factor VII (ASIS)) is a 50‐kDa protein that binds with high affinity to its receptor, tissue factor (TF). TF is a transmembrane glycoprotein that plays an important role in, for example, thrombosis, metastasis, tumor growth, and tumor angiogenesis. The aim of this study was to develop an 18F‐labeled ASIS derivative to assess TF expression in tumors.Active site inhibited factor VII was labeled using N‐succinimidyl‐4‐[18F]fluorobenzoate, and the [18F]ASIS was purified on a PD‐10 desalting column. The radiochemical yield was 25 ± 6%, the radiochemical purity was >97%, and the pseudospecific radioactivity was 35 ± 9 GBq/µmol. The binding efficacy was evaluated in pull‐down experiments, which monitored the binding of unlabeled ASIS and [18F]ASIS to TF and to a specific anti‐factor VII antibody (F1A2‐mAb). No significant difference in binding efficacy between [18F]ASIS and ASIS could be detected. Furthermore, [18F]ASIS was relatively stable in vitro and in vivo in mice.In conclusion, [18F]ASIS has for the first time been successfully synthesized as a possible positron emission tomography tracer to image TF expression levels. In vivo positron emission tomography studies to evaluate the full potential of [18F]ASIS are in progress.

100 Deals associated with 18F-ASIS

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