Delving into the Latest Updates on [18F]THK-5105 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

TAU

Mechanism

TAU modulators(Microtubule-associated protein tau modulators), PET imaging(Positron-emission tomography enhancers)

Therapeutic Areas

Nervous System Diseases

Active Indication

Alzheimer Disease

Inactive Indication-

Originator Organization

Tohoku University

Active Organization

Tohoku University

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC20H21FN2O2

InChIKeyYECXMTCPEPHEAA-GJQNQZCXSA-N

CAS Registry1374108-16-3

PURPOSENoninvasive imaging of tau and amyloid-β pathologies would facilitate diagnosis of Alzheimer's disease (AD). Recently, we have developed [(18)F]THK-5105 for selective detection of tau pathology by positron emission tomography (PET). The purpose of this study was to clarify biological properties of optically pure [(18)F]THK-5105 enantiomers.PROCEDURESBinding for tau aggregates in AD brain section was evaluated by autoradiography (ARG). In vitro binding assays were performed to evaluate the binding properties of enantiomers for AD brain homogenates. The pharmacokinetics in the normal mouse brains was assessed by ex vivo biodistribution assayRESULTSThe ARG of enantiomers showed the high accumulation of radioactivity corresponding to the distribution of tau deposits. In vitro binding assays revealed that (S)-[(18)F]THK-5105 has slower dissociation from tau than (R)-[(18)F]THK-5105. Biodistribution assays indicated that (S)-[(18)F]THK-5105 eliminated faster from the mouse brains and blood compared with (R)-[(18)F]THK-5105.CONCLUSION(S)-[(18)F]THK-5105 could be more suitable than (R)-enantiomer for a tau imaging agent.

100 Deals associated with [18F]THK-5105

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