Flortaucipir F-18

DB14914ApprovedInvestigationalSmall molecule

Flortaucipir F-18 is a small lipophilic tracer containing [18F]fluoride capable of crossing the blood-brain barrier and binding to aggregated tau protein; used in PET imaging for the diagnosis of Alzheimer's disease. Flortaucipir F-18, also known as 18F-T807 and 18F-AV-1451, is a small indole molecule synthesized with a radioactive fluorine isotope.

Mechanism: Alzheimer's disease is a progressive neurodegenerative disease characterized by the build-up of hyperphosphorylated tau protein aggregates. Hyperphosphorylated tau forms dimers termed paired helical filaments (PHFs), which aggregate further to form neurofibrillary tangles (NFTs) associated with neurodegeneration and severity of Alzheimer's symptoms.
Flortaucipir F-18 is a small molecule that contains radioactive 18F, which decays by positron emission to 18O with a half-life of 109.8 minutes. As a small relatively lipophilic molecule, flortaucipir F-18, following intravenous injection, quickly passes through systemic circulation, crosses the blood-brain barrier, and binds to NFTs. Once bound, the ensuing radioactive decay emits pairs of 511 keV gamma photons useful in diagnostic imaging. The pattern and intensity of emission during imaging is used in the diagnosis of Alzheimer's disease.
Curator reviewed · 5 references
Primary indication: Flortaucipir F-18 is a radioactive agent indicated for positron emission tomography (PET) imaging of aggregated tau neurofibrillary tangles (NFTs) in adult patients under evaluation for Alzheimer's disease.Curator reviewed · 1 structured indication
Formula / weight: C₁₆H₁₀FN₃ · 262.278 g/mol (avg)
First approval: United States, 2020 · European Union, 2024
Also known as: Flortaucipir (18F) · Flortaucipir F 18
Code names: 18F-AV-1451 · (F-18)T807 · LY-3191748 · T-807 F-18