Tracers / [11C]ibrutinib

[11C]ibrutinib

Also written as [11C]Ibrutinib; [C-11]Ibrutinib
Radionuclide
C-11 t½ 20.36 min
Modality
PET
Production route
Stage
Syntheses indexed
4

What it is

Compound class
Bruton's tyrosine kinase (BTK) inhibitor (small molecule, ibrutinib analog)
Target / mechanism
Bruton's tyrosine kinase (BTK) PMID 27043721
Clinical application
Theranostic pair

Regulatory status

FDA
EMA (centralised)
Other approvals
Brand names

Clinical use

Typical injected activity
Uptake time

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
TRACERlab FX (model not stated)
GE HealthCare
HPLC37513867
2023 Pharmaceuticals (Basel)
Recently, Scott, Shao, and co-workers developed an automated and good manufacturing practice (GMP)-compliant "in-loop" 11C-carbonylation procedure using a modified GE TracerLabTM synthesis platform — three clinically relevant BTK inhibitors, [11C]ibrutinib, [11C]tolebrutinib, and [11C]evobrutinib, were synthesized at good RCYs
TRACERlab FX C Pro
GE HealthCare
custom manifoldHPLC+SPE5%
no
>99%precursor 11
Bristol-Myers Squibb
27043721
2016 Bioconjug Chem
the procedure was fully automated on a GE TRACERLab FXC-Pro synthesis module — gave 150 mCi of isolated and formulated product (5% non-decay corrected RCY based upon [11C]CO2; RCP >99%; specific activity = 55 mCi/μmol; pH = 6.0)
TracerMaker
Scansys Laboratorieteknik
HPLC+SPE5.4 ± 2.5%
no
>99%3-(4-phenoxyphenyl)-1-(piperidin-3-yl)-2,3-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Bristol Myer-Squibb Pharmaceuticals, Princeton, NJ, USA
39355638
2021 Front Nucl Med
The radiosynthesis of [11C]ibrutinib was fully automated using a commercial TracerMaker™ 11C synthesis platform. — [11C]Ibrutinib was synthesized in 5.4 ± 2.5% (n = 9) RCY (non-decay corrected) relative to [11C]CO2
TracerMaker
Scansys Laboratorieteknik
HPLC5
no
39831838
2025 ChemistryOpen
was delivered to a TracerMaker synthesis platform (Scansys Laboratorieteknik, Denmark) — The fully automated syntheses yielded [11C]Ibrutinib in RCY of 5 %

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Quality control Preliminary — inferred from compound class

Ph. Eur. monograph
USP monograph
AppearancepHRCP HPLCRCP TLCHPLC UVRadionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrity
How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); organic-phase radiosynthesis assumed from isotope/compound class, no synthesis data confirming it -> GC residual solvents (preliminary)

Tests listed by reference only. Monograph texts are copyrighted and are not reproduced here. How these are derived

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Notes

Added from reverse module search (stage 6); 2 article(s) with C-11.