[18F]FPIA PET

18F-labelled pivalate

[18F]Fluoro-pivalic acid ([18F]FPIA, [18F]RAD101) is based on a non-natural short-chain fatty acid (SCFA) pivalate (trimethylacetate). Pivalate cannot be oxidized to CO2 in mammalian cells, but pivalate can be activated to a coenzyme A thioester in cells, and in humans, formation and urinary excretion of pivaloylcarnitine generated from pivaloyl-CoA is the major route of pivalate elimination (Brass, 2002). Its tissue uptake is associated with carnitine transport and fatty acid oxidation (Witney et al., 2014).

[18F]FPIA production is GMP compliant (Dubash et al., 2020; Enriquez et al., 2026; Barnes et al., 2026). The tracer is safe and well tolerated, and has suitable dosimetry for studying SCFA metabolism in humans (Dubash et al., 2020).

[18F]FPIA has high tumour uptake, slow metabolism, and it does not defluorinate like [18F]fluoroacetate (Pisanechi et al., 2013; Dubash et al., 2020). Biodistribution is similar in fed and fasted subjects (Dubash et al., 2020). It could be useful in detecting, grading, and monitoring brain tumours (Witney et al., 2014; Vassileva et al., 2021; Islam et al., 2023 and 2025).


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Literature

Brass EP. Pivalate-generating prodrugs and carnitine homeostasis in man. Pharmacol Rev. 2002; 54(4): 589-598. doi: 10.1124/pr.54.4.589.

Pisaneschi F, Witney TH, Iddon L, Aboagye EO. Synthesis of [18F]fluoro-pivalic acid: An improved PET imaging probe for the fatty acid synthesis pathway in tumours. MedChemComm. 2013; 4(10): 1350-1353. doi: 10.1039/c3md00169e.

Vassileva V, Braga M, Barnes C, Przystal J, Ashek A, Allott L, Brickute D, Abrahams J, Suwan K, Carcaboso AM, Hajitou A, Aboagye EO. Effective detection and monitoring of glioma using [18F]FPIA PET imaging. Biomedicines 2021; 9(7): 811. doi: 10.3390/biomedicines9070811.



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Updated at: 2026-06-12
Created at: 2025-06-02
Written by: Vesa Oikonen