Flurpiridaz F-18
The newest heart PET tracer, approved in the US in September 2024. It sticks tightly to a protein inside heart-muscle mitochondria in proportion to blood flow, lasts long enough to be made off site and shipped like a hospital's regular PET drug, and is the first cardiac PET tracer practical to pair with a treadmill exercise test.
Overview
Flyrcado (flurpiridaz F-18) is a fluorine-18 mitochondrial complex I-binding PET myocardial perfusion agent approved by the FDA on 27 September 2024 (NDA 215168, GE HealthCare), the first new PET MPI agent approved in the US in over a decade and the first cardiac PET tracer with a half-life practical for exercise stress protocols. Its mechanism, high-affinity binding to complex I rather than ion-pump uptake, gives a first-pass extraction fraction of about 94%, markedly higher and flatter across flow rates than sestamibi (55-68%), tetrofosmin (54%) or Rb-82 (roughly 40-70%), which its sponsor and independent reviews report translates into sharper contrast for smaller or milder perfusion defects.
The approved indication is PET myocardial perfusion imaging under rest or stress (pharmacologic or exercise) in adult patients with known or suspected coronary artery disease, to evaluate for myocardial ischaemia and infarction. Because F-18's 110-minute half-life is roughly ten times that of Rb-82 and eleven times N-13 ammonia's, Flyrcado can be manufactured off site and delivered as a ready-to-use unit dose like FDG, potentially widening PET MPI access beyond centres with an on-site generator or cyclotron, including for patients who are difficult to image by SPECT (high body-mass index, women with breast attenuation artefact).
Most common adverse reactions in the pivotal programme (occurring in at least 2% of subjects across rest and stress imaging) were dyspnoea, headache, angina pectoris, chest pain, fatigue, ST-segment changes, flushing, nausea, abdominal pain, dizziness and arrhythmia. As a newly approved agent, real-world comparative outcome and cost-effectiveness data against SPECT and existing PET tracers are still accumulating.
Flurpiridaz F-18 is a fluorinated structural analogue of pyridaben, an insecticidal inhibitor of mitochondrial complex I (NADH:ubiquinone oxidoreductase). It binds with high affinity to complex I in cardiomyocyte mitochondria without impairing viability, giving a very high and largely flow-independent first-pass myocardial extraction fraction (reported at approximately 94% in preclinical and kinetic modelling studies) and slow washout, so uptake tracks blood flow more linearly across a wider flow range than the older SPECT or Rb-82 agents, with less roll-off at high flow. Its 110-minute F-18 half-life, more than ten times longer than Rb-82 or N-13 ammonia, allows off-site cyclotron production and unit-dose distribution like FDG, and is long enough to support exercise stress imaging, which is impractical with the shorter-lived PET perfusion tracers.
1.Flurpiridaz F-18 slips into a pocket on its target.
- Route
- Intravenous injection
- Schedule
- Per FDA label dosing tables for rest and stress imaging (pharmacologic or exercise stress); supplied at 190-2,050 MBq/mL (5-55 mCi/mL) at end of synthesis
Source: www.accessdata.fda.gov/drugsatfda_docs/label/2024/215168s000lbl.pdf. Doses are for orientation; the current label governs.
- 27 Sept 2024ApprovalUS
FDA approved Flyrcado (flurpiridaz F 18) injection, NDA 215168, for PET myocardial perfusion imaging under rest or stress (pharmacologic or exercise) in adults with known or suspected CAD. source
Approvals
| Region | Year | Indication |
|---|---|---|
| US | 2024 | PET myocardial perfusion imaging (MPI) under rest or stress (pharmacologic or exercise) in adult patients with known or suspected coronary artery disease, to evaluate for myocardial ischaemia and infarction |
| Adverse event |
|---|
| Dyspnoea, headache, angina pectoris, chest pain, fatigue, ST-segment changes, flushing, nausea, abdominal pain, dizziness, arrhythmia (most common, combined rest and stress imaging) |
Rates read from the source. Blank cells mean the figure was not sourced, not that it is zero.
Trials
topTrials recruiting now
Country and place are remembered in this browser only. A postcode is sent to OpenStreetMap's Nominatim service to find coordinates when you press the button; nothing else leaves your device.
Latest papers
topQuery for this drug: (TITLE:"Flurpiridaz F-18" OR ABSTRACT:"Flurpiridaz F-18" OR TITLE:"Flyrcado" OR ABSTRACT:"Flyrcado" OR TITLE:"18F-flurpiridaz" OR ABSTRACT:"18F-flurpiridaz" OR TITLE:"BMS-747158-02" OR ABSTRACT:"BMS-747158-02") AND (radiopharmaceutical OR radioligand OR radionuclide OR theranostic OR "nuclear medicine" OR "molecular imaging" OR radiotracer OR scintigraphy OR cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Flurpiridaz F-18, not a curated reading list.
Similar pages
not linked directly; found by shared links- IndicationCardiac sarcoidosis
Shares Ammonia N-13, Rubidium Rb-82 chloride, Technetium Tc-99m sestamibi, Nitrogen-13.
- AgentTechnetium Tc-99m tetrofosmin
Shares Technetium Tc-99m sestamibi, Coronary artery disease and the tag myocardial perfusion.
- AgentThallous chloride Tl-201
Shares Technetium Tc-99m sestamibi, Coronary artery disease and the tag myocardial perfusion.
- InstitutionAmerican Society of Nuclear Cardiology
Shares Nitrogen-13, Rubidium-82, Coronary artery disease, Fluorine-18.
- TrialAURORA
Shares Rubidium-82, Fluorine-18 and the tag myocardial perfusion.
- AgentSodium fluoride F-18
Shares GE HealthCare, Fluorine-18 and the tag PET.
- IsotopeThallium-201
Shares Technetium Tc-99m sestamibi, Coronary artery disease.
- TechnologyRadiohybrid (rh) chemistry
Shares Fluorine-18 and the tag PET.