Flurpiridaz (18F)

Last updated

Flurpiridaz (18F)
Flurpiridaz F18.svg
Clinical data
Trade names Flyrcado
Other namesNMB58, BMS-747158-02, flurpiridaz F-18, flurpiridaz F 18 [1] (USAN US)
License data
Routes of
administration
Intravenous
ATC code
  • None
Legal status
Legal status
Identifiers
  • 2-tert-butyl-4-chloro-5-({4-[(2- [18F]fluoroethoxy)methyl]phenyl}methoxy)pyridazin-3(2H)-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
Chemical and physical data
Formula C18H22Cl[18F]N2O3 [2]
Molar mass 367.8 [2]
3D model (JSmol)
  • CC(C)(C)N1N=CC(OCC2=CC=C(COCC[18F])C=C2)=C(Cl)C1=O
  • InChI=1S/C18H22ClFN2O3/c1-18(2,3)22-17(23)16(19)15(10-21-22)25-12-14-6-4-13(5-7-14)11-24-9-8-20/h4-7,10H,8-9,11-12H2,1-3H3/i20-1
  • Key:RMXZKEPDYBTFOS-LRFGSCOBSA-N

Flurpiridaz (18F), sold under the brand name Flyrcado, is a cyclotron-produced radioactive diagnostic agent for use with positron emission tomography (PET) myocardial perfusion imaging under rest or stress (pharmacologic or exercise). [3] Flurpiridaz (18F) It is given by intravenous injection. [3]

Contents

The most common adverse reactions include dyspnea (shortness of breath), headache, angina pectoris (severe pain in the chest), chest pain, fatigue, ST segment changes, flushing, nausea, abdominal pain, dizziness, and arrhythmia (irregular heartbeat). [3]

Flurpiridaz (18F) was approved for medical use in the United States in September 2024. [3] [4]

Medical uses

Flurpiridaz (18F) is indicated for positron emission tomography myocardial perfusion imaging under rest or stress (pharmacologic or exercise) in adults with known or suspected coronary artery disease to evaluate for myocardial ischemia and infarction. [2] [3]

History

Flurpiridaz F-18 is a fluorine 18-labeled agent developed by Lantheus Medical Imaging for the diagnosis of coronary artery disease. [5]

The efficacy and safety of flurpiridaz (18F) were evaluated in two prospective, multicenter, open-label clinical studies in adults with either suspected CAD (Study 1: NCT03354273) or known or suspected CAD (Study 2: NCT01347710). [3] Study 1 evaluated the sensitivity (ability to designate an imaged patient with disease as positive) and specificity (ability to designate an imaged patient without disease as negative) of flurpiridaz (18F) for the detection of significant CAD in subjects with suspected CAD who were scheduled for invasive coronary angiography (ICA). [3] Across three flurpiridaz (18F) imaging readers, estimates of sensitivity ranged from 74% to 89% and estimates of specificity ranged from 53% to 70% for CAD defined as at least 50% narrowing of an artery. [3]

Study 2 evaluated the sensitivity and specificity of flurpiridaz (18F) for the detection of significant CAD in subjects with known or suspected CAD who had ICA without intervention within 60 days prior to imaging or were scheduled for ICA. [3] Across three flurpiridaz (18F) imaging readers, estimates of sensitivity ranged from 63% to 77% and estimates of specificity ranged from 66% to 86% for CAD defined as at least 50% narrowing of an artery. [3]

Society and culture

Flurpiridaz (18F) was approved for medical use in the United States in September 2024. [2] [3] [4]

Names

Flurpiridaz (18F) is the international nonproprietary name. [6]

Related Research Articles

<span class="mw-page-title-main">Coronary artery disease</span> Reduction of blood flow to the heart

Coronary artery disease (CAD), also called coronary heart disease (CHD), ischemic heart disease (IHD), myocardial ischemia, or simply heart disease, involves the reduction of blood flow to the cardiac muscle due to build-up of atherosclerotic plaque in the arteries of the heart. It is the most common of the cardiovascular diseases. Types include stable angina, unstable angina, and myocardial infarction.

<span class="mw-page-title-main">Angina</span> Chest discomfort due to disorder of the heart muscles

Angina, also known as angina pectoris, is chest pain or pressure, usually caused by insufficient blood flow to the heart muscle (myocardium). It is most commonly a symptom of coronary artery disease.

<span class="mw-page-title-main">Nuclear medicine</span> Medical specialty

Nuclear medicine, or nucleology, is a medical specialty involving the application of radioactive substances in the diagnosis and treatment of disease. Nuclear imaging is, in a sense, radiology done inside out, because it records radiation emitted from within the body rather than radiation that is transmitted through the body from external sources like X-ray generators. In addition, nuclear medicine scans differ from radiology, as the emphasis is not on imaging anatomy, but on the function. For such reason, it is called a physiological imaging modality. Single photon emission computed tomography (SPECT) and positron emission tomography (PET) scans are the two most common imaging modalities in nuclear medicine.

<span class="mw-page-title-main">Cardiac stress test</span> Measures the hearts ability to respond to external stress in a controlled clinical environment

A cardiac stress test is a cardiological examination that evaluates the cardiovascular system's response to external stress within a controlled clinical setting. This stress response can be induced through physical exercise or intravenous pharmacological stimulation of heart rate.

<span class="mw-page-title-main">Scintigraphy</span> Diagnostic imaging test in nuclear medicine

Scintigraphy, also known as a gamma scan, is a diagnostic test in nuclear medicine, where radioisotopes attached to drugs that travel to a specific organ or tissue (radiopharmaceuticals) are taken internally and the emitted gamma radiation is captured by gamma cameras, which are external detectors that form two-dimensional images in a process similar to the capture of x-ray images. In contrast, SPECT and positron emission tomography (PET) form 3-dimensional images and are therefore classified as separate techniques from scintigraphy, although they also use gamma cameras to detect internal radiation. Scintigraphy is unlike a diagnostic X-ray where external radiation is passed through the body to form an image.

<span class="mw-page-title-main">Drug-eluting stent</span> Medical implant

A drug-eluting stent (DES) is a tube made of a mesh-like material used to treat narrowed arteries in medical procedures both mechanically and pharmacologically. A DES is inserted into a narrowed artery using a delivery catheter usually inserted through a larger artery in the groin or wrist. The stent assembly has the DES mechanism attached towards the front of the stent, and usually is composed of the collapsed stent over a collapsed polymeric balloon mechanism, the balloon mechanism is inflated and used to expand the meshed stent once in position. The stent expands, embedding into the occluded artery wall, keeping the artery open, thereby improving blood flow. The mesh design allows for stent expansion and also for new healthy vessel endothelial cells to grow through and around it, securing it in place.

<span class="mw-page-title-main">Myocardial perfusion imaging</span> Nuclear medicine imaging method

Myocardial perfusion imaging or scanning is a nuclear medicine procedure that illustrates the function of the heart muscle (myocardium).

Avijit Lahiri is a researcher in cardiology in the UK.

Technetium (<sup>99m</sup>Tc) tetrofosmin Chemical compound

Technetium (99mTc) tetrofosmin is a drug used in nuclear medicine cardiac imaging. It is sold under the brand name Myoview. The radioisotope, technetium-99m, is chelated by two 1,2-bis[di-(2-ethoxyethyl)phosphino]ethane ligands which belong to the group of diphosphines and which are referred to as tetrofosmin.

Rubidium-82 (82Rb) is a radioactive isotope of rubidium. 82Rb is widely used in myocardial perfusion imaging. This isotope undergoes rapid uptake by myocardiocytes, which makes it a valuable tool for identifying myocardial ischemia in Positron Emission Tomography (PET) imaging. 82Rb is used in the pharmaceutical industry and is marketed as Rubidium-82 chloride under the trade names RUBY-FILL and CardioGen-82.

Cardiac PET is a form of diagnostic imaging in which the presence of heart disease is evaluated using a PET scanner. Intravenous injection of a radiotracer is performed as part of the scan. Commonly used radiotracers are Rubidium-82, Nitrogen-13 ammonia and Oxygen-15 water.

<span class="mw-page-title-main">Cardiac magnetic resonance imaging perfusion</span>

Cardiac magnetic resonance imaging perfusion, also known as stress CMR perfusion, is a clinical magnetic resonance imaging test performed on patients with known or suspected coronary artery disease to determine if there are perfusion defects in the myocardium of the left ventricle that are caused by narrowing of one or more of the coronary arteries.

Cardiac imaging refers to minimally invasive imaging of the heart using ultrasound, magnetic resonance imaging (MRI), computed tomography (CT), or nuclear medicine (NM) imaging with PET or SPECT. These cardiac techniques are otherwise referred to as echocardiography, Cardiac MRI, Cardiac CT, Cardiac PET and Cardiac SPECT including myocardial perfusion imaging.

Florbetapir (18F), sold under the brand name Amyvid, is a PET scanning radiopharmaceutical compound containing the radionuclide fluorine-18 that was approved for use in the United States in 2012, as a diagnostic tool for Alzheimer's disease. Florbetapir, like Pittsburgh compound B (PiB), binds to beta-amyloid, however fluorine-18 has a half-life of 109.75 minutes, in contrast to PiB's radioactive half life of 20 minutes. The longer life allows the tracer to accumulate significantly more in the brains of people with AD, particularly in the regions known to be associated with beta-amyloid deposits.

Flutemetamol (<sup>18</sup>F) Chemical compound

Flutemetamol (18F) is a PET scanning radiopharmaceutical containing the radionuclide fluorine-18, used as a diagnostic tool for Alzheimer's disease.

Fluciclovine (<sup>18</sup>F) Chemical compound

Fluciclovine (18F), also known as anti-1-amino-3-18F-fluorocyclobutane-1-carboxylic acid, and sold under the brand name Axumin, is a diagnostic agent used for positron emission tomography (PET) imaging in men with suspected prostate cancer recurrence based on elevated prostate specific antigen (PSA) levels.

<span class="mw-page-title-main">Oxygen-15 labelled water</span> Chemical compound

Oxygen-15 labelled water (also known as 15O-water, [O-15]-H2O, or H215O) is a radioactive variation of regular water, in which the oxygen atom has been replaced by oxygen-15 (15O), a positron-emitting isotope. 15O-water is used as a radioactive tracer for measuring and quantifying blood flow using positron emission tomography (PET) in the heart, brain and tumors.

Flortaucipir (<sup>18</sup>F) Chemical compound

Flortaucipir (18F), sold under the brand name Tauvid, is a radioactive diagnostic agent indicated for use with positron emission tomography (PET) imaging to image the brain.

<span class="mw-page-title-main">Piflufolastat F-18</span> Chemical compound

Piflufolastat F-18, sold under the brand name Pylarify among others, is a radioactive diagnostic agent used for positron emission tomography (PET) imaging. It is given by intravenous injection.

Gallium (<sup>68</sup>Ga) gozetotide Radiopharmaceutical medication

Gallium (68Ga) gozetotide or Gallium (68Ga) PSMA-11 sold under the brand name Illuccix among others, is a radiopharmaceutical made of 68Ga conjugated to prostate-specific membrane antigen (PSMA) targeting ligand, Glu-Urea-Lys(Ahx)-HBED-CC, used for imaging prostate cancer by positron emission tomography (PET). The PSMA targeting ligand specifically directs the radiolabeled imaging agent towards the prostate cancerous lesions in men.

References

  1. "Flurpiridaz F 18". AMA Finder. Retrieved 27 September 2024.
  2. 1 2 3 4 5 "Flyrcado (flurpiridaz F 18) injection, for intravenous use" (PDF). U.S. Food and Drug Administration (FDA). Retrieved 27 September 2024.
  3. 1 2 3 4 5 6 7 8 9 10 11 "FDA approves imaging drug for evaluation of myocardial ischemia". U.S. Food and Drug Administration. 27 September 2024. Retrieved 27 September 2024.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  4. 1 2 "Flyrcado: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 27 September 2024.
  5. "Flurpiridaz F-18". Inxight Drugs. Retrieved 27 September 2024.
  6. World Health Organization (2011). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 65". WHO Drug Information. 25 (1). hdl: 10665/74623 .

Further reading