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Showing posts with the label Radiopharmaceuticals

New Drug Approvals 2013 - Pt. XVII - Flutemetamol F18 (VizamylTM)

ATC Code: V09AX04 On October 25 th , the FDA approved Flutemetamol F18 (Tradename: Vizamyl ; Research Code: [ 18 F]AH110690 ), a radioactive diagnostic agent, for intravenous (i.v.) use in Positron Emission Tomography (PET) imaging of the brain in adult patients with cognitive impairment , who are being evaluated for Alzheimer’s disease (AD) and dementia. Alzheimer's disease is a non-treatable, progressively worsening and fatal disease, characterised by a decrease in cognitive functions, such as memory, and is usually associated with an accumulation of β amyloid (Uniprot: P05067 ) plaques in several brain regions. These deposits are believed to be responsible for cellular damage and ultimately cell death. Flutemetamol F18 is the second approved diagnostic drug to estimate β-amyloid neuritic plaque density, after the approval of Florbetapir F18 in 2012. Like Florbetapir F18, Flutemetamol F18 binds to β amyloid plaques in the brain where the F-18 isotope produces...

New Drug Approvals 2013 - Pt. VII - Radium Ra 223 dichloride (Xofigo)

ATC code: Wikipedia:   Xofigo On May 15th, 2013 the FDA approved the alpha particle-emitting Radium Ra 223 dichloride (Xofigo) as a radiotherapeutic agent for the treatment of patients with castration-resistant prostate cancer, symptomatic bone metastases and no known visceral metastatic disease. The therapeutic component is the alpha particle-emiting Radium 223 isotope. It mimics calcium and binds to bone minerals is areas of rapid cell division, where it preferentially affects cancer cells. The radiation causes high levels of DNA double-strand breaks in adjacent cells, causing the killing of rapidly dividing cells, such as bone metastases. After intravenous injection, Ra 223 is rapidly cleared from the blood and distributed primarily into bone or is excreted into intestine. The levels of radioactivity detected in the blood rapidly decrease and, at 24 hours, reach less than 1% of the administered dose. The alpha particle emission range of Ra 223 is 100 micrometers ...

New Drug Approvals 2012 - Pt. XXVII - Choline C-11

On September 12, FDA approved Choline C-11, an intravenous  radioactive diagnostic agent to be used as tracer during Positron Emission Tomography ( PET ) scan to help detect sites of recurrent Prostate Cancer  (OMIM :  176807  ; MeSH :  D011471 ) . Prostate cancer is the most common cause of death from cancer in men over age 75, and is rarely found in men younger that 40. Unlike many other cancers, prostate cancer usually progresses very slowly. Sometimes the cancer cells may metastasize from the prostate to other parts of body. Overall, it is estimated to be the sixth leading cause of cancer-related death in men. Choline is a naturally occurring component of the numerous Vitamin-B complex, and is necessary for normal cell structure and signalling. Choline C-11 is a radiolabeled synthetic analog of choline that releases a positron by beta decay which can be visualised by PET. Choline is rapidly taken up by the prostate cells an...

New Drug Approvals 2011 - Pt. III Ioflupane 123I (DaTSCANTM)

ATC code : V09AB03 On January 14 th 2011, the FDA approved Ioflupane 123 I (USAN:  Ioflupane I123 USAN date: 2009 tradename: DaTSCAN , NDA 022454)) for the imaging of dopamine transporters in the brain of adult patients with potential Parkinsonian Syndromes . Ioflupane is a radiopharmaceutical agent intended for use with single photon emission computed tomography ( SPECT ) imaging, to help physicians differentiate essential tremor , from tremor due to Parkinsonian Syndromes. Ioflupane 123 I binds to, and allows imaging of, the Dopamine Transporter (DaT) (K i = 0.62 nM IC 50 = 0.71 nM). Synonym: SLC6A3 UniProt: Q01959 Pfam: PF00209 ). Variation or malfunction of the Dopamine Transporter is linked to many neurological and psychiatric disorders. The chemical structure of Ioflupane (IUPAC: methyl(1S,3S,4S,5R)-8-(3-fluoropropyl)-3-(4-iodanylphenyl)-8-azabicyclo[3.2.1]octane-4-carboxylate PubChem: CID3086674 ) is a tropane derivative; tropanes are a ...