Radiopharmaceuticals

Glicocer (Fludesoxiglicose 18 F)
PSMA-1007 (18 F)
18F-Florbetabeno

  • GLICOCER (FLUDESOXYCLICOSE (18 F)

    The radiopharmaceutical fludesoxyglucose (18 F), registered at ANVISA by InsCer in October 2017 under the trade name GLICOCER (MS No. 9961.0001), is produced at the Institute on a regular basis, being the most used PET-CT marker in Brazil and in the world. The available presentations are:

    • Glycocer: 370 MBq (10 mCi) of fludesoxyglucose (18 F)
    • Glycocer: 740 MBq (20 mCi) of fludesoxyglucose (18 F)
    • Glycocer: 1,110 MBq (30 mCi) of fludesoxyglucose (18 F)
    • Glycocer: 1,480 MBq (40 mCi) of fludesoxyglucose (18 F)
    • Glycocer: 1,850 MBq (50 mCi) of fludesoxyglucose (18 F)
    • Glycocer: 2,220 MBq (60 mCi) of fludesoxyglucose (18 F)
    • Glycocer: 2,590 MBq (70 mCi) of fludesoxyglucose (18 F)
    • Glycocer: 2,960 MBq (80 mCi) of fludesoxyglucose (18 F)
    • Glycocer: 3,330 MBq (90 mCi) of fludesoxyglucose (18 F)
    • Glycocer: 3,700 MBq (100 mCi) of fludesoxyglucose (18 F)
    • Glycocer: 4,070 MBq (110 mCi) of fludesoxyglucose (18 F)

    This radiopharmaceutical is a glucose analog where the hydroxyl group of carbon 2 is replaced by the radioactive isotope of fluorine, 18 F. The molecule crosses the cell membrane using the glucose transporters GLUT, subtype GLUT-1, which are the same ones used by the non-radioactive glucose molecule. Despite helping to visualize the most important transporter (GLUT-1), fludesoxyglucose (18 F) is not so selective as to differentiate cells where GLUT-3 or GLUT-4 transporters may be involved. Once inside the cell, the molecule is phosphorylated by the enzyme hexokinase, being converted to [18F] FDG-6-phosphate. However, this metabolite is not recognized as a substrate for the next enzyme in the chain, and cannot follow the glycolytic pathway, accumulating inside the cell and remaining trapped in it. In this way, it is possible to acquire a functional image, showing the distribution of glucose in the body.

    This radiopharmaceutical has great clinical utility, mainly in oncology due to the biological characteristics of tumors. It has long been known that cancer cells have an increase in glycolysis in relation to oxidative metabolism (up to 30 times greater than healthy cells). When compared to normal cells, the high uptake of radiopharmaceutical by cancer cells provides important evidence of the degree of malignancy and biological aggressiveness of the tumor. The smallest tumors that this marker is able to detect are around 2-6 mm, depending on the sensitivity of the PET-CT machine used. Thus, in some cases it is possible to locate the tumor tissue even before it can be seen in other imaging techniques, such as computed tomography. However, not all tumors have an abnormal glucose consumption rate, and there are tissues, such as the brain, that consume a lot of glucose naturally, limiting the use of fludesoxyglucose (18 F) to differentiate normal tissue from cancer.

    For these reasons, we work at InsCer to meet the eminent need to develop more specific radiopharmaceuticals for each target, making each product completely different from the other, seeking to meet the demands of society.

    For more information on products under development and used in research, visit XXXXXXXX.

  • PSMA-1007 (18 F)

    It is already a consensus among the medical profession that PET-CT with PSMA is essential to define the approach to be used in patients with prostate cancer, providing a more complete and effective investigation of the tumor. Especially in cases of biochemical recurrence, which is when the patient has been previously treated, but returns to increased PSA (prostate specific antigen), this diagnostic technique is able to locate the foci of metastasis, assisting the physician in deciding the most appropriate treatment proper. Often patients have increased PSA, however, no lesions can be identified using imaging techniques such as MRI. In these cases, PET-CT with PSMA is essential.

    Prostate-specific membrane antigen (PSMA), when labeled with the 18 F radioisotope, can be used for the diagnosis of primary and metastatic prostate cancer with high specificity. When compared to other radiopharmaceuticals used for a longer time for this purpose, PSMA was more sensitive and specific, even when the individual had PSA levels below 0.5 ng / mL.

    This antigen is expressed in the vast majority of prostate AC tissue samples and its degree of expression correlates with a number of important parameters of the aggressiveness of the prostate AC tumor, including Gleason score, propensity to metastasis and the development of resistance to castration. As a result, PSMA becomes one of the best targets for PET / CT scans, with the development of different binding molecules.

  • 18F-Florbetabeno

    After the synthesis of the Pittsburg compound B (PiB), researchers from different parts of the world saw the need to develop a marker using the 18F radiosiotope, which has a physical half-life much higher than carbon-11 and, therefore, allows the large-scale production and distribution. One of the developed molecules was 18F-Florbetabeno, which, like 11C-PiB, has a high affinity and specificity with beta-amyloid plaques present in Alzheimer's patients, enabling their early detection and differentiation of Alzheimer's disease with others types of dementia. The deposition of the beta-amyloid peptide is considered to be one of the initial events in Alzheimer's disease. The formation of these plaques happens long before the onset of cognitive symptoms and leads to the gradual progression of the disease. Early detection represents a major step forward in understanding and treating this disease.