FACBC

132.12 g/mol

132.056441 g/mol

38R1Q0L1ZE

C74002

V09IX12|V - Various

63.3 Ų

0.60070

0ºC

100ºC

Soluble

The hasn't been long-term carcinogenity or fertility studies in animals. Even though all reports have shown no mutagenicity, fluciclovine has the potential to be mutagenic.

Pre clinical studies showed that fluciclovine does not bind to plasma proteins.

Fluciclovine is indicated as a detection agent for positron emission tomography (PET) in men with suspected prostate cancer recurrence based on elevated blood prostate specific antigen (PSA) levels following prior treatment. The overexpression of L-type amino acid transporters such as LAT1 and LAT3 that mediate the uptake of essential amino acids has been extensively reported as a tumoral mechanism of cell growth.|FDA Label|This medicinal product is for diagnostic use only.Axumin is indicated for Positron Emission Tomography (PET) imaging to detect recurrence of prostate cancer in adult men with a suspected recurrence based on elevated blood prostate specific antigen (PSA) levels after primary curative treatment.|Diagnosis of amino acid metabolism in solid malignant tumours

Following intravenous administration, the tumor-to-normal tissue contrast is highest between 2 and 10 minutes after injection, with a 63% reduction in mean tumor uptake at 90 minutes after injection. The scanning time point should be evaluated carefully as an early scanning can present an increased blood pool and a late scanning will translate into an increased muscle uptake. These variations should always be considered in the image interpretation.

After intravenous administration of fluciclovine, the major distribution happens in liver (14%), red bone marrow (12%), lung (7%), myocardium (4%) and pancreas (3%). With increasing time, the dose gets distributed into skeletal muscle.|In the first four hours post-injection, 3% of administered dose is excreted in the urine which increases to 5% after 24 hours post-injection.|The compartmental volume of distribution of fluciclovine is in prostate 0.97 L, vesicle 0.79 L, red bone marrow 0.98 L, gluteus muscle 2.13 L and obturator muscle 2.23 L.|Fluciclovine renal clearance and excretion is minimal.

Fluciclovine is not metabolized and it is not incorporated into newly synthesized proteins.

Fluciclovine is a cyclotron produced radionuclide that decays by positron emission (ß+ decay, 96.7%) and orbital electron capture (3.3%) to stable oxygen 18 with a physical half-life of 109.7 minutes.

Fluciclovine is transported into the prostate cancer cells via ASCT2 and LAT1 transporters. The activity of LAT1 gets increased in acidic pH, condition that is developed intra-tumorally at certain size. The uptake of fluciclovine presents an androgen-dependent dynamic in hormone sensitive cells.

(18F)GE-148

Human drugs -> Axumin -> EMA Drug Category|Diagnostic radiopharmaceuticals -> Human pharmacotherapeutic group|Human drugs -> Rare disease (orphan)|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients