(68)Ga Labeled Glu-NH-CO-NH-Lys(ahx)-hbed-CC

1011.32165

C118961

There is limited information on the LD50 value of Ga-68 PSMA-11. In the event of an overdose, it is recommended to enhance drug elimination by hydration, frequent bladder voiding, or the use of diuretics.

There is no information on plasma protein binding.

Gallium Ga-68 gozetotide, or Gallium Ga-68 PSMA-11, is a radioactive diagnostic agent indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA)-positive lesions in patients with suspected prostate cancer metastasis who are also candidates for initial surgical or radiation therapy. It is also indicated for patients with suspected prostate cancer recurrence based on elevated serum prostate-specific antigen (PSA) levels.

Ga-68 PSMA-11 works by binding to prostate-specific membrane antigen (PSMA) expressed on malignant prostate cancer cells. Gallium-68 (Ga-68) is a β+-emitting radionuclide and Ga-68 PSMA-11 can be imaged by PET to indicate the presence of PSMA-positive prostate cancer lesions in the tissues of the body. Ga-68 PMSA-11 has a high affinity to PSMA and was shown to be effective in imaging of both local prostate cancer tumours and distant metastatic lesions in clinical trials. In a clinical trial comprising patients with relapsed prostate cancer, Ga-68 PSMA-11 PET detection rate was different depending on the clinical stage of biochemical recurrence.

Compounds that are used in medicine as sources of radiation for radiotherapy and for diagnostic purposes. They have numerous uses in research and industry. (Martindale, The Extra Pharmacopoeia, 30th ed, p1161) (See all compounds classified as Radiopharmaceuticals.)

Following intravenous injection, Ga-68 PSMA-11 uptake occurs in the adrenal and prostate glands, with high uptake in PSMA-expressing tissues. Uptake of the drug is very minimal in the cerebral cortex, heart, and lungs. Mean maximum standardized uptake value (SUV_max) at later acquisition times is about 15.3.|About 14% of the total injected dose is excreted in the urine within two hours following intravenous administration.|Ga-68 PSMA-11 accumulates in the liver (15%), kidneys (7%), spleen (2%), and salivary glands (0.5%). Ga-68 PSMA-11 accumulation increases at later acquisition times.|There is limited information on the clearance rate, but Ga-68 PSMA-11 shows fast blood clearance.

Ga-68 PSMA-11 decays to stable zinc-68.

Gallium-68 (Ga-68) decays with a half-life of 68 minutes.

Prostate-specific membrane antigen (PSMA) is a type II transmembrane glycoprotein expressed throughout the body, such as in lacrimal and salivary glands, the kidneys, small intestine, liver and spleen. It is highly associated with tumour-associated angiogenesis and has been described in various tumours, such as prostate cancer, glioblastoma, thyroid cancer, gastric cancer, breast cancer, renal cancer, and colorectal cancers. The expression of PSMA has been linked to the degree of tumour differentiation, as it is overexpressed particularly in poorly differentiated and metastatic lesions. PSMA has been extensively studied as a reliable target for imaging and therapy for prostate cancer, as it is overexpressed one-hundred to one thousand-fold in over 90 % of primary prostate cancers. Positron emission tomography (PET) is a type of molecular imaging used to improve the accuracy of detecting prostate cancer at an earlier time and examine tumour characteristics. Ga-68 PSMA-11 is a PSMA-targeted imaging agent for PET that binds to PSMA via clathrin-coated pits, resulting in endosome accumulation and the internalization of the PSMA-drug complex.

(68)Ga-PSMA