Gallium (68Ga) Gozetotide

Gallium (68Ga) Gozetotide Uses, Dosage, Side Effects, Food Interaction and all others data.

Gallium (Ga) 68 prostate-specific membrane antigen (PSMA)-11, or Ga-68 gozetotide, is a radiopharmaceutical agent used to identify and assess prostate-specific membrane antigen (PSMA)-positive lesions in adult men with prostate cancer during positron emission tomography (PET). Prostate cancer is one of the most commonly diagnosed cancers among men in Western countries and many patients treated with androgen-deprivation therapy relapse with castration-resistant prostate cancer. In nearly all prostate cancers, malignant cells express a transmembrane protein called prostate-specific membrane antigen (PSMA). Ga-68 PSMA-11 is an imaging agent that binds PSMA during positron emission tomography: it emits positrons to indicate the presence of PSMA-positive prostate cancer lesions in patients with suspected prostate cancer or in patients who may have recurrent prostate cancer. On December 1, 2020, Ga-68 PSMA-11 was approved by the FDA as the first molecular-targeted drug for positron emission tomography (PET) imaging of prostate-specific membrane antigen (PSMA) positive lesions in men with prostate cancer. It is administered intravenously.

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.

Gallium (68Ga) Gozetotide
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
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Interaction With other Medicine
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Trade Name	Gallium (68Ga) Gozetotide
Generic	Gallium Ga-68 gozetotide
Gallium Ga-68 gozetotide Other Names	68Ga-Psma-11, Ga-68 PSMA-11, Ga-68-Labeled PSMA-11, Gallium (68Ga) gozetotide, Gallium Ga 68 PSMA-11, PSMA-11 Ga 68, PSMA-11 Ga-68, Ga 68 PSMA-11
Type
Formula	C₄₄H₅₉GaN₆O₁₇
Weight	Average: 1011.909 Monoisotopic: 1011.321652961
Protein binding	There is no information on plasma protein binding.
Groups	Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Ga 68 PSMA-11 is a radiopharmaceutical agent used in the diagnosis of prostate-specific membrane antigen (PSMA) positive lesions in male patients during positron emission tomography.

Gallium (68Ga) 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.

Gallium (68Ga) Gozetotide is also used to associated treatment for these conditions: Prostate-specific Membrane Antigen Positive Tumors

How Gallium (68Ga) Gozetotide works

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.

Toxicity

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.

Food Interaction

No interactions found.

Volume of Distribution

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.

Elimination Route

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.