Clinical data | |
---|---|
Trade names | Illuccix, Locametz |
Other names | Gallium 68 PSMA-11, Gallium Ga 68 gozetotide ( USAN US) |
AHFS/ Drugs.com | Micromedex Detailed Consumer Information |
License data |
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Pregnancy category |
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Routes of administration | Intravenous [2] |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Excretion | Urine [2] |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
Chemical and physical data | |
3D model ( JSmol) | |
| |
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Gallium (68Ga) gozetotide or Gallium (68Ga) PSMA-11 sold under the brand name Illuccix among others, is a radiopharmaceutical made of 68Ga conjugated to prostate-specific membrane antigen (PSMA) targeting ligand, Glu-Urea-Lys(Ahx)-HBED-CC, used for imaging prostate cancer by positron emission tomography (PET). [10] The PSMA targeting ligand specifically directs the radiolabeled imaging agent towards the prostate cancerous lesions in men. [11]
The most common side effects with gallium (68Ga)-radiolabelled gozetotide are tiredness, nausea (feeling sick), constipation and vomiting. [9]
Gallium (68Ga) gozetotide was approved for medical use in the United States in December 2021, [12] [13] and in the European Union in December 2022. [9] It is the first drug approved by the US Food and Drug Administration (FDA) as a PET imaging agent. [11]
Radiopharmaceuticals based on HBED are composed of three components: a chelator that has a HBED structure and two functions, a radiometal coordinated with the chelator, and a binding motif or pharmacophore that is conjugated to the chelator (such as a peptide or antibody). One of the most popular HBED chelators is HBED-CC. This chelator can create stable complexes with trivalent gallium at normal temperatures and it attaches to bioactive molecules through its propionic acid moieties. [14]
Gallium (68Ga) gozetotide is a radioactive diagnostic agent indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA)-positive lesions in men with prostate cancer. [7] [8] [9]
Ga 68 PSMA-11 injections are used for PET imaging of prostate-specific membrane antigen (PSMA) positive lesions in males with prostate cancer. It can be given for the patients with suspected metastasis, and the candidates with initial definitive therapy. [2]
In the early 2000s, researchers began exploring the use of PSMA as a target for imaging and therapy. The first PSMA-targeted radiotracer was developed using a different radioactive element, technetium-99m. This radiotracer, called 99mTc-MIP-1404, showed promise in preclinical studies but did not perform well in clinical trials. [15]
In 2011, researchers started investigating the use of gallium-68, a different radioactive element, as a more suitable alternative for PSMA-targeted radiotracers. In 2013, the first Ga-PSMA radiotracer was developed by researchers at DKFZ in Germany, and it showed promising results in early clinical studies. [16]
Since then, Ga-PSMA has been extensively studied in clinical trials, and it has been found to be a highly effective imaging agent for detecting prostate cancer lesions. It is now widely used in clinical practice, particularly for patients with recurrent prostate cancer and those with high-risk disease.
Initially gallium (68Ga) chloride solution injections used for radiolabelling, [17] in 2019 European Pharmacopoeia mentions gallium (68Ga) DOTATOC injection for radiolabelling and PET imaging. [18]
Ga 68 PSMA-11 is co-developed by University of California, Los Angeles and University of California, San Francisco, they conducted phase III clinical trial. [19] In December 2020, the drug was first approved by US Food and Drug Administration (FDA) for PET imaging. [11]
Gallium (68Ga) gozetotide binds with prostate-specific membrane antigen (PSMA). [2] This binds to cells that express PSMA, including malignant prostate cancer cells. [2] The radioactive isotope of gallium, 68Ga is responsible for emitting β+ radiations and X-rays. [2] This helps in recording images by positron emission tomography (PET) and CT scan. [2]
On 13 October 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Locametz, intended for the diagnosis of prostate cancer. [20] The applicant for this medicinal product is Novartis Europharm Limited. [20] Locametz was approved for medical use in the European Union in December 2022. [9] [21]
Gallium (68Ga) gozetotide is the international nonproprietary name (INN). [22]
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Clinical data | |
---|---|
Trade names | Illuccix, Locametz |
Other names | Gallium 68 PSMA-11, Gallium Ga 68 gozetotide ( USAN US) |
AHFS/ Drugs.com | Micromedex Detailed Consumer Information |
License data |
|
Pregnancy category |
|
Routes of administration | Intravenous [2] |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Excretion | Urine [2] |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
Chemical and physical data | |
3D model ( JSmol) | |
| |
|
Gallium (68Ga) gozetotide or Gallium (68Ga) PSMA-11 sold under the brand name Illuccix among others, is a radiopharmaceutical made of 68Ga conjugated to prostate-specific membrane antigen (PSMA) targeting ligand, Glu-Urea-Lys(Ahx)-HBED-CC, used for imaging prostate cancer by positron emission tomography (PET). [10] The PSMA targeting ligand specifically directs the radiolabeled imaging agent towards the prostate cancerous lesions in men. [11]
The most common side effects with gallium (68Ga)-radiolabelled gozetotide are tiredness, nausea (feeling sick), constipation and vomiting. [9]
Gallium (68Ga) gozetotide was approved for medical use in the United States in December 2021, [12] [13] and in the European Union in December 2022. [9] It is the first drug approved by the US Food and Drug Administration (FDA) as a PET imaging agent. [11]
Radiopharmaceuticals based on HBED are composed of three components: a chelator that has a HBED structure and two functions, a radiometal coordinated with the chelator, and a binding motif or pharmacophore that is conjugated to the chelator (such as a peptide or antibody). One of the most popular HBED chelators is HBED-CC. This chelator can create stable complexes with trivalent gallium at normal temperatures and it attaches to bioactive molecules through its propionic acid moieties. [14]
Gallium (68Ga) gozetotide is a radioactive diagnostic agent indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA)-positive lesions in men with prostate cancer. [7] [8] [9]
Ga 68 PSMA-11 injections are used for PET imaging of prostate-specific membrane antigen (PSMA) positive lesions in males with prostate cancer. It can be given for the patients with suspected metastasis, and the candidates with initial definitive therapy. [2]
In the early 2000s, researchers began exploring the use of PSMA as a target for imaging and therapy. The first PSMA-targeted radiotracer was developed using a different radioactive element, technetium-99m. This radiotracer, called 99mTc-MIP-1404, showed promise in preclinical studies but did not perform well in clinical trials. [15]
In 2011, researchers started investigating the use of gallium-68, a different radioactive element, as a more suitable alternative for PSMA-targeted radiotracers. In 2013, the first Ga-PSMA radiotracer was developed by researchers at DKFZ in Germany, and it showed promising results in early clinical studies. [16]
Since then, Ga-PSMA has been extensively studied in clinical trials, and it has been found to be a highly effective imaging agent for detecting prostate cancer lesions. It is now widely used in clinical practice, particularly for patients with recurrent prostate cancer and those with high-risk disease.
Initially gallium (68Ga) chloride solution injections used for radiolabelling, [17] in 2019 European Pharmacopoeia mentions gallium (68Ga) DOTATOC injection for radiolabelling and PET imaging. [18]
Ga 68 PSMA-11 is co-developed by University of California, Los Angeles and University of California, San Francisco, they conducted phase III clinical trial. [19] In December 2020, the drug was first approved by US Food and Drug Administration (FDA) for PET imaging. [11]
Gallium (68Ga) gozetotide binds with prostate-specific membrane antigen (PSMA). [2] This binds to cells that express PSMA, including malignant prostate cancer cells. [2] The radioactive isotope of gallium, 68Ga is responsible for emitting β+ radiations and X-rays. [2] This helps in recording images by positron emission tomography (PET) and CT scan. [2]
On 13 October 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Locametz, intended for the diagnosis of prostate cancer. [20] The applicant for this medicinal product is Novartis Europharm Limited. [20] Locametz was approved for medical use in the European Union in December 2022. [9] [21]
Gallium (68Ga) gozetotide is the international nonproprietary name (INN). [22]
{{
cite book}}
: CS1 maint: location missing publisher (
link)
{{
cite book}}
: CS1 maint: location missing publisher (
link)