Английская Википедия:Gallium (68Ga) gozetotide
Шаблон:Use dmy dates Шаблон:Infobox drug
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).[1] The PSMA targeting ligand specifically directs the radiolabeled imaging agent towards the prostate cancerous lesions in men.[2]
The most common side effects with gallium (68Ga)-radiolabelled gozetotide are tiredness, nausea (feeling sick), constipation and vomiting.[3]
Gallium (68Ga) gozetotide was approved for medical use in the United States in December 2021,[4][5] and in the European Union in December 2022.[3] It is the first drug approved by the US Food and Drug Administration (FDA) as a PET imaging agent.[2]
Structure
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.[6]
Medical uses
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][3]
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.[9]
History
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.[10]
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.[11]
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,[12] in 2019 European Pharmacopoeia mentions gallium (68Ga) DOTATOC injection for radiolabelling and PET imaging.[13]
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.[14] In December 2020, the drug was first approved by US Food and Drug Administration (FDA) for PET imaging.[2]
Mechanism of action
Gallium (68Ga) gozetotide binds with prostate-specific membrane antigen (PSMA).[9] This binds to cells that express PSMA, including malignant prostate cancer cells.[9] The radioactive isotope of gallium, 68Ga is responsible for emitting β+ radiations and X-rays.[9] This helps in recording images by positron emission tomography (PET) and CT scan.[9]
Society and culture
Legal status
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.[15] The applicant for this medicinal product is Novartis Europharm Limited.[15] Locametz was approved for medical use in the European Union in December 2022.[3][16]
Names
Gallium (68Ga) gozetotide is the international nonproprietary name (INN).[17]
References
External links
Шаблон:Radiopharmaceuticals Шаблон:Portal bar
- ↑ Шаблон:Cite web
- ↑ 2,0 2,1 2,2 Шаблон:Cite press release Шаблон:PD-notice
- ↑ 3,0 3,1 3,2 3,3 Ошибка цитирования Неверный тег
<ref>; для сносокLocametz EPARне указан текст - ↑ Шаблон:Cite web
- ↑ Шаблон:Cite web
- ↑ Шаблон:Cite journal
- ↑ Ошибка цитирования Неверный тег
<ref>; для сносокIlluccix FDA labelне указан текст - ↑ Ошибка цитирования Неверный тег
<ref>; для сносокLocametz FDA labelне указан текст - ↑ 9,0 9,1 9,2 9,3 9,4 Ошибка цитирования Неверный тег
<ref>; для сносокGallium GA-68 PSMA-11 FDA labelне указан текст - ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite book
- ↑ Шаблон:Cite book
- ↑ Шаблон:Cite journal
- ↑ 15,0 15,1 Шаблон:Cite web Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
- ↑ Шаблон:Cite web
- ↑ Шаблон:Cite journal
