Gallium (68Ga) gozetotide

Gallium (68Ga) gozetotide, 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).[6] The PSMA targeting ligand specifically directs the radiolabeled imaging agent towards the prostate cancerous lesions in men. [7] This is the first drug approved by the US Food and Drug Administration (FDA) as a PET imaging agent.[7]

Gallium (68Ga) gozetotide
Clinical data
Trade namesIlluccix, Locametz
Other namesGallium 68 PSMA-11, Gallium Ga 68 gozetotide (USAN US)
AHFS/Drugs.comMicromedex Detailed Consumer Information
License data
Pregnancy
category
Routes of
administration		Intravenous[2]
ATC code
Legal status
Legal status
Pharmacokinetic data
ExcretionUrine[2]
Identifiers
IUPAC name
  • 2-[[5-[3-[[6-[[(5S)-5-carboxy-5-[[(1S)-1,3-dicarboxypropyl]carbamoylamino]pentyl]amino]-6-oxohexyl]amino]-3-oxopropyl]-2-oxidophenyl]methyl-[2-[[5-(2-carboxyethyl)-2-oxidophenyl]methyl-(carboxylatomethyl)amino]ethyl]amino]acetate;gallium-68(3+);hydron
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
Chemical and physical data
3D model (JSmol)
SMILES
  • [H+].C1=CC(=C(C=C1CCC(=O)NCCCCCC(=O)NCCCC[C@@H](C(=O)O)NC(=O)N[C@@H](CCC(=O)O)C(=O)O)CN(CCN(CC2=C(C=CC(=C2)CCC(=O)O)[O-])CC(=O)[O-])CC(=O)[O-])[O-].[68Ga+3]
InChI
  • InChI=1S/C44H62N6O17.Ga/c51-34-13-8-28(22-30(34)24-49(26-40(59)60)20-21-50(27-41(61)62)25-31-23-29(9-14-35(31)52)11-16-38(55)56)10-15-37(54)46-18-4-1-2-7-36(53)45-19-5-3-6-32(42(63)64)47-44(67)48-33(43(65)66)12-17-39(57)58;/h8-9,13-14,22-23,32-33,51-52H,1-7,10-12,15-21,24-27H2,(H,45,53)(H,46,54)(H,55,56)(H,57,58)(H,59,60)(H,61,62)(H,63,64)(H,65,66)(H2,47,48,67);/q;+3/p-3/t32-,33-;/m0./s1/i;1-2
  • Key:AEBYHKKMCWUMKX-LNTZDJBBSA-K

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.[4][5]

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]

Development

Initially gallium (68Ga) chloride solution injections used for radiolabelling,[8] in 2019 European Pharmacopoeia mentions gallium (68Ga) DOTATOC injection for radiolabelling and PET imaging.[9]

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.[10] In December 2020, the drug was first approved by US Food and Drug Administration (FDA) for PET imaging.[7]

Mechanism of action

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]

Society and culture

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.[11] The applicant for this medicinal product is Novartis Europharm Limited.[11]

Names

Gallium (68Ga) gozetotide is the international nonproprietary name (INN).[12]

References
  1. "AusPAR: Glu-urea-Lys(ahx)-hbed-CC". Therapeutic Goods Administration (TGA). 27 June 2022. Retrieved 17 July 2022.
  2. "Gallium GA-68 PSMA-11- gallium ga-68 gozetotide injection, solution". DailyMed. 21 November 2021. Archived from the original on 3 July 2022. Retrieved 27 May 2022.
  3. "Gallium GA-68 PSMA-11- gallium ga-68 gozetotide injection, solution". DailyMed. 30 November 2021. Archived from the original on 3 July 2022. Retrieved 27 May 2022.
  4. "Illuccix- kit for the preparation of gallium ga 68 gozetotide injection kit". DailyMed. 12 May 2022. Archived from the original on 3 July 2022. Retrieved 27 May 2022.
  5. "Locametz- kit for the preparation of gallium ga 68 gozetotide injection, powder, lyophilized, for solution". DailyMed. 23 March 2022. Archived from the original on 3 July 2022. Retrieved 27 May 2022.
  6. "gallium Ga 68 gozetotide". National Cancer Institute. 2 February 2011. Archived from the original on 18 November 2021. Retrieved 18 November 2021.
  7. "FDA Approves First PSMA-Targeted PET Imaging Drug for Men with Prostate Cancer". U.S. Food and Drug Administration (FDA) (Press release). 2 December 2020. Archived from the original on 4 November 2021. Retrieved 9 November 2021. This article incorporates text from this source, which is in the public domain.
  8. "Gallium (68Ga) Chloride Solution for Radiolabelling". European Pharmacopoeia (9th ed.). Stuttgart. 2018. p. 1148. ISBN 978-3-7692-6816-4.
  9. "Gallium (68Ga) DOTATOC injection". European Pharmacopoeia (10th ed.). Stuttgart. 2019. p. 1208. ISBN 978-3-7692-7453-0.
  10. Carlucci G, Ippisch R, Slavik R, Mishoe A, Blecha J, Zhu S (February 2021). "68Ga-PSMA-11 NDA Approval: A Novel and Successful Academic Partnership". Journal of Nuclear Medicine. 62 (2): 149–155. doi:10.2967/jnumed.120.260455. PMC 8679592. PMID 33443068.
  11. "Locametz: Pending EC decision". European Medicines Agency. 13 October 2022. Retrieved 14 October 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  12. World Health Organization (2021). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 85" (PDF). WHO Drug Information. 35 (1). Archived (PDF) from the original on 19 April 2021. Retrieved 28 May 2022.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.