Gallium 68 PSMA-11

Gallium 68 PSMA-11
Clinical data
Other names	GALLIUM GA-68 GOZETOTIDE; ; (68)Ga Labeled Glu-NH-CO-NH-Lys(ahx)-hbed-CC
AHFS/Drugs.com
Routes of; administration	intravenous (IV)
Pharmacokinetic data
Excretion	Urine
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	1906894-20-9;
PubChem CID	154572876;
DrugBank	DB16019;
ChemSpider	52083842 ;
UNII	ZJ0EKR6M10;
Chemical and physical data
3D model (JSmol)	Interactive image;
	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;

Short description: Drug approved by USFDA

Gallium 68 PSMA-11, or Ga 68 PSMA-11, 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).^[2] The PSMA targeting ligand specifically directs the radiolabeled imaging agent towards the prostate cancerous lesions in men. ^[3] This is the first drug approved by USFDA as a PET imaging agent.^[3]

Development

Initially Gallium (68Ga) chloride solution injections used for radiolabelling,^[4] in 2019 European Pharmacopoeia mentions Gallium (68Ga) DOTATOC injection for radiolabelling and PET imaging.^[5]

Ga 68 PSMA-11 is co-developed by University of California, Los Angeles and University of California, San Francisco, they conducted phase 3 clinical trial.^[6] On 1st December 2020, the drug was first approved by USFDA for PET imaging.^[3]

Mechanism of action

PSMA-11, Glu-Urea-Lys(Ahx)-HBED-CC of Ga 68 PSMA-11, directs and binds with prostate-specific membrane antigen (PSMA). This usually binds to cells that overexpress PSMA, such as the malignant prostate cancer cells. The radioactive Isotope of Gallium, Ga-68 is responsible for emitting β+ radiations and X-rays. This helps in recording images by positron emission tomography (PET) and CT scan.^[1]

Usage

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.^[1]

References

↑ ^1.0 ^1.1 ^1.2 ^1.3 "Highlights of Prescribing Information: Gallium Ga 68 PSMA-11 Injection, for intravenous use". FDA. https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212642s000lbl.pdf. "These highlights do not include all the information needed to use Gallium Ga 68 PSMA-11 Injection safely and effectively. See full prescribing information for Gallium Ga 68 PSMA-11 Injection."
↑ "gallium Ga 68 gozetotide" (in en). 2 February 2011. https://www.cancer.gov/publications/dictionaries/cancer-drug/def/gallium-ga-68-gozetotide?redirect=true.
↑ ^3.0 ^3.1 ^3.2 Office of the Commissioner (2 December 2020). "FDA Approves First PSMA-Targeted PET Imaging Drug for Men with Prostate Cancer" (in en). https://www.fda.gov/news-events/press-announcements/fda-approves-first-psma-targeted-pet-imaging-drug-men-prostate-cancer. This article incorporates text from this source, which is in the public domain.
↑ "Gallium (68Ga) Chloride Solution for Radiolabelling". European Pharmacopoeia (9th ed.). Stuttgart. 2018. p. 1148. ISBN 978-3-7692-6816-4.
↑ "Gallium (68Ga) DOTATOC injection". European Pharmacopoeia (10th ed.). Stuttgart. 2019. p. 1208. ISBN 978-3-7692-7453-0.
↑ "⁶⁸Ga-PSMA-11 NDA Approval: A Novel and Successful Academic Partnership". Journal of Nuclear Medicine 62 (2): 149–155. February 2021. doi:10.2967/jnumed.120.260455. PMID 33443068.

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[FDA_pdf-1] 1.0 ^1.1 ^1.2 ^1.3 "Highlights of Prescribing Information: Gallium Ga 68 PSMA-11 Injection, for intravenous use". FDA. https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/212642s000lbl.pdf. "These highlights do not include all the information needed to use Gallium Ga 68 PSMA-11 Injection safely and effectively. See full prescribing information for Gallium Ga 68 PSMA-11 Injection."

[2] "gallium Ga 68 gozetotide" (in en). 2 February 2011. https://www.cancer.gov/publications/dictionaries/cancer-drug/def/gallium-ga-68-gozetotide?redirect=true.

[fda-3] 3.0 ^3.1 ^3.2 Office of the Commissioner (2 December 2020). "FDA Approves First PSMA-Targeted PET Imaging Drug for Men with Prostate Cancer" (in en). https://www.fda.gov/news-events/press-announcements/fda-approves-first-psma-targeted-pet-imaging-drug-men-prostate-cancer. This article incorporates text from this source, which is in the public domain.

[4] "Gallium (68Ga) Chloride Solution for Radiolabelling". European Pharmacopoeia (9th ed.). Stuttgart. 2018. p. 1148. ISBN 978-3-7692-6816-4.

[5] "Gallium (68Ga) DOTATOC injection". European Pharmacopoeia (10th ed.). Stuttgart. 2019. p. 1208. ISBN 978-3-7692-7453-0.

[6] "⁶⁸Ga-PSMA-11 NDA Approval: A Novel and Successful Academic Partnership". Journal of Nuclear Medicine 62 (2): 149–155. February 2021. doi:10.2967/jnumed.120.260455. PMID 33443068.

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Gallium 68 PSMA-11

Topic: Chemistry

Contents

Development

Mechanism of action

Usage

References

Clinical data


Other names	GALLIUM GA-68 GOZETOTIDE; (68)Ga Labeled Glu-NH-CO-NH-Lys(ahx)-hbed-CC
AHFS/Drugs.com
Routes of administration	intravenous (IV)^[1]
Pharmacokinetic data
Excretion	Urine^[1]
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	1906894-20-9
PubChem CID	154572876
DrugBank	DB16019
ChemSpider	52083842^N
UNII	ZJ0EKR6M10
Chemical and physical data
3D model (JSmol)	Interactive image
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