Ga 68 PSMA-11

Identification

Summary

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.

Generic Name

Gallium Ga-68 gozetotide
Commonly known or available as Ga 68 PSMA-11

DrugBank Accession Number

DB16019

Background

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).⁷ 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.¹ In nearly all prostate cancers, malignant cells express a transmembrane protein called prostate-specific membrane antigen (PSMA).¹ 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.⁸

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.⁸ It is administered intravenously. In October 2022, the EMA's Committee for Medicinal Products for Human Use (CHMP) recommended Ga-68 gozetotide be granted marketing authorization for the diagnosis of prostate cancer.¹⁰ In December of the same year, the drug was fully authorized by the EMA.¹² In Octer 2022, Ga-68 PSMA-11 was approved by Health Canada for diagnostic use in men with prostate cancer.¹⁴

Type

Small Molecule

Groups

Approved

Structure

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MOLSDFPDBSMILESInChI

Similar Structures

Structure for Gallium Ga-68 gozetotide (DB16019)

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Weight

Average: 1011.909
Monoisotopic: 1011.321652961

Chemical Formula

C₄₄H₅₉GaN₆O₁₇

Synonyms

• (68)Ga Labeled Glu-NH-CO-NH-Lys(ahx)-hbed-CC
• (68Ga)Hbed-psma
• (68Ga)Psma-hbed-CC
• 68Ga-Psma-11
• 68Ga-Psma-hbed-CC
• DKFZ-PSMA-11 Ga-68
• Ga-68 PSMA-11
• Ga-68-Labeled PSMA-11
• Ga-Psma-hbed-CC Ga-68
• Gallium (68Ga) gozetotide
• Gallium Ga 68 PSMA-11
• Gallium Ga 68-labeled psma ligand Glu-urea-Lys(ahx)-hbed-CC
• PSMA-11 Ga 68
• PSMA-11 Ga-68
• Psma-hbed-CC Ga-68

Pharmacology

Indication

Gallium Ga-68 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 men with prostate cancer metastasis with:

• Primary staging of patients with high-risk or suspected metastatic prostate cancer prior to primary curative therapy, such as initial surgical or radiation therapy.^7,9,11
• Suspected prostate cancer recurrence based on elevated serum prostate-specific antigen (PSA) levels.^7,9,11
• Identification of patients with PSMA-positive progressive metastatic castration-resistant prostate cancer (mCRPC) for whom lutetium Lu 177 vipivotide tetraxetan PSMA-directed therapy is indicated.¹³

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Associated Conditions

• Prostate-specific Membrane Antigen Positive Tumors

Contraindications & Blackbox Warnings

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Pharmacodynamics

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.⁷ 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.^3,4 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.⁶

Mechanism of action

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.^3,5,2 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.⁶ The expression of PSMA has been linked to the degree of tumour differentiation, as it is overexpressed particularly in poorly differentiated and metastatic lesions.^1,5 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.⁶

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.⁶

Target	Actions	Organism
AProstate-specific antigen	binder	Humans

Absorption

Following intravenous injection, Ga-68 PSMA-11 uptake occurs in the adrenal and prostate glands, with high uptake in PSMA-expressing tissues.⁶ Uptake of the drug is very minimal in the cerebral cortex, heart, and lungs.⁷ Mean maximum standardized uptake value (SUV_max) at later acquisition times is about 15.3.⁴

Volume of distribution

Ga-68 PSMA-11 accumulates in the liver (15%), kidneys (7%), spleen (2%), and salivary glands (0.5%).⁷ Ga-68 PSMA-11 accumulation increases at later acquisition times.⁴

Protein binding

There is no information on plasma protein binding.

Metabolism

Ga-68 PSMA-11 decays to stable zinc-68.⁷

Route of elimination

About 14% of the total injected dose is excreted in the urine within two hours following intravenous administration.⁷

Half-life

Gallium-68 (Ga-68) decays with a half-life of 68 minutes.⁷

Clearance

There is limited information on the clearance rate, but Ga-68 PSMA-11 shows fast blood clearance.⁶

Adverse Effects

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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.⁷

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
Integrate drug-drug interactions in your software
Apalutamide	Apalutamide may increase effectiveness of Gallium Ga-68 gozetotide as a diagnostic agent.
Bicalutamide	Bicalutamide may increase effectiveness of Gallium Ga-68 gozetotide as a diagnostic agent.
Cyproterone acetate	Cyproterone acetate may increase effectiveness of Gallium Ga-68 gozetotide as a diagnostic agent.
Darolutamide	Darolutamide may increase effectiveness of Gallium Ga-68 gozetotide as a diagnostic agent.
Enzalutamide	Enzalutamide may increase effectiveness of Gallium Ga-68 gozetotide as a diagnostic agent.
Flutamide	Flutamide may increase effectiveness of Gallium Ga-68 gozetotide as a diagnostic agent.
Nilutamide	Nilutamide may increase effectiveness of Gallium Ga-68 gozetotide as a diagnostic agent.
Relugolix	Relugolix may increase effectiveness of Gallium Ga-68 gozetotide as a diagnostic agent.

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Food Interactions

No interactions found.

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International/Other Brands

Prostamedix

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Gallium Ga-68 PSMA-11	Injection, solution	5 mCi/1mL	Intravenous	Ucsf Radiopharmaceutical Facility	2020-12-14	Not applicable
Gallium Ga-68 PSMA-11	Injection, solution	5 mCi/1mL	Intravenous	UCLA Biomedical Cyclotron	2020-12-09	Not applicable

Categories

ATC Codes

V09IX14 — Gallium (68ga) gozetotide

• V09IX — Other diagnostic radiopharmaceuticals for tumour detection
• V09I — TUMOUR DETECTION
• V09 — DIAGNOSTIC RADIOPHARMACEUTICALS
• V — VARIOUS

Drug Categories

• Compounds used in a research, industrial, or household setting
• Diagnostic Radiopharmaceuticals
• Diagnostic Uses of Chemicals
• Elements
• Gallium
• Gallium Isotopes
• Gallium Radioisotopes
• Indicators and Reagents
• Isotopes
• Laboratory Chemicals
• Metals
• Metals, Heavy
• Positron Emitting Activity
• Radioactive Diagnostic Agent
• Radioisotopes
• Radiopharmaceuticals
• Tumour Detection

Classification

Not classified

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

ZJ0EKR6M10

CAS number

1906894-20-9

InChI Key

AEBYHKKMCWUMKX-LNTZDJBBSA-K

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

IUPAC Name

(68Ga)gallium(3+) 3-(3-{[(2-{[(5-{2-[(5-{[(5S)-5-carboxy-5-({[(1S)-1,3-dicarboxypropyl]carbamoyl}amino)pentyl]carbamoyl}pentyl)carbamoyl]ethyl}-2-hydroxyphenyl)methyl](carboxylatomethyl)amino}ethyl)(carboxylatomethyl)amino]methyl}-4-hydroxyphenyl)propanoate

SMILES

[68Ga+3].OC(=O)CC[C@H](NC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)CCC1=CC(CN(CCN(CC([O-])=O)CC2=C(O)C=CC(CCC([O-])=O)=C2)CC([O-])=O)=C(O)C=C1)C(O)=O)C(O)=O

References

General References

1. Hope TA, Truillet C, Ehman EC, Afshar-Oromieh A, Aggarwal R, Ryan CJ, Carroll PR, Small EJ, Evans MJ: 68Ga-PSMA-11 PET Imaging of Response to Androgen Receptor Inhibition: First Human Experience. J Nucl Med. 2017 Jan;58(1):81-84. doi: 10.2967/jnumed.116.181800. Epub 2016 Sep 22. [Article]
2. Lenzo NP, Meyrick D, Turner JH: Review of Gallium-68 PSMA PET/CT Imaging in the Management of Prostate Cancer. Diagnostics (Basel). 2018 Feb 11;8(1). pii: diagnostics8010016. doi: 10.3390/diagnostics8010016. [Article]
3. Bakht MK, Oh SW, Youn H, Cheon GJ, Kwak C, Kang KW: Influence of Androgen Deprivation Therapy on the Uptake of PSMA-Targeted Agents: Emerging Opportunities and Challenges. Nucl Med Mol Imaging. 2017 Sep;51(3):202-211. doi: 10.1007/s13139-016-0439-4. Epub 2016 Aug 6. [Article]
4. Park SY, Zacharias C, Harrison C, Fan RE, Kunder C, Hatami N, Giesel F, Ghanouni P, Daniel B, Loening AM, Sonn GA, Iagaru A: Gallium 68 PSMA-11 PET/MR Imaging in Patients with Intermediate- or High-Risk Prostate Cancer. Radiology. 2018 Aug;288(2):495-505. doi: 10.1148/radiol.2018172232. Epub 2018 May 22. [Article]
5. Silver DA, Pellicer I, Fair WR, Heston WD, Cordon-Cardo C: Prostate-specific membrane antigen expression in normal and malignant human tissues. Clin Cancer Res. 1997 Jan;3(1):81-5. [Article]
6. Ceci F, Castellucci P, Graziani T, Farolfi A, Fonti C, Lodi F, Fanti S: (68)Ga-PSMA-11 PET/CT in recurrent prostate cancer: efficacy in different clinical stages of PSA failure after radical therapy. Eur J Nucl Med Mol Imaging. 2019 Jan;46(1):31-39. doi: 10.1007/s00259-018-4189-7. Epub 2018 Oct 22. [Article]
7. FDA Approved Drug Products: Gallium Ga 68 PSMA-11 Injection, for intravenous use [Link]
8. FDA Press Announcements: FDA Approves First PSMA-Targeted PET Imaging Drug for Men with Prostate Cancer [Link]
9. FDA Approved Drug Products: Illuccix ((kit for the preparation of gallium Ga 68 gozetotide) for intravenous injection [Link]
10. EMA Summary of Opinion: Locametz (gozetotide) [Link]
11. EMA Approved Drug Products: Locametz (gozetotide) Intravenous Injection [Link]
12. EMA Medicines: Locametz [Link]
13. FDA Approved Drug Products: JILLUCCIX ® (kit for the preparation of gallium Ga 68 gozetotide injection), for intravenous use (March 2023) [Link]
14. Health Canada Approved Drug Proucts: ILLUCCIXTM Powder for Solution, 25 microgram PSMA-11 per vial Kit for the preparation of gallium (68Ga) PSMA-11 for intravenous injection [Link]

External Links

Human Metabolome Database

HMDB0304854

ChemSpider

52083842

RxNav

2586016

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
3	Active Not Recruiting	Treatment	Neoplasms of the Prostate	2
3	Completed	Diagnostic	Prostate Cancer	1
3	Enrolling by Invitation	Diagnostic	Castration-Resistant Prostate Carcinoma / Metastatic Carcinoma of the Prostate / Stage IVB Prostate Cancer AJCC v8	1
3	Recruiting	Diagnostic	BCR Prostate Carcinoma / Biochemical Recurrence of Malignant Neoplasm of Prostate / Prostate Cancer	1
3	Unknown Status	Diagnostic	Prostate Cancer	1
2	Active Not Recruiting	Diagnostic	Castration-Resistant Prostate Carcinoma / Metastatic Carcinoma of the Prostate / Stage IV Prostate Cancer AJCC v8 / Stage IVA Prostate Cancer AJCC v8 / Stage IVB Prostate Cancer AJCC v8	1
2	Completed	Diagnostic	Adenocarcinoma of Prostate / Biochemically Recurrent Prostate Carcinoma / Metastatic Carcinoma of the Prostate / Prostate Carcinoma / PSA Level Greater Than Fifty / PSA Progression / Stage IV Prostate Cancer AJCC v8 / Stage IVA Prostate Cancer AJCC v8 / Stage IVB Prostate Cancer AJCC v8	1
2	Completed	Diagnostic	Latent Cancer (Prostate)	1
2	Completed	Diagnostic	Prostate Cancer	1
2	Completed	Diagnostic	Recurrent Prostate Carcinoma	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, solution	Intravenous	5 mCi/1mL
Powder, for solution	Intravenous	25 mcg / vial

Prices

Not Available

Patents

Not Available

Properties

State

Not Available

Experimental Properties

Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.0121 mg/mL	ALOGPS
logP	1.46	ALOGPS
logP	-3.2	Chemaxon
logS	-5	ALOGPS
pKa (Strongest Acidic)	0.85	Chemaxon
pKa (Strongest Basic)	9.5	Chemaxon
Physiological Charge	-5	Chemaxon
Hydrogen Acceptor Count	19	Chemaxon
Hydrogen Donor Count	9	Chemaxon
Polar Surface Area	378.56 Å2	Chemaxon
Rotatable Bond Count	35	Chemaxon
Refractivity	268.15 m3·mol-1	Chemaxon
Polarizability	95.33 Å3	Chemaxon
Number of Rings	2	Chemaxon
Bioavailability	0	Chemaxon
Rule of Five	No	Chemaxon
Ghose Filter	No	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Not Available

Spectra

Mass Spec (NIST)

Not Available

Spectra

Not Available

Targets

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Details1. Prostate-specific antigen

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Binder

General Function

Hydrolyzes semenogelin-1 thus leading to the liquefaction of the seminal coagulum.

Specific Function

Endopeptidase activity

Gene Name

KLK3

Uniprot ID

P07288

Uniprot Name

Prostate-specific antigen

Molecular Weight

28741.1 Da

References

1. FDA Approved Drug Products: Gallium Ga 68 PSMA-11 Injection, for intravenous use [Link]

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Drug created at December 13, 2020 23:28 / Updated at April 04, 2023 03:32