PSMA-11 - Radioligand

PSMA-11 (INN: Gozetotide) is a small-molecule ligand with high affinity for the prostate-specific membrane antigen (PSMA), which is a transmembrane glycoprotein strongly overexpressed on prostate cancer cells. It contains a HBED-CC chelator that enables stable radiolabeling and a PSMA-inhibiting Glu-urea-Lys pharmacophore. When labeled with radionuclides such as Gallium-68, PSMA 11 forms a radioligand widely used in PET/CT scans to visualize and localize PSMA-expressing tumor cells. This application has established PSMA-11 as the gold standard for prostate cancer diagnosis, staging, and recurrence detection.

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PSMA-11 - Radioligand, precursor for radiolabeled PSMA-11 and with high affinity for the prostate-specific membrane antigen (PSMA). Can be bound to radionuclides for development of cancer treatment and diagnosis. For research use only!

PSMA-11 - Radioligand - Specifications

• Peptide sequence: Glu-urea-Lys(HBED-CC-Ahx)-OH
• Amount: 5 mg (50 x100µg)
• Purity: >95% (HPLC-MS)
• Delivery Format: Freeze-dried in glass vial
• CAS: 1366302-52-4
• Application(s): Nuclear medicine
• Condition(s)/Topic(s): Cancer
• Standard Delivery Time: approx. 3 weeks

Radiolabeled PSMA-11 (PSMA-HBED-CC) variants:

PSMA 11 is itself a non-radioactive precursor that can be labeled with radionuclides through its HBED-CC chelator and form various radioligands.

• The most widely used and clinically important variant is [^68Ga]Ga-PSMA-11 (Gallium-68 PSMA 11, INN: Gozetotide), which is established as the standard PET tracer for diagnosing and staging prostate cancer. In this compound, the PSMA-targeting ligand Glu-urea-Lys-HBED-CC directs the tracer to cancerous cells, while the radiometal Gallium-68 emits positrons (β+) that are detected by PET/CT or PET/MRI, enabling precise localization and visualization of the disease.
• In addition to Gallium-68, other radiolabeled variants, such as [^18F]AlF-PSMA-11 are being investigated, as the longer half-life and potentially higher image resolution of fluorine-18 may offer broader advantages for clinical imaging.

Collectively, these variants establish PSMA-HBED-CC as a benchmark tracer for diagnostic imaging and staging of prostate cancer.

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Research areas and applications of HBED-CC-PSMA, CAS: 1366302-52-4:

• Prostate cancer imaging research: Widely studied as a ⁶⁸Ga-labeled PET tracer (INN: Gozetotide) for detecting primary prostate tumors, lymph node involvement, and distant metastases.
• Early detection and staging studies: Applied in research to identify prostate cancer at an early stage and determine the extent of disease spread.
• Tumor recurrence investigations: Used to identify sites of recurrent prostate cancer, even at very low PSA levels, to guide timely treatment decisions.
• Theranostic framework research: Functions as the diagnostic partner for therapeutic PSMA ligands (e.g., ¹⁷⁷Lu-PSMA-617), enabling integrated imaging and therapy.
• Tumor heterogeneity studies: Utilized to assess differences in PSMA expression across lesions within the same patient, guiding treatment decisions.
• Comparative tracer research: Studied alongside other PSMA-targeting agents to evaluate differences in affinity, kinetics, and clinical performance.
• Exploration in non-prostatic PSMA-expressing diseases: Investigated in other cancers with reported PSMA expression, including glioblastoma, renal cell carcinoma, and hepatocellular carcinoma.
• Dosimetry and radiation safety studies: Studied to measure radiation absorbed by organs and tumors after administration, supporting safer and more personalized therapy planning.
• Pharmacokinetic and biodistribution research: Studied to understand how it is cleared from the body, which organs it accumulates in (especially kidneys and salivary glands), and how effectively it targets prostate cancer tumors.

Benefits of Gozetotide (Glu-urea-Lys(Ahx)-HBED-CC):

• High specificity and affinity for PSMA: Precisely targets prostate cancer cells with exceptional selectivity.
• Stable radiolabeling: The HBED-CC chelator enables reliable and efficient Gallium-68 labeling.
• Clear PET/CT imaging: PSMA-expressing tissues can be visualized clearly and accurately in PET/CT scans.
• Reliable pharmacokinetics: Shows rapid tumor uptake combined with fast clearance from non-target tissues.
• Gold standard tracer for prostate cancer diagnosis: Recognized as the benchmark tracer, supporting accurate diagnosis, staging, and recurrence detection.

Key Concepts

What is a HBED/HBED-CC chelator?

HBED (N,N’-bis(2-hydroxybenzyl)ethylenediamine-N,N’-diacetic acid) is a chelating agent originally developed for binding metal ions. It provides six donor atoms that strongly coordinate trivalent cations like Fe3+ and Ga3+, yielding highly stable complexes.

Its most popular derivative, HBED-CC (N,N’-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N’-diacetic acid), preserves this hexadentate framework but introduces carboxyethyl substituents on the aromatic rings, which add reactive carboxyl groups for efficient conjugation to peptides, antibodies, or small-molecule ligands.

• Through its propionic acid groups, HBED-CC rapidly and stably binds Ga3+ under mild conditions and enables versatile tracer design.
• Widely used in radiopharmaceutical chemistry, it maintains excellent thermodynamic stability and kinetic inertness, preventing radionuclide dissociation that could impair image quality or safety.

In PSMA-11, this chelator links the Glu-urea-Lys pharmacophore to the radionuclide (e.g., GA-68), enabling selective PSMA targeting and yielding benchmark PET tracers for prostate cancer diagnostics.

What is a pharmacophore?

In medicinal chemistry, a pharmacophore is defined as the minimal set of structural features in a molecule that is essential for its interaction with a biological target.

In PSMA-11, the pharmacophore is the Glu-urea-Lys binding motif, designed to mimic natural glutamate-containing substrates of prostate-specific membrane antigen (PSMA, also known as glutamate carboxypeptidase II).

• PSMA normally cleaves terminal glutamate residues, but the central urea bond linked to the glutamate residue in PSMA 11 cannot be hydrolyzed, making the motif a potent inhibitor that locks into the enzyme’s active site. This inhibitory interaction ensures high affinity and specificity for PSMA-expressing tumor cells, providing the structural basis for the selective targeting observed in HBED-CC-PSMA radioligands.
• In addition, the lysine residue functions as a handle to link the pharmacophore to the HBED-CC chelator for radiolabeling and imaging.

What are radionuclides and radioligands?

Radionuclides are unstable isotopes of elements that emit radiation as they decay, such as gamma rays, beta particles, or alpha particles. Because of these emissions, they can be detected with imaging systems or used therapeutically to deliver cytotoxic radiation to diseased tissue.

Radioligands are molecules that are specifically designed to bind to a biological target, such as a receptor or enzyme, through a ligand and are also labeled with a radionuclide. By combining the targeting ability of the ligand with the radioactive signal of the radionuclide, radioligands can be used either for imaging (e.g., PET or SPECT scans) or for therapy (e.g., targeted radionuclide therapy). This dual role makes them essential tools in both diagnostics and personalized treatment approaches, especially in oncology.

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