Novel Tumor Antigen Binding Agents and Uses Thereof

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent discloses a new class of compounds that specifically bind to tumor antigens, particularly prostate-specific membrane antigen (PSMA), and are optimized for use as diagnostic or therapeutic radiopharmaceuticals. The key innovation is the use of ibuprofen as an albumin binding entity in these agents, improving their stability and pharmacokinetic profile. These compounds are designed to better target and visualize tumors (e.g., via PET or SPECT imaging), or deliver targeted radiotherapy, with enhanced tumor uptake and optimized clearance from the body, potentially reducing side effects and off-target toxicity.

Use CasesContent extracted from patent full text and abstract with AI.

• Early and accurate diagnosis of prostate cancer using targeted radiotracers in PET or SPECT imaging.
• Therapeutic treatment of cancers (including prostate, pancreatic, renal, and bladder cancer) by delivering radioactive payloads directly to tumor cells expressing the target antigen.
• Monitoring disease progression or recurrence in cancer patients via highly specific tumor imaging agents.
• Research tools for studying tumor antigen expression and distribution in preclinical and clinical settings.
• Development of companion diagnostics for personalized cancer therapy based on PSMA expression.

BenefitsContent extracted from patent full text and abstract with AI.

• Enhanced selectivity and high affinity for tumor-associated antigens, especially PSMA, leading to increased tumor uptake.
• Favorable pharmacokinetics due to ibuprofen-mediated albumin binding: improved blood circulation time and optimized tumor/background ratios.
• Reduced accumulation in non-tumor tissues, thereby minimizing radiation exposure to healthy organs such as kidneys and salivary glands.
• Improved safety profile and reduced side effects compared to earlier generations of radiopharmaceuticals.
• Flexibility for both diagnostic (imaging) and therapeutic (radiotherapy) applications within a single molecular platform ('theranostics').
• Potential for lower administered doses due to increased targeting efficiency.

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Patent Abstract

The present invention provides compounds according to General Formula (1 )(i) or (1 )(ii): wherein A is a diagnostic or therapeutic agent comprising a binding site for a tumor antigen, and the spacer comprises at least one C-N bond.