Novel albumin binder for improving the targeting efficacy of diagnostic or therapeutic reagents

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Albumin binders have been developed to improve tumor uptake of therapeutic radioisotopes (radiopeptides) by prolonging radiopeptide blood circulation.  However, use of these albumin binders also results in an increased uptake of radiopeptide in healthy organs, negating the benefits of the treatment.  Researchers at Oregon Health & Science University have developed a new class of albumin binder that significantly increases tumor uptake without negatively impacting non-tumor organs, thereby allowing for an improved therapeutic index.

Technology Overview

Radiopeptide therapy is an important treatment modality for cancer, particularly in metastatic and highly disseminated disease where surgery or conventional radiation therapy may no longer be possible.  It involves the use of a targeting agent (for example, an antibody, peptide, or small molecule) labeled with a therapeutic radioisotope to deliver a cytotoxic dose of radiation to the targeted cancer cells.  However, despite the initial promise of radiopeptide therapy, low tumor uptake and fast tumor clearance resulted in an insufficient radiation dose on tumor, tempering enthusiasm for this therapeutic modality.  Over the past decade, a number of small molecule albumin binders have been developed to improve tumor uptake of radiopeptides by prolonging their bioavailability in the blood.  Among them, 4-(p-iodophenyl) butyric acid (ABI) and Evans Blue (EB) are the two most studied albumin binders.  Although high tumor uptake was observed with ABI and EB conjugated radiopeptides, their use also led to increased uptake in healthy organs (such as blood, red bone marrow, kidneys), resulting in a reduced radiotherapeutic index (tumor radiation dose/non-tumor radiation dose).

In order to improve tumor uptake and also enhance tumor/non-tumor ratios, OHSU researchers invented a novel reversible small-molecule albumin binder, which exhibits comparable tumor uptake and greatly enhanced tumor/non-tumor uptake ratio, compared to ABI.  Moreover, the novel albumin binder-radiopeptide exhibited an 8-fold higher uptake in pancreatic tumors in the KPC mouse tumor model, compared to normal tissue in a healthy wildtype mouse, while the non-tumor uptake in both the diseased and control mice was similar (Fig. 1).


Figure 1. Evaluation of albumin binder-radiopeptide: A) PET/CT images; and b) post-imaging ex vivo biodistribution.

OHSU’s improved albumin binder will greatly benefit cancer patients by enhancing the radiopeptide therapeutic index and reducing the radiation dose needed to kill tumor cells. This albumin binder is a versatile platform technology, as it can be incorporated into a variety of peptide/small molecule-based radioligands to improve their tumor uptake and tumor/non-tumor ratios in therapeutic and diagnostic applications.

Licensing Opportunity

This technology is available for exclusive licensing and/or collaborative co-development. 



Patent Information:
For Information, Contact:
Anne Carlson
Assoc Dir, Tech Dev & Licensing
Oregon Health & Science University
Dexing Zeng
Lingyi Sun
Zhonghan Li
Diagnostics - Cancer
Therapeutics - Cancer
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