Nuclear Imaging and Radiotherapeutics Agents Targeting Carbonic Anhydrase IX (second generation)

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Unmet Need
Clear cell renal cell carcinoma (ccRCC) is the most common type of cancer affecting kidney in adults, accounting for up to 70% of renal cell carcinomas (RCCs). When small (< 4 cm) and localized within the kidney, ccRCCs are indistinguishable from a number of benign renal masses on the basis of most technologies and methods currently available. Biopsy of renal masses can distinguish between benign and malignant lesions, however, this procedure is often forgone due to a relatively high rate of non-diagnostic procedures and the potential for complications. Although the majority of patients with small renal tumors are cured with surgery alone, up to 30% of patients with ccRCC will experience a recurrence following extirpation. Substantial clinical needs remain for improved imaging of ccRCC to enhance initial surgical resection and prevent long-term disease recurrence.
Technology Overview
Dr. Martin Pomper and colleagues have developed novel low-molecular-weight ligands (LWM) of carbonic anhydrase IX (CAIX). These potent and selective CAIX ligands are armed with a dual-targeting moiety and conjugated with metal chelators, metal complexes and fluorine prosthetic groups, enabling radio-labeling with a wide array of PET, SPECT and radiotherapeutic isotopes. This novel technology overcomes the limitations of similarly existing products by enhancing specificity for CAIX ligands, enabling detection with existing clinical instrumentation, and reducing non-specific organ uptake. Use of radioisotope-labeled CAIX targeting agents stand to enable a wide range of imaging and therapeutic applications.

Stage of Development 
Proof of concept experiments completed in a mouse xenograft tumor model.  Agents exhibit selective tumor uptake and pharmacokinetic properties suitable for clinical imaging.

Related Technologies

C13559, C14017



Oncotarget (2015), 6(32), 33733-42; Oncotarget (2016), 7(35), 56471-56479

Patent Information:
Title App Type Country Serial No. Patent No. File Date Issued Date Expire Date Patent Status
Nuclear Imaging and Radiotherapeutics Agents Targeting Carbonic Anhydrase IX (second generation) PCT: Patent Cooperation Treaty PCT PCT/US2017/032384   5/12/2017     Pending
For Information, Contact:
Jeanine Pennington
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