Technology ID

Evans Blue Modified Small Molecule-based Prostate-specific Membrane Antigen (PSMA) Radiotherapy and Nuclear Imaging

Lead Inventor
Chen, Xiaoyuan (Shawn) (NIBIB)
Jacobson weiss, Orit (NIBIB)
Therapeutic Areas
Development Stages
Clinical Phase I
Research Products
Lead IC

This technology includes anti-PSMA antibody labeled with 177Lu, which has shown to be an effective treatment for prostate cancer. Several small molecules targeting PSMA were also evaluated in prostate cancer patients labeled with betta emitters such as 177Lu. The most common one is 177Lu-PSMA-617 which is under clinical evaluation in many countries. Usual treatment in patients in most clinical trials was composed of up to 3 cycles of 177Lu-PSMA-617. The limited data available suggest partial response rates of up to 70%–80% that was limited to as few as several weeks in some of the patients. Encouragingly, only stage 1 -2 hematologic toxicities and sporadically mild xerostomia and fatigue were reported as side effects.

Commercial Applications
This product will be of use in nuclear imaging and radiotherapy of PSMA-positive tumors, and the EB derivative can be used for increasing the blood half-life of small molecules targeting PSMA.

Competitive Advantages
Our modification of small molecule-based radiotherapy attaches an albumin binding domain based on the structure of Evans blue that results in significantly increased blood half-life, increased tumor uptake, and more effective anti-tumor radiotherapy. This may improve therapy of patients with PSMA-positive tumors and the general design may be applicable to other therapeutic small molecules.
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