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KDDF-201712-12 Development of Novel Radiopharmaceutical for Prostate Specific Membrane Antigen Targeted Therapy(Oncology, Chemical) [2020-06-24]

Ongoing Project
Section Lead
Preclinical Phase I Phase II Phase III

Development and Market Objectives

Recent published studies have raised the possibility of targeted radionuclide therapies such as 177 Lutetium-PSMA as a viable therapeutic treatment in men with metastatic prostate cancer. The aim of this project is to develop a cold kit of Lu-177 labelled PSMA-targeting tracer and complete the pre-clinical and IND application for this new radio-pharmaceutical.

Unmet Medical Need & Target Patients

Prostate cancer (PCa) is one of the major cancers affecting men and a significant population of elderly patients suffers from this the world over. Although many patients present with localized or indolent disease, there are still a signi?cant proportion of patients that eventually progress to advanced metastatic disease, for which no curative treatment exists. In men who fail initial therapy of curative intent (radical prostatectomy or primary radiotherapy), treatment options include androgen deprivation therapy followed by chemotherapy if the disease progresses. However, conventional chemotherapy responses are often transient, leaving many men with symptomatic metastatic cancer and few treatment options.


Because of the high international incidence of Pca, and in particular, the advanced disease presenting with skeletal metastases and cells with resistance to androgen therapy, chemotherapy and orchidectomy, extensive research is focused on the development of many types of technologies both for the high resolution visualization/detection of prostate cancer lesions, as well as cost effective and selective therapeutic technologies. Therefore, developing new strategies for diagnosis, imaging and treatment of metastatic prostate cancer is of major importance.


On prostate cancer (PC) cells, the cell surface enzyme prostate-speci?c membrane antigen (PSMA), also known as glutamate carboxypeptidase II or N-acetyl-L-aspartylL-glutamate peptidase, is highly upregulated, whereas it shows low or no expression in the normal prostate. PSMA expression correlates with the malignancy of the disease, being further increased in metastatic and hormone-refractory patients. As a consequence, PSMA has attracted attention as a target for molecular imaging and for targeted radioligand therapy, especially in metastatic castrate-resistant prostate cancer (mCRPC).


Cellbion is focusing on the development of radiopharmaceuticals for both diagnosis and therapy of prostate cancer mainly based on PSMA as a target molecule. This compound is composed of Glutamate-Urea-Lysine moiety known as a pharmacophore for PSMA inhibitors, and a chelating agent for a radioisotope connected by a linker. This linker is distinctive to make this molecule stable and safe in blood plasma.


Development of process for mass production of PSMA-GUL-DOTA is completed and validation for efficacy is being performed by pre-clinical test.

Intellectual Property

- Registered patent in Korea

- Title ; Peptide thiourea derivatives, their radioisotope labeled compounds and pharmaceutical composition for treatment or diagnosis of prostate cancer comprising the same as an active ingredient

- PCT examined by International Preliminary Examining Authorities and preparing National Phase Entry

Competitive Advantages

- PSMA targeting radiopharmaceuticals with small molecular weight

- Stable molecule due to linker between pharmacophore peptide and a chelating agent

- GMP manufacturing facility

Contact & Company Overview

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