Treating oncologic diseases successfully, continues to be challenging. In recent years much attention has been drawn to the use of theranostic agents, consisting both alpha and beta emitting radionuclides. Although results are encouraging, several weaknesses persist. For example, Lutetium-177 PSMA-617 ( Lu-177-PSMA-617), used widely in many countries, targets prostate specific membrane antigen (PSMA) expressed on prostate cancer (PCa) cell membrane, i) eliminates 10-15% of the PCa patients from treatment, ii) induces mild to severe xerostomia, requiring botulinum toxin treatment of salivary glands ,iii) risks renal impairment, iv) induces , a considerable myelotoxicity and v) creates , due to Lu-177m contaminant, a radioactive waste disposal problem particularly for patients who are incontinent and wear diapers. We have developed a small radioactive molecule (Cu-64-TP3805) with a high affinity (Kd 3.1 x 10 -9M) for genomic, VPAC receptors expressed in high density on cells of all PCa type, that detects, in humans, primary PCa, bone metastatic lesions and malignant lymph nodes with &gt;95% sensitivity. The agent has no urinary excretion, has no salivary gland or bone marrow uptake and has only a small uptake in the renal cortex, not sensitive to radiation damage. Beta emitting Copper-67, (t½= 2.6 d, γ-185 KeV (40%) ,βmax- 580 KeV) can be easily used to synthesize Cu-67-TP3805. Since i) the tissue penetration range (0.6 mm) and the linear energy transfer for Cu-67 is the same as Lu-177,and ii) Cu-67-TP3805, will have, the same tissue distribution as that of Cu-64-TP-3805 with high uptake both in primary PCa and metastatic lesions, iii) no urinary excretion, iv) no salivary gland uptake, v) no bone marrow uptake, Cu-67-TP3805 treatment will be readily applicable to all PCa patients without having to perform patient suitability examination or any anti-toxicity treatment. The data will be discussed.

VPAC targeted Cu-67-TP3805 for prostate cancer therapy

ACS Spring Meeting 2021

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