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Case Reports in Surgery and Invasive Procedures | Volume 3

March 11-12, 2019 | London, UK

Biomarkers

Plastic and Cosmetic Surgery

International Conference on

International Conference on

Joint Event

&

In vitro

evaluation of the new radiotracer

99m

Tc-HYNIC-PSMA for prostate cancer diagnosis

Monika Orzelowska, Michał Maurin

and

Piotr Garnuszek

National Centre for Nuclear Research Radioisotope Centre POLATOM, Poland

Introduction:

Prostate cancer is the second commonly occurring

malignance in men. The selection of an effective therapy form

depends on the proper assessment of the disease progression.

The prostate-specific membrane antigen (PSMA) is becoming

increasingly recognizedas a viable target for imaging and therapy

of prostate and other types of cancer.

As it is important to fully characterize the properties of

radiolabelled compounds before in vivo studies, the aim

of this work was to evaluate the in vitro biological activity

of new developed PSMA inhibitor -

99m

Tc-HYNIC-PSMA-

potential tracer for SPECT diagnosis of prostate cancer.

Method:

Saturationbindingassaywasperformedtodetermine

specificity of binding, dissociation constant (Kd) and maximal

concentration of receptors on the cell surface (Bmax). HYNIC-

PSMA inhibitor was labelled with

99m

Tc. The binding of

99m

Tc-

HYNIC-PSMA was evaluated by carrying out the studies using

the cellmembranes isolated fromLNCaP cells. Thenon-specific

binding was determined using membranes isolated from PC3

cells known not to express PSMA. IC50 values of the tested

compounds were determined by competitive binding assay

on LNCaP cell membranes using 131I-MIP1095 radioligand

with known high affinity to PSMA (IC50=0.3). As a reference

substance, PSMA11 was used.

Results:

99m

Tc-PSMA-T4 showed high specific affinity to

PSMA, which represented 99% of total binding. The Kd value

determined from the specific binding of the tested radioligand

was 5.47 nMand the Bmax was 9533 pmol/mg. The IC50 value

of HYNIC-PSMA was assessed at the level of 79.5 and it was 10

times lower than value obtained for PSMA11.

Conclusion:

High specific binding of

99m

Tc-HYNIC-PSMA to

the PSMA suggests its huge potential for prostate cancer

diagnosis. Comparison of the affinities of

99m

Tc-HYNIC-PSMA

and 68Ga-PSMA11 points out that despite SPECT technique

has a lower spatial resolution than PET,

99m

Tc-HYNIC-PSMA

can be a useful alternative in diagnosis and staging of prostate

cancer.

Speaker Biography

Monika Orzełowska graduated in Biotechnology from the Faculty of Biology and

Biotechnology in Maria-Curie Sklodowska University in Lublin, Poland. She obtained a

master’s degree in 2014. In August 2015, she started work in R&D Department at National

Centre for Nuclear Research, Radioisotope Centre POLATOM.

e:

Monika.Orzelowska@polatom.pl