Total chemical synthesis of PSMA-11: API for 68Ga-PSMA-11 used for prostate cancer diagnosis
The imaging of prostate tumours by targeting Prostate Specific Membrane Antigen (PSMA), using binding tracer, 68Ga-PSMA-11, offer lots of promises for specific detection of prostate associated malignancies. The popularity of 68Ga-PSMA-11 as a radioligand tool for prostate cancer diagnosis has gained...
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Main Authors: | , |
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Format: | Book |
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Elsevier,
2021-12-01T00:00:00Z.
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Summary: | The imaging of prostate tumours by targeting Prostate Specific Membrane Antigen (PSMA), using binding tracer, 68Ga-PSMA-11, offer lots of promises for specific detection of prostate associated malignancies. The popularity of 68Ga-PSMA-11 as a radioligand tool for prostate cancer diagnosis has gained a major boost upon its FDA approval in December 2020. Development of an economically benign protocol for the synthesis of PSMA-11, using solution phase method, is particularly important to get a better access to this highly important and expensive Active Pharmaceutical Ingredient (API). The PSMA-11 synthesized using the protocol presented here, involves the use of a flow reactor based catalytic hydrogenation as the key step. Using the method portrayed, PSMA-11 with purity >99.5% was achieved, while, radiolabelling with 68Ga afforded 68Ga-PSMA-11 with radiochemical purity >95%, which is appropriate for imaging applications. |
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Item Description: | 2772-4174 10.1016/j.ejmcr.2021.100014 |