- PSMA-TARGETED RADIOPHARMACEUTICAL FOR DIAGNOSING AND TREATING PROSTATE CANCER
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The present invention relates to a pharmaceutical composition for diagnosing and treating prostate cancer, capable of targeting PSMA, and a compound provided by one aspect of the present invention has a glutamine-urea-lysine compound to which a radioactive metal-coupled chelator is structurally coupled and to which an aryl group that can additionally bind to PSMA protein is coupled. Coupling between the glutamine-urea-lysine compound and the chelator includes a polar spacer so as to serve the role of reducing in vivo nonspecific coupling and exhibit an effect of being rapidly removed from vital organs, but not from prostate cancer. These characteristics lower the radiation exposure, which is caused by a therapeutic radioisotope-coupled compound, to normal tissue and organs, and thus reduce side effects. In addition, a compound that contains a phenyl group having a coupling force with albumin has an increased residence time in the blood, thereby becoming more accumulated in prostate cancer.
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Paragraph 0183; 0184
(2021/02/18)
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- 18F-LABELLED COMPOUND FOR PROSTATE CANCER DIAGNOSIS, AND USE THEREOF
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The present invention relates to an 18F-labelled compound, and a use thereof. The compound selectively binds to a prostate-specific membrane antigen (PSMA), and enables the acquisition of clear prostate cancer images in a short time when used in positron
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Paragraph 0062-0063
(2020/05/30)
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- PROCESS FOR PRODUCTION OF HETERODIMERS OF GLUTAMIC ACID
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A manufacturing process for the preparation of radiolabeled compounds of formula (I) includes reacting compounds of formula (II) with a source of readionuclide of a halogen in the presence of an oxidant under acidic condition, wherein: *I is 123I, 124I, 125I or 131I; R is lower alkyl, optionally substituted with one or more fluorine atoms; Q is C(O), O, NR', S, S(O)2, C(O)2, (CH2)P; Y is C(O), O, NR', S, S(O)2, C(O)2, (CH2)P; R is H, C(O), S(O)2, C(O)2; Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl; m is O, 1, 2, 3, 4 or 5; n is O, 1, 2, 3, 4, 5 or 6; and p is O, 1, 2, 3, 4, 5 or 6.
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Page/Page column 20-22
(2010/12/31)
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- A series of halogenated heterodimeric inhibitors of prostate specific membrane antigen (PSMA) as radiolabeled probes for targeting prostate cancer
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Prostate specific membrane antigen (PSMA) is a validated molecular marker for prostate cancer. A series of glutamate-urea (Glu-urea-X) heterodimeric inhibitors of PSMA were designed and synthesized where X = ε-N-(o-I, m-I, p-I, p-Br, o-Cl, m-Cl, p-Cl, p-F
- Maresca,Hillier,Femia,Keith,Barone,Joyal,Zimmerman,Kozikowski,Barrett,Eckelman,Babich
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experimental part
p. 347 - 357
(2009/10/17)
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