2009
DOI: 10.1158/0008-5472.can-09-1682
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Abstract: Prostate-specific membrane antigen (PSMA) is expressed in normal human prostate epithelium and is highly upregulated in prostate cancer. We previously reported a series of novel small molecule inhibitors targeting PSMA. Two compounds, MIP-1072, (S)-2-(3-((S)-1-carboxy-5-(4–iodobenzylamino)pentyl)ureido)pentanedioic acid and MIP-1095, (S)-2-(3-((S)-1-carboxy-5-(3-(4-iodophenyl)ureido)pentyl)ureido)pentanedioic acid, were selected for further evaluation. MIP-1072 and MIP-1095 potently inhibited the glutamate car… Show more

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Cited by 279 publications
(270 citation statements)
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“…During the last 2 decades, many efforts have been undertaken to develop PSMA ligands (8)(9)(10)(11)(12)(13)(14)(15)(16). One of these ligands, the smallmolecule Glu-NH-CO-NH-Lys-(Ahx)-[ 68 Ga(HBED-CC)], also known as PSMA-11, PSMA HBED , Glu-CO-Lys(Ahx)-HBED-CC, DKFZ-PSMA-11, PSMA-HBED-CC, PSMA-HBED, PSMA, or Prostamedix, developed at the German Cancer Research Center Heidelberg (DKFZ), has become the most clinically used radiotracer.…”
mentioning
confidence: 99%
“…During the last 2 decades, many efforts have been undertaken to develop PSMA ligands (8)(9)(10)(11)(12)(13)(14)(15)(16). One of these ligands, the smallmolecule Glu-NH-CO-NH-Lys-(Ahx)-[ 68 Ga(HBED-CC)], also known as PSMA-11, PSMA HBED , Glu-CO-Lys(Ahx)-HBED-CC, DKFZ-PSMA-11, PSMA-HBED-CC, PSMA-HBED, PSMA, or Prostamedix, developed at the German Cancer Research Center Heidelberg (DKFZ), has become the most clinically used radiotracer.…”
mentioning
confidence: 99%
“…Can the lessons learned from multiple successesfor the imaging of PC were introduced into clinical settings in 2008 by Molecular Insight Pharmaceuticals, Inc. (MIP, now a subsidiary of Progenics Pharmaceuticals Inc.) (ClinicalTrials.gov identifier: NCT00712829). These ligands, 123 I-MIP-1072 and 123 I-MIP-1095, were based on the Glu-urea-Lys motif and contained aromatic substituents for stable introduction of the single-photon-emitting radionuclide 123 I (half-life, 13.2 h) (5,6). However, worldwide, 68 Ga-PSMA-11 currently is the most prominent 68 Ga-labeled PSMA radioligand for the PET imaging of PSMA-positive PC.…”
mentioning
confidence: 99%
“…The first clinical theranostic approach with radioiodinated versions of PSMA inhibitor MIP-1095 for the treatment of patients with late-stage disease (that is, metastatic castration-resistant PC) was reported in 2014 (18). The tracer MIP-1095 was first described by Hillier et al in 2009 (Fig. 3) (5), and the first-in-human evaluation of the 123 I-labeled version was finally published in 2013 (19).…”
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confidence: 99%
“…However, minimizing kidney uptake without losing tumor dose is a real challenge because PSMA is physiologically expressed in the kidney tubules (1). The pharmacokinetics of MIP1072 versus MIP1095 in animals have already been evaluated in detail (7,14). The authors of the mentioned studies reported a similar accumulation of both compounds in PSMA-expressing LNCaP xenografts but with very different pharmacokinetic profiles.…”
mentioning
confidence: 99%