PET-pharmacokinetics of 18F-octreotide: A comparison with 67Ga-DFO and 86Y-DTPA-octreotide

Wester, Hans‐Jürgen; Βrockmann, J.; Rösch, Frank; Wutz, Walter; Herzog, Hans; Smith‐Jones, Peter; Stolz, Barbara; Berthou, Christian; Stöcklin, G.

doi:10.1016/s0969-8051(97)00039-5

Cited by 73 publications

(49 citation statements)

References 33 publications

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“…The overall yield was 62%. 1 After subsequent Fmoc-deprotection using 20% piperidine in DMF, N 2 -terminal glycosylation was achieved by reaction with Gluc(4Ac)/S-1-heptaacetyl-cellobiosyl-mercaptopropionic acid pentafluorophenyl ester (1.1 eq) in the presence of N-ethyldiisopropylamine (1.1 eq). Dde deprotection of the Lys 5 side chain was performed using 2% hydrazine hydrate in DMF, followed by removal of the acetyl protecting groups in the sugar moiety using potassium cyanide in methanol (31).…”

Section: Synthesis Of Small Organic Precursorsmentioning

confidence: 99%

“…Despite the loss of the positive charge on N ␣ of D-Phe 1 (Fig. 1) [1][2][3][4][5] has been determined ( Table 2). The corresponding 19 F reference compounds all showed very high hsst 2 affinity comparable with that of native somatostatin 28, including no affinity to hsst 1 , very low affinity to hsst 3 , and moderate affinity to hsst 4 and hsst 5 .…”

Section: Synthesismentioning

confidence: 99%

“…One significant drawback of Gluc-Lys([ 18 F]FP)-TOCA, especially with respect to clinical routine application, is generally encountered in 18 F-labeling of small bioactive peptides via prosthetic groups (1,13,14,(23)(24)(25)(26): the time consuming, multistep radiosynthesis of the [ 18 F]fluorinated precursor used for prosthetic group labeling, in this case 4-nitrophenyl 2-[…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

First 18F-Labeled Tracer Suitable for Routine Clinical Imaging of sst Receptor-Expressing Tumors Using Positron Emission Tomography

Schottelius

Poethko

Herz

et al. 2004

Clinical Cancer Research

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Section: Synthesis Of Small Organic Precursorsmentioning

confidence: 99%

Section: Synthesismentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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First 18F-Labeled Tracer Suitable for Routine Clinical Imaging of sst Receptor-Expressing Tumors Using Positron Emission Tomography

Schottelius

Poethko

Herz

et al. 2004

Clinical Cancer Research

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“…Several strategies have been studied to develop a somatostatin analog-based PET tracer using different positronemitting radionuclides. Wester et al 19 successfully labeled OC with 18 F, but despite specific accumulation in the tumor, this radioligand was of limited clinical application, owing to fast tumor washout, high liver uptake and, hence, insufficient visualization of abdominal tumors. Various 64 Cu-labeled somatostatin analogs were synthesized which showed favorable biodistribution in animal models 20,21 and good performance for PET imaging in patients; 22 however, the use of 64 Cu relies on the availability of a cyclotron.…”

mentioning

confidence: 99%

Neuroendocrine tumor targeting: Study of novel gallium‐labeled somatostatin radiopeptides in a rat pancreatic tumor model

Froidevaux

Eberlé

Christe

et al. 2002

Intl Journal of Cancer

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Somatostatin analogs labeled with radionuclides are of considerable interest in the diagnosis and therapy of SSTRexpressing tumors, such as gastroenteropancreatic, small cell lung, breast and frequently nervous system tumors. In view of the favorable physical characteristics of the Ga isotopes 67 Ga and 68 Ga, enabling conventional tumor scintigraphy, PET and possibly internal radiotherapy, we focused on the development of a Ga-labeled somatostatin analog suit- SSTRs are overexpressed by a variety of neuroendocrine tumors and frequently by tumors of the nervous system, 1-4 making somatostatin analogs, such as OC, 5 attractive candidates for tumor targeting. 111 In-labeled DTPA-OC (OctreoScan) was the first radiopeptide routinely used in the clinic for imaging SSTR-positive tumors by scintigraphy. 6 -10 A new generation of somatostatin analogs, incorporating the macrocyclic chelator DOTA instead of DTPA, have been developed, which ensure better stability of the radiometal-peptide complex. After labeling with 90 Y (␤ --emitter 2.28 MeV, t 1 ⁄2 64.1 hr) or 111 In (␥-emitter, Auger-and conversionelectron emitter, 0.5-245 keV, t 1 ⁄2 67.9 hr), they showed improved biodistribution and tumor uptake in animal models [11][12][13] and their clinical utility as diagnostic and therapeutic tools was confirmed in patients. 14 -18 These findings prompted us and others to develop somatostatin analogs suitable for PET, which offers higher sensitivity and resolution than SPECT, making it possible to visualize very small metastatic lesions, including tumor deposits in regional draining lymph nodes. Several strategies have been studied to develop a somatostatin analog-based PET tracer using different positronemitting radionuclides. Wester et al. 19 successfully labeled OC with 18 F, but despite specific accumulation in the tumor, this radioligand was of limited clinical application, owing to fast tumor washout, high liver uptake and, hence, insufficient visualization of abdominal tumors. Various 64 Cu-labeled somatostatin analogs were synthesized which showed favorable biodistribution in animal models 20,21 and good performance for PET imaging in patients; 22 however, the use of 64 Cu relies on the availability of a cyclotron.Another interesting positron emitter is 68 Ga (t 1 ⁄2 68 min, ␤ ϩ 88%), which is produced by a 68 Ge/ 68 Ga generator available at most PET centers and is not dependent on a cyclotron. Gallium as radiometal is of even broader interest in nuclear medicine because it is also available as 67 Ga (t 1 ⁄2 78 hr), which is not only a ␥-emitter useful for tumor diagnosis (␥-camera scintigraphy, SPECT) but also an emitter of Auger (0.1-8 keV) and conversion (80 -90 keV) electrons, which makes it attractive for internal radiotherapy. 23 The radiotoxicity of 67 Ga has been demonstrated in vitro in a lymphoma cell line 24 and myeloid leukemic blasts. 25 The use of a low-energy emitter might increase the therapeutic index because most of the electrons deposit their energy within the target, i.e., the tumor, thereby min...

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“…For example, somatostatin derivatives radiolabeled with F-18, Y-86 or Ga-68 are extensively studied in patients with neuroendocrine tumors [54,55,56]. …”

Section: Future Developmentsmentioning

confidence: 99%

Controversies in the Management of Colorectal Liver Metastases: Role of PET and PET/CT

Wiering

Vogel²,

Ruers³

et al. 2008

Dig Surg

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Positron emission tomography (PET) using [F-18]-2-deoxy-2-fluoro-D-glucose (FDG) has emerged as a promising diagnostic modality in recurrent colorectal cancer. Data in the literature show that the addition of FDG-PET changes patient management in up to 30% of patients with potentially resectable liver metastases, mainly by detecting previously unknown extrahepatic disease. Furthermore, FDG-PET is useful in the follow-up of patients who underwent surgical procedures of the liver, since it is sensitive in detecting residual or relapse malignancy in scarred liver tissue following both resection and local ablative techniques. For follow-up during systemic therapy, early FDG-PET appears predictive for response to therapy. FDG-PET, computerized tomography and magnetic resonance imaging are complementary techniques in staging and restaging patients with advanced colorectal cancer. A combination of FDG-PET and CT scanning characteristics seems promising, and integrated PET/ CT is becoming more widely available, although the exact clinical value and efficacy is not yet fully established. In addition, assessment of these modalities in joint reading sessions with radiologist, nuclear medicine physician, medical and surgical oncologists significantly impacts upon patient management. This review evaluates the potential of FDG-PET and combined PET/CT in patients with colorectal liver metastases and discusses potential future possibilities.

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PET-pharmacokinetics of 18F-octreotide: A comparison with 67Ga-DFO and 86Y-DTPA-octreotide

Cited by 73 publications

References 33 publications

First 18F-Labeled Tracer Suitable for Routine Clinical Imaging of sst Receptor-Expressing Tumors Using Positron Emission Tomography

First 18F-Labeled Tracer Suitable for Routine Clinical Imaging of sst Receptor-Expressing Tumors Using Positron Emission Tomography

Neuroendocrine tumor targeting: Study of novel gallium‐labeled somatostatin radiopeptides in a rat pancreatic tumor model

Controversies in the Management of Colorectal Liver Metastases: Role of PET and PET/CT

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