DOTA-TATE
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| Names | |
|---|---|
| Other names
DOTA-(Tyr3)-octreotate | |
| Identifiers | |
| 177943-89-4 | |
| 3D model (Jmol) | Interactive image |
| ChemSpider | 9345959 |
| PubChem | 11170867 |
| |
| |
| Properties | |
| C65H90N14O19S2 | |
| Molar mass | 1,435.63 g·mol−1 |
| Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| Infobox references | |
DOTA-TATE, DOTATATE or DOTA-octreotate is a substance which, when bound to various radionuclides, has been tested for the treatment and diagnosis of certain types of cancer, mainly neuroendocrine tumours.
Chemistry and mechanism of action
DOTA-TATE is an amide of the acid DOTA (top left in the image), which acts as a chelator for a radionuclide, and (Tyr3)-octreotate, a derivative of octreotide. The latter binds to somatostatin receptors, which are found on the cell surfaces of a number of neuroendocrine tumours, and thus directs the radioactivity into the tumour.
Usage examples
Gallium (68Ga) DOTA-TATE (GaTate[1]) is used for tumour diagnosis in positron emission tomography (PET).[2] DOTA-TATE PET/CT has a much higher sensitivity compared to In-111 octreotide imaging.[1]
Lutetium (177Lu) DOTA-TATE[3] has been tested for the treatment of tumors such as carcinoid and endocrine pancreatic tumor.
Patients are typically treated with an intravenous infusion of 7.5 GBq of lutetium-177 octreotate. After about four to six hours, the exposure rate of the patient has fallen to less than 25 microsieverts per hour at one metre and the patients can be discharged from hospital.
A course of therapy consists of four infusions at three monthly intervals.[4]
Availability
Lu177 octreotate therapy is currently available under research protocols in four different medical centers in North America: Quebec City, (Qc), Edmonton, (Ab), London, (On) as Houston (Tx) on clinical trial.[5] Medical centers in Europe also offer this treatment. For instance: Uppsala Centre of Excellence in Neuroendocrine Tumors in Sweden and Erasmus University in the Netherlands.[6] In Israel, treatment is available at Hadassah Ein Kerem Medical Center. In Australia, treatment is available at Liverpool Hospital and St Vincent's Hospital, Sydney;[7] the Peter MacCallum Cancer Centre [1] and at the Department of Nuclear Medicine at Fremantle Hospital in Western Australia.[8] In Aarhus universitet hospital in Denmark. In the coming years such therapy will also become commercially available in Latvia, Riga - "Clinic of nuclear medicine".
See also
- DOTATOC or edotreotide, a similar compound
References
- 1 2 3 Hofman, M. S.; Kong, G.; Neels, O. C.; Eu, P.; Hong, E.; Hicks, R. J. (2012). "High management impact of Ga-68 DOTATATE (GaTate) PET/CT for imaging neuroendocrine and other somatostatin expressing tumours". Journal of Medical Imaging and Radiation Oncology. 56 (1): 40–47. doi:10.1111/j.1754-9485.2011.02327.x. PMID 22339744.
- ↑ Breeman, W. A. P.; De Blois, E.; Sze Chan, H.; Konijnenberg, M.; Kwekkeboom, D. J.; Krenning, E. P. (2011). "68Ga-labeled DOTA-Peptides and 68Ga-labeled Radiopharmaceuticals for Positron Emission Tomography: Current Status of Research, Clinical Applications, and Future Perspectives". Seminars in Nuclear Medicine. 41 (4): 314–321. doi:10.1053/j.semnuclmed.2011.02.001. PMID 21624565.
- ↑ Bodei, L.; Cremonesi, M.; Grana, C. M.; Fazio, N.; Iodice, S.; Baio, S. M.; Bartolomei, M.; Lombardo, D.; Ferrari, M. E.; Sansovini, M.; Chinol, M.; Paganelli, G. (2011). "Peptide receptor radionuclide therapy with 177Lu-DOTATATE: The IEO phase I-II study". European Journal of Nuclear Medicine and Molecular Imaging. 38 (12): 2125–2135. doi:10.1007/s00259-011-1902-1. PMID 21892623.
- ↑ Claringbold, P. G.; Brayshaw, P. A.; Price, R. A.; Turner, J. H. (2010). "Phase II study of radiopeptide 177Lu-octreotate and capecitabine therapy of progressive disseminated neuroendocrine tumours". European Journal of Nuclear Medicine and Molecular Imaging. 38 (2): 302–311. doi:10.1007/s00259-010-1631-x. PMID 21052661.
- ↑ Clinical trial number NCT01237457 for "177Lutetium-DOTA-Octreotate Therapy in Somatostatin Receptor-Expressing Neuroendocrine Neoplasms" at ClinicalTrials.gov
- ↑ "PRRT Behandelcentrum Rotterdam". PRRT Behandelcentrum Rotterdam. Erasmus Universiteit.
- ↑ http://www.swslhd.nsw.gov.au/liverpool/pet/PET.html
- ↑ Turner, J. H. (2012). "Outpatient therapeutic nuclear oncology". Annals of Nuclear Medicine. 26 (4): 289–97. doi:10.1007/s12149-011-0566-z. PMID 22222779.
- Freedman, N; Klein, M; Gross, D; Glasberg, S; Meirovitz, A; Maimon, O; Krausz, Y; Bar-Shalom, R (2014). "Lu177-DOTATATE therapy for NET: Does tumor dose predict response?". J Nucl Med. 55 (Supplement 1).