DOTA-TATE

From Wikipedia, the free encyclopedia
  (Redirected from Lutetium (177Lu) DOTA-octreotate)
Jump to: navigation, search
DOTA-TATE
DOTATATE.svg
Identifiers
CAS number 177943-89-4
Jmol-3D images Image 1
Properties
Molecular formula C65H90N14O19S2
Molar mass 1,435.62 g mol−1
Except where noted otherwise, 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[edit]

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[edit]

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. It is presently available in North America in Quebec City, Quebec, Edmonton, Alberta and London, Ontario (Canada) as an approved therapeutic and in Houston on clinical trial,[4] which may soon be expanding to additional cancer centers as a multicenter study.[citation needed] Select medical centers in Europe offer this treatment, for instance Uppsala Centre of Excellence in Neuroendocrine Tumors in Sweden and Erasmus University.[citation needed] in the Netherlands. In Israel, treatment is available at Hadassah Ein Kerem Medical Center. In Australia, treatment is available at the Peter MacCallum Cancer Centre [1] and at the Department of Nuclear Medicine at Fremantle Hospital in Western Australia.[5] At Fremantle Hospital, patients are 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.[6]

See also[edit]

  • DOTATOC or edotreotide, a similar compound

References[edit]

  1. ^ a b c 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.  edit
  2. ^ 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.  edit
  3. ^ 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.  edit
  4. ^ ClinicalTrials.gov NCT01237457 177Lutetium-DOTA-Octreotate Therapy in Somatostatin Receptor-Expressing Neuroendocrine Neoplasms
  5. ^ 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.  edit
  6. ^ 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.  edit