- DOTATATE
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DOTATATE 
Other namesDOTA-(Tyr3)-octreotateIdentifiers CAS number 177943-89-4 Jmol-3D images Image 1 - c6nc2ccccc2c6CC(C(=O)NC(CCCCN)C(=O)NC1C(O)C)NC(=O)C(Cc4ccc(O)cc4)NC(=O)C(CSSCC(NC1=O)C(=O)NC(C(=O)O)C(O)C)NC(=O)C(Cc5ccccc5)NC(=O)CN(CC3)CCN(CC(=O)O)CCN(CC(O)=O)CCN3CC(=O)O
- InChI=1S/C65H90N14O19S2/c1-38(80)56-64(96)73-51(63(95)75-57(39(2)81)65(97)98)37-100-99-36-50(72-59(91)47(28-40-10-4-3-5-11-40)68-52(83)32-76-20-22-77(33-53(84)85)24-26-79(35-55(88)89)27-25-78(23-21-76)34-54(86)87)62(94)70-48(29-41-15-17-43(82)18-16-41)60(92)71-49(30-42-31-67-45-13-7-6-12-44(42)45)61(93)69-46(58(90)74-56)14-8-9-19-66/h3-7,10-13,15-18,31,38-39,46-51,56-57,67,80-82H,8-9,14,19-30,32-37,66H2,1-2H3,(H,68,83)(H,69,93)(H,70,94)(H,71,92)(H,72,91)(H,73,96)(H,74,90)(H,75,95)(H,84,85)(H,86,87)(H,88,89)(H,97,98)/t38-,39-,46+,47-,48+,49-,50+,51+,56+,57+/m1/s1
Key: QVFLVLMYXXNJDT-CSBVGUNJSA-N
Properties Molecular formula C65H90N14O19S2 Molar mass 1435.62 g mol−1 Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) Infobox references 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.
Contents
Chemistry and mechanism of action
DOTATATE 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) DOTATATE is used for tumour diagnosis in positron emission tomography (PET).[1]
Lutetium (177Lu) DOTATATE[2] has been tested for the treatment of tumors such as carcinoid and endocrine pancreatic tumor. It is presently unavailable in North America. Select medical centers in Europe offer this treatment, for instance Uppsala Centre of Excellence in Neuroendocrine Tumors and Erasmus University.[citation needed]
See also
- DOTATOC or edotreotide, a similar compound
References
- ^ 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. et al. (2011). "Peptide receptor radionuclide therapy with 177Lu-DOTATATE: The IEO phase I-II study". European Journal of Nuclear Medicine and Molecular Imaging. doi:10.1007/s00259-011-1902-1. PMID 21892623.
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