Gallate(1-)-68Ga, [N-[[4,7,10-tris[(carboxy-κO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN1,κN4,κN7,κN10]acetyl-κO]-D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-threonyl-L-cysteinyl-L-threonine cyclic (2→7)-disulfidato(4-)]-, hydrogen (1:1)

CAS NO.：1027785-90-5
Empirical Formula: C65H86GaN14O19S2.H
Molecular Weight: 1500.53
Update Date: 2023-05-09 09:30:54

What is Gallate(1-)-68Ga, [N-[[4,7,10-tris[(carboxy-κO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN1,κN4,κN7,κN10]acetyl-κO]-D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-threonyl-L-cysteinyl-L-threonine cyclic (2→7)-disulfidato(4-)]-, hydrogen (1:1)?

Absorption

Dotatate gallium 68 presents a higher affinity for the somatostatin receptor subtype 2 when compared with the other gallium 68 analogues. Intravenous administration of dotatate gallium 68 is absorbed and distributed to all the somatostatin subtype 2 receptor-containing organs like pituitary, thyroid, spleen, adrenals, kidney, pancreas, prostate, liver and salivary glands. There is no uptake in cerebral cortex or in the heart and the uptake presented in thymus and lung are very low.

Toxicity

Studies on dotatate gallium 68 have not been studied but the comparative studies to other non-radioactivity compounds showed no mutation.

Background

Dotatate gallium (Ga-68) is a somatostatin-2 receptor analog which is radiolabeled with gallium 68 as a positron-emitting radioisotope. Ga-68 dotatate has a high affinity for somatostatin-2 receptor and it is rapidly excreted from the nontarget sites which gives it an ideal candidate for imaging neuroendocrine tumors. Dotatate gallium (Ga-68) explotes its ability to detect somatostatin receptor scintigraphy and this characteristic tends to change with tumor grade which gives Ga-68 dotate a high diagnostic value. Dotatate gallium 68 was developed by Advanced Accelerator Applications USA, Inc. and FDA approved in June 1, 2016.

Indications

Dotatate gallium 68 is one of the most prominent radiopharmaceuticals used in imaging with positron emission tomography. It binds to the somatostatin-2 receptor which is usually overexpressed in many neuroendocrine tumors in both adult and pediatric patients. The neuroendocrine tumors are bening or malignant tumors produced in the hormone producing cells of the neuroendocrine system.

Pharmacokinetics

The overexpression of somatostatin receptor in tumor tissue has been widely studied and the usage of scintigraphy for the diagnostic of neuroendocrine tumors has been happening since the beggining of the 90s. The development of positron-emission tomography there has been an emerging and growing field for the discovery of tracer labeled somatostatin analogues like dotatate gallium 68. Even after all the reportes, the pharmacodynamic profile of dotatate gallium 68 has not been studied.

Metabolism

Not Available

Safety information for Gallate(1-)-68Ga, [N-[[4,7,10-tris[(carboxy-κO)methyl]-1,4,7,10-tetraazacyclododec-1-yl-κN1,κN4,κN7,κN10]acetyl-κO]-D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-threonyl-L-cysteinyl-L-threonine cyclic (2→7)-disulfidato(4-)]-, hydrogen (1:1)

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