Gallium 68 Dotatate
Gallium 68 Dotatate Uses, Dosage, Side Effects, Food Interaction and all others data.
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.
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.
| Trade Name | Gallium 68 Dotatate |
| Generic | Dotatate gallium Ga-68 |
| Dotatate gallium Ga-68 Other Names | (68Ga)Gallium dotatate, 68Ga-DOTATATE, 68Ga-DOTATOC, Dotatate gallium Ga-68, Ga 68 DOTATOC, Gallium (68Ga) DOTA-tate, Gallium (68Ga) dotatate, Gallium (Ga 68) dotatate, Gallium 68 dotatate, Gallium dotatate, Ga-68, Gatate |
| Type | |
| Formula | C65H87GaN14O19S2 |
| Weight | Average: 1500.54 Monoisotopic: 1499.499317482 |
| Protein binding | It presents binding to plasma proteins. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
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.
Gallium 68 Dotatate is also used to associated treatment for these conditions: Neuroendocrine Tumors
How Gallium 68 Dotatate works
The somatostatin receptor-based imaging is the preferred choice in the diagnostic and management of neuroendocrine tumors. The basis for the mechanism of dotatate gallium 68 is the binding of a ligand analog that is radiolabeled, in this case thye preferred binding site is the receptors of the subtype 2. The malignant cells are reported to overexpress the somatostatin subtype 2 receptor. Dotatate gallium 68 is a β+ emiting radionuclide with an emission yield that can be detected by the positron emission tomography and thus the seletive binding to the overexpressed somatostatin receptor will be detected.
Toxicity
Studies on dotatate gallium 68 have not been studied but the comparative studies to other non-radioactivity compounds showed no mutation.
Volume of Distribution
The volume of distribution is registered in a range from 0.25-0.65 ml/cm3.
Elimination Route
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.
Half Life
The half-life of gallium 68 is estimated to be of 68 min.
Clearance
The pharmacokinetics of dotatate gallium 68 is matched to the short half-life of the isotope gallium 68 thus, this pharmaceutical presents a very fast blood clearance.
Elimination Route
In the first four hours after the intravenous administration of dotatate gallium 68 there is an elimination of about 12% of the injected dose by the urine.
Innovators Monograph
You find simplified version here Gallium 68 Dotatate
