Injection: Gallium Ga 68 DOTATOC Injection is a clear, colorless solution in a 30 mL multiple-dose vial containing 18.5 MBq/mL to 148 MBq/mL (0.5 mCi/mL to 4 mCi/mL) of Ga 68 DOTATOC Injection at calibration date and time.
Ga 68 DOTATOC Injection contributes to a patient’s overall long-term cumulative radiation exposure. Long-term cumulative radiation exposure is associated with an increased risk of cancer. Ensure safe handling and preparation procedures to protect patients and health care workers from unintentional radiation exposure. Advise patients to hydrate before and after administration and to void frequently after administration [see Dosage and Administration (2.1, 2.3)].
The uptake of Ga 68 DOTATOC Injection reflects the level of somatostatin receptor density in NETs, however, uptake can also be seen in a variety of other tumors that also express somatostatin receptors. Increased uptake might also be seen in other non-cancerous pathologic conditions that express somatostatin receptors including thyroid disease or in subacute inflammation, or might occur as a normal physiologic variant (e.g. uncinate process of the pancreas) [see Dosage and Administration (2.5)].
A negative scan after the administration of Ga 68 DOTATOC Injection in patients who do not have a history of NET disease does not rule out disease [see Clinical Studies (14)].
Clinical Trial Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The safety of Ga-68 DOTATOC injection was evaluated in 334 patients in clinical trials of patients receiving a single dose of Ga-68 DOTATOC injection for imaging known or suspected NET.
The following adverse reactions occurred at a rate of < 2%:
Gastrointestinal Disorders: nausea
The following adverse reactions occurred at a rate of a < 1%
Skin and Subcutaneous Tissue Disorders: pruritusVascular Disorders: flushing
Non-radioactive somatostatin analogs bind to the same somatostatin receptors as Ga 68 DOTATOC Injection. Image patients with Ga 68 DOTATOC Injection just prior to dosing with long-acting analogs of somatostatin. Short-acting analogs of somatostatin can be used up to 24 hours before imaging with Ga 68 DOTATOC Injection [see Dosage and Administration (2.3)].
There are no available data on the use of Ga 68 DOTATOC Injection in pregnant women to identify a risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. Animal reproduction studies have not been conducted with Ga 68 DOTATOC. However, all radiopharmaceuticals, including Ga 68 DOTATOC Injection have the potential to cause fetal harm depending on the fetal stage of development and the magnitude of the radiation dose. If considering Ga 68 DOTATOC Injection administration to a pregnant woman, inform the patient of the potential for adverse pregnancy outcomes based on the radiation dose from Ga 68 DOTATOC Injection and the gestational timing of exposure.
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S general population, the estimated background risks of major birth defects and miscarriage in clinically recognized pregnancies are 2-4% and 15-20%, respectively.
There is no information on the presence of Ga 68 DOTATOC in human milk, the effect on the breastfed infant, or the effect on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for Ga 68 DOTATOC Injection and any potential adverse effects on the breastfed child from Ga 68 DOTATOC Injection or from the underlying maternal condition.
To decrease exposure to the breastfed infant, advise a lactating woman to interrupt breastfeeding and pump and discard breast milk for 8 hours after Ga 68 DOTATOC Injection administration.
The safety and efficacy of Ga 68 DOTATOC Injection have been established in pediatric patients with neuroendocrine tumors. Efficacy is based on data from 14 patients in Study A and B demonstrating the ability of Ga 68 DOTATOC to image NETs [see Clinical Studies (14)]. The safety profile of Ga 68 DOTATOC Injection is similar in adult and pediatric patients with somatostatin receptor positive tumors. The recommended Ga 68 DOTATOC injected dose in pediatric patients is weight based [see Dosage and Administration (2.2)].
Clinical studies of Ga 68 DOTATOC did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
In the event of a radiation overdose, reduce the absorbed dose to the patient by increasing the elimination of the radionuclide from the body by reinforced hydration, frequent bladder voiding, and diuretics, if needed. If possible, perform an estimate of the radioactive dose given to the patient.
Ga 68 DOTATOC Injection is a radioactive diagnostic agent for intravenous administration. It contains 3.6 mcg/mL (DOTA-0-Phe1-Tyr3) octreotide, 18.5 MBq/mL to 148 MBq/mL (0.5 mCi to 4 mCi/mL) of Ga 68 DOTATOC at calibration time, and ethanol (10% v/v) in sodium chloride (9 mg/mL) solution (approximately 14 mL volume). Ga 68 DOTATOC Injection is a sterile, pyrogen free, clear, colorless, buffered solution, with a pH between 4 to 8.
Ga 68 DOTATOC, also known as Gallium-68 (DOTA0-Phe1-Tyr3) octreotide, is a cyclic 8 amino acid peptide with a covalently bound chelator (DOTA). The peptide has the amino acid sequence: H-D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Cys-Thr-OH, and contains one disulfide bond. Ga 68 DOTATOC has a molecular weight of 1489.65 g/mol and its chemical structure is shown in Figure 1.
Figure 1: Chemical Structure of Ga 68 DOTATOC
Gallium-68 labeled 2-[4-[2-[[(2R)-1-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-4-[[(2R,3R)-1,3-dihydroxybutan-2-yl]carbamoyl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]-7,10-bis(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid.
Table 3 and Table 4 display the principal radiation emission data and physical decay of Ga 68.
Gallium-68 (Ga 68) decays with a half-life of 68 minutes to stable Zn 68:
- 89% through positron emission with a mean energy of 836 keV followed by emission of two 511 keV annihilation photons (178%),
- 10% through orbital electron capture (with associated X-ray or Auger emissions), and
- 3% through 13 gamma transitions from 5 excited levels of the daughter Zn 68 nucleus. The most probable prompt gamma emission is a 1088 keV gamma with a 3.2% per decay probability.
|Radiation/Emission||% Disintegration||Mean Energy (MeV)|
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