copper CU 64 dotatate (Rx)

1-10%

Nausea (<2%)

Vomiting (<2%)

Flushing (<2%)

Postmarketing reports

Immune system disorders: Hypersensitivity reactions, predominantly rash, pruritus, less frequently angioedema or features of anaphylaxis

Contraindications

None

Cautions

Hypersensitivity reactions consisting of cutaneous reactions such as rash and pruritus reported; reactions reversed either spontaneously or with routine symptomatic management; less frequently hypersensitivity reactions included angioedema or cases with features of anaphylaxis

Radiation risk

• Contributes to a patient’s overall long-term cumulative radiation exposure; long-term cumulative radiation exposure associated with increased cancer risk
• Ensure safe handling and preparation procedures to protect patients and healthcare workers from unintentional radiation exposure

Risk for image misinterpretation

• Uptake of copper CU 64 dotatate reflects somatostatin receptor density in NETs
• Uptake can also be seen in a variety of other tumor types that express somatostatin receptors (eg, thyroid disease) or in subacute inflammation, or a normal physiologic variant (eg, uncinate process of the pancreas)
• Uptake may need to be confirmed by histopathology or other assessments to confirm NET diagnosis

Drug interaction overview

• Nonradioactive somatostatin analogs competitively bind to the same somatostatin receptors as copper CU 64 dotatate
• Long-acting somatostatin analogs: 28-day washout period recommended before imaging
• Short-acting somatostatin analogs: 2-day washout period recommended before imaging

Pregnancy

There are no studies in pregnant females to inform any drug-associated risks; however, all radiopharmaceuticals have the potential to cause fetal harm

Assess pregnancy status in females of reproductive potential before administering

Lactation

There is no information on the presence of copper CU 64 dotatate in human milk, the effect on the breastfed infant, or the effect on milk production

Advise breastfeeding females to interrupt breastfeeding and pump and discard breast milk for 12 hr after administration to minimize radiation exposure to a breastfed infant

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Copper Cu 64 dotatate binds to somatostatin receptors with highest affinity for subtype 2 receptors (SSTR2); dotatate, also known as DOTA-0-Tyr3-octreotate, is a cyclic 8-amino acid peptide with a covalently bound chelator (dota)

It binds to cells that express somatostatin receptors, including malignant cells, which overexpress SSTR2 receptors

Copper CU 64 is a positron beta-emitting radionuclide with an emission yield that allows PET imaging

Distribution

After 1-3 hr following single dose, maximum radioactivity observed in in SSTR2-expressing organs (eg, adrenal glands, kidneys, pituitary glands, spleen, liver)

Metabolism

Unknown

Elimination

Excretion: 16-40% recovered in urine over 6 hours after injection

IV Preparation

See full prescribing information for drug preparation using a lead glass shield for radioprotection purposes

Drug handling

• Use waterproof gloves, effective radiation shielding, and appropriate safety measures when preparing and handling
• Radiopharmaceuticals should be used by or under the control of physicians and nuclear pharmacists who are qualified by specific training and experience in the safe use and handling of radionuclides, and whose experience and training have been approved by the appropriate governmental agency authorized to license the use/preparation of radionuclides
• Inspect visually for particulate matter and discoloration before administration; do not use if solution contains particulate matter or is discolored; copper CU 64 dotatate is a clear, colorless- to-yellow solution
• Calculate necessary volume to administer based on measured activity, volume, calibration time, and date
• Use dose calibrator to measure dose immediately before administration

Patient preparation

• Instruct patients to drink a sufficient amount of water to ensure adequate hydration prior to administration

IV Administration

Administer as IV bolus over ~1 minute; flush IV with 0.9% NaCl

Use within 2 hr after calibration time

Dispose of any unused drug in a safe manner in compliance with applicable regulations

Patients must drink and void frequently during the first hours following administration to reduce radiation exposure

Image patients just prior to dosing with somatostatin analogs (also see warnings for washout period)

A negative scan after administration in patients without history of NET disease does not rule out disease

Image acquisition

• A whole-body acquisition from the skull vertex to mid thigh recommended
• Image acquisition can begin 45-90 minutes after IV bolus
• Adapt copper CU 64 dotatate uptake time and scan duration according to the equipment used and the patient and tumor characteristics, to obtain the optimal image quality

Storage

Store in upright position within lead shielding to protect handlers from exposure to radiation

Store at controlled room temperature 20-25ºC (68-77ºF)

Do not use and discard 2 hr after calibration date and time