piflufolastat F 18 (Rx)

1-10%

Headache (2%)

Dysgeusia (2%)

Fatigue (1%)

<1%

Hypersensitivity (0.2%)

Contraindications

None

Cautions

Monitor for hypersensitivity reactions, particularly in patients with a history of allergy to other drugs and foods; reactions may not be immediate; trained staff and resuscitation equipment should always be available

Risk of image misinterpretation

• Imaging interpretation errors can occur
• A negative image does not rule out presence of prostate cancer and a positive one does not confirm presence of prostate cancer
• Drug uptake is not specific for prostate cancer and may occur with other types of cancer, nonmalignant processes, and in normal tissues
• Clinical correlation, which may include histopathological evaluation of suspected prostate cancer site, is recommended

Radiation risks

• Diagnostic radiopharmaceuticals expose patients to radiation
• Radiation exposure is associated with a dose-dependent increased risk of cancer
• Ensure safe drug handling and patient preparation procedures to protect patients and healthcare providers from unintentional radiation exposure

Drug interaction overview

• Androgen-deprivation therapy (ADT) and other therapies targeting the androgen pathway

  • ADT and other therapies targeting the androgen pathway (eg, androgen receptor antagonists) may result in changes in uptake of piflufolastat F18 in prostate cancer
  • Effect of these therapies on performance has not been established

Pregnancy

Not indicated for use in females

There is no information on the risk of adverse developmental outcomes in pregnant females or animals

All radiopharmaceuticals, including piflufolastat F18, may potentially cause fetal harm depending on fetal stage of development and magnitude of radiation dose

Lactation

Not indicated for use in females

There is no information on drug presence in human milk, effects on breastfed infants, or effects on milk production

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

Radiolabeled PSMA inhibitor imaging agent

Binds to cells that express PSMA, including malignant prostate cancer cells

Fluorine-18 (F18) is a beta-positive–emitting radionuclide that enables PET

Distribution

Distributes to kidneys (16.5% of administered activity), liver (9.3%), and lung (2.9%), within 60 minutes of IV administration

Distribution half-life: 0.17 hr

Elimination

Half-life: 3.47 hr

Excretion: Urine (~50% [first 8 hr post dose])

IV Preparation

Use aseptic technique and radiation shielding when withdrawing and administering

Visually inspect solution; do not use if it contains particulate matter or is cloudy or discolored; solution is clear and colorless

Calculate the necessary volume to administer based on calibration time and required dose; piflufolastat F18 may be diluted with 0.9% NaCl

Assay dose in a suitable dose calibrator before administration

Radiation safety

• Piflufolastat F18 is a radioactive drug; only authorized persons qualified by training and experience should receive, use, or administer
• Handle with appropriate safety measures to minimize radiation exposure during administration
• Use waterproof gloves and effective radiation shielding, including syringe shields, when preparing and handling

Patient preparation

• Instruct patients to drink water to ensure adequate hydration before administration and continue drinking and voiding frequently during the first few hours following administration to reduce radiation exposure

IV Administration

Administer IV over 1-2 minutes

Follow injection with IV flush of 0.9% NaCl

Dispose of any unused drug in compliance with radiopharmaceutical regulations

Image acquisition

Start 60 minutes after administration

Starting image acquisition >90 minutes after injection may affect imagining performance

Advise patients to void immediately before image acquisition

Position patient supine with arms above head

Start image acquisition from mid thigh and proceed to skull vertex

Scan duration: 12-40 minutes depending on number of bed positions (typically 6-8) and acquisition time per bed position (typically 2-5 minutes)

Storage

Unopened vials

• Store at 20-25ºC (68-77ºF)
• Store upright in original container with radiation shielding
• Expiration date and time are provided on container label
• Use within 10 hr from the time of the end of synthesis