pafolacianine (Rx)

>10%

Nausea (15%)

1-10%

Vomiting (5.8%)

Abdominal pain (2.7%)

Flushing (1.7%)

Dyspepsia (1%)

Chest discomfort (1%)

Pruritus (1%)

Hypersensitivity (1%)

Contraindications

None

Cautions

Infusion-related reactions consisting of nausea, vomiting, abdominal pain, flushing, dyspepsia, hypersensitivity, elevated blood pressure, and chest discomfort reported; reactions typically occurred within 15 min after starting infusion

Errors may occur during intraoperative fluorescence imaging to detect ovarian cancer and lesions in the lung, including false negatives and false positives; nonfluorescing tissue in the surgical field does not rule out the presence of ovarian or lung cancer; fluorescence may be seen in normal tissues including bowel, kidneys, lymph nodes, and lungs as well as in inflamed tissues

Based on its mechanism of action, fetal harm may occur when administered to pregnant females

Use only D5W to dilute drug; using an incorrect diluent to prepare infusion solution can cause aggregation of pafolacianine; aggregation may induce infusion reactions, such as nausea, vomiting, abdominal pain, or rash

Drug interactions overview

• Folate, folic acid, or folate-containing supplements

  • Avoid use within 48 hr before administration
  • Use of folate, folic acid, or folate-containing supplements may reduce binding of pafolacianine to folate receptors overexpressed on ovarian cancer cells and could reduce the detection of malignant lesion

Pregnancy

Based on its mechanism of action, fetal harm may occur when administer to pregnant females

No human data are available to evaluate for drug-associated risk of major birth defects, miscarriage, or other adverse maternal fetal outcomes

Verify pregnancy status of females of reproductive potential before administration

Lactation

There are no data on the presence of pafolacianine in either human or animal 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

Fluorescent drug; targets folate receptor, which may be overexpressed in ovarian cancer

Binds to folate receptors, overexpressed in ovarian cancer and absorbs light near-infrared region, thereby serving as an adjunct to provide greater certainty during surgery of complete resection

Absorption

Peak plasma concentration: 59.1 ng/mL

AUC: 63.6 ng⋅hr/mL

Distribution

Vd: 17.1 L

Protein bound: 93.7%; no notable partitioning into red blood cells observed

Metabolism

Not metabolized by CYP enzymes

Elimination

Half-life: 0.44 hr

Plasma clearance: 28.6 L/hr

Excretion: ~35% of dose was recovered in urine (19.1%) and in feces (15.8%) after ~3-5 weeks

IV Incompatibilities

Do not use other diluents

IV Compatibilities

D5W

IV Preparation

Use aseptic technique to prepare solution

Thaw frozen vials in original carton at controlled room temperature of 20-25ºC (68-77ºF) for at least 90 min

Hand shake or vortex thawed vial for 60 seconds

Withdraw calculated drug volume; discard any unused portion in vial

Add to 250-mL D5W infusion bag; do NOT use other diluents

Gently swirl bag by hand for 1 min to mix solution

Visually inspect infusion bag; diluted solution is light-blue/green to clear in color and should not contain any visible particulate matter

Protect infusion bag from light using light-blocking cover during infusion and storage

If not immediately used, refrigerate diluted solution at 2-8ºC (36-46ºF) for up to 24 hr

Once bag removed from refrigeration, infusion must be completed within 3 hr

IV Administration

Consider administering antihistamines and/or antinausea medication for prophylaxis against infusion-related reactions

Infuse over 60 min using dedicated infusion line, 1-9 hr before surgery

Imaging

• Clinical data demonstrate that NIR imaging devices that excite at 760-785 nm and detect emission at 794-796 nm are suitable for use
• Use with an NIR imaging system cleared by the FDA for specific use with pafolacianine
• Use only by surgeons who have completed a training program on the use of NIR imaging systems for fluorescence imaging during surgery; training is provided by the device manufacturer

Storage

Unopened vials

• Freeze at -25º to -15ºC (-13ºto 5ºF)
• Store in original carton to protect from light

Diluted solution

• If not immediately used, refrigerate at 2-8°C (36-46°F) for up to 24 hr
• Once bag removed from refrigeration, complete infusion within 3 hr