Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 2mg/mL (3.2mg/1.6mL single-dose vial); equivalent to 3.4 mg/1.6 mL pafolacianine sodium
Ovarian Cancer Imaging
Indicated as an adjunct for intraoperative identification of ovarian cancer malignant lesions
0.025 mg/kg IV x 1 dose; administer 1-9 hr before surgery
Lung Lesion Imaging
Indicated as an adjunct for intraoperative identification of malignant and non-malignant pulmonary lesions in adults with known or suspected lung cancer
0.025 mg/kg IV x 1 dose; administer 1-24 hr before surgery
Dosage Modifications
Infusion-related reactions
- If infusion reaction develops, interrupt infusion and treat with antihistamines and/or antinausea medication as necessary, based on clinical decision
- Complete infusion within 3 hr of the start of initial administration
Renal impairment
- Mild-to-moderate (CrCl 30-89 mL/min): No dosage adjustment necessary
- Severe (CrCl <30 mL/min): Not studied
Hepatic impairment
- Mild-to-moderate (total bilirubin <3x ULN and AST > ULN): No dosage adjustment necessary
- Severe (total bilirubin >3x ULN and any AST): Not studied
Dosing Considerations
Consider administering antihistamines and/or antinausea medication for prophylaxis against infusion-related reactions
Before administration
- Verify pregnancy status in females of reproductive potential
- Discontinue folate, folic acid, or folate-containing supplements 48 hr before administration
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (0)
Serious - Use Alternative (2)
- folic acid
folic acid decreases effects of pafolacianine by receptor binding competition. Avoid or Use Alternate Drug. Avoid coadministration with folic acid or folic acid-containing supplements for 48 hr before administering pafolacianine. 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 lesions with. .
- iron/folic acid/vitamin/mineral
iron/folic acid/vitamin/mineral decreases effects of pafolacianine by receptor binding competition. Avoid or Use Alternate Drug. Avoid coadministration with folic acid or folic acid-containing supplements for 48 hr before administering pafolacianine. 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 lesions with. .
Monitor Closely (0)
Minor (0)
Adverse Effects
>10%
Nausea (15%)
1-10%
Vomiting (5.8%)
Abdominal pain (2.7%)
Flushing (1.7%)
Dyspepsia (1%)
Chest discomfort (1%)
Pruritus (1%)
Hypersensitivity (1%)
Warnings
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 & Lactation
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.Pharmacology
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
Administration
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
Images
Formulary
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