Note: Discontinue folate, folic acid, or folate-containing supplements 48 hours prior to pafolacianine administration. Consider administering an antihistamine and/or antiemetics as prophylaxis for infusion-related reactions.
Optical imaging agent, ovarian cancer: IV: 0.025 mg/kg as a single dose, administered 1 to 9 hours prior to surgery. Use with a near-infrared (NIR) imaging device cleared for specific use with pafolacianine; clinical data demonstrates that NIR imaging devices that excite at 760 to 785 nm and detect emission at 794 to 796 nm are suitable for use with pafolacianine.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl ≥30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling; however, mild or moderate renal impairment had no clinically significant effect on pafolacianine pharmacokinetics.
CrCl <30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Mild or moderate impairment (total bilirubin <3 times ULN and AST > ULN): There are no dosage adjustments provided in the manufacturer's labeling; however, mild or moderate hepatic impairment had no clinically significant effect on pafolacianine pharmacokinetics.
Severe impairment (total bilirubin >3 times ULN and any AST): There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Refer to adult dosing.
Infusion reaction: Interrupt infusion and manage with antihistamines and/or antiemetic agents as clinically indicated; may resume infusion after treatment of reaction.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution, Intravenous:
Cytalux: 3.2 mg/1.6 mL [2 mg/mL] (10s)
IV: Infuse over 60 minutes, 1 to 9 hours prior to surgery. Administer via a dedicated infusion line. Protect infusion bag from light during infusion using a light-blocking cover.
Consider administering an antihistamine and/or antiemetic medications as prophylaxis for infusion-related reactions. Monitor for signs/symptoms of infusion-related reactions.
Optical imaging agent (ovarian cancer): As an adjunct for intraoperative identification of malignant lesions in adult patients with ovarian cancer.
Infusion related reaction consisting of nausea, vomiting, abdominal pain, flushing, dyspepsia, chest discomfort, and pruritus may frequently occur with pafolacianine.
Onset: Rapid; typically occurs within 15 minutes of infusion initiation.
Risk factors:
• Incorrect diluent to prepare infusion (only D5W should be used when diluting pafolacianine for infusion; the use of other solutions may result in pafolacianine aggregation, which may be associated with infusion reactions)
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.
>10%: Gastrointestinal: Nausea (15%)
1% to 10%:
Cardiovascular: Chest discomfort (1%), flushing (2%)
Dermatologic: Pruritus (1%)
Gastrointestinal: Abdominal pain (3%), dyspepsia (1%), vomiting (6%)
Hypersensitivity: Hypersensitivity reaction (1%)
Frequency not defined: Miscellaneous: Infusion related reaction
There are no contraindications listed in the manufacturer's labeling.
Other warnings/precautions:
• Imaging interpretation risk: Interpretation errors may occur during intraoperative fluorescence imaging with pafolacianine to detect ovarian cancer, including false negatives and false positives. Nonfluorescing tissue in the surgical field does not rule out the presence of ovarian cancer. Fluorescence may be seen in noncancerous tissue including areas of the bowel, kidneys, lymph nodes, and inflamed tissue.
Substrate of OAT1/3, OATP1B1/1B3 (SLCO1B1/1B3)
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Folic Acid: May diminish the diagnostic effect of Pafolacianine. Risk X: Avoid combination
Folic acid may reduce binding of pafolacianine to folate receptors on ovarian cancer cells and may interfere with the detection of cancer tissue when using pafolacianine. Management: Discontinue folate, folic acid, or folate-containing supplements 48 hours prior to pafolacianine administration.
Verify pregnancy status prior to therapy; pregnancy must be excluded prior to use in patients who may become pregnant.
Based on the mechanism of action, in utero exposure to pafolacianine may cause fetal harm.
It is not known if pafolacianine is present in breast milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.
Verify pregnancy status prior to therapy (in patients who could become pregnant). Monitor for signs/symptoms of infusion-related reactions.
Pafolacianine is a folate analog conjugated to a near-infrared (NIR) fluorescent dye (Hoogstins 2016). Pafolacianine is an imaging agent that targets folate receptor (FR), which may be overexpressed in ovarian cancer; it binds to FR-expressing cancer cells, internalizes via receptor mediated endocytosis, and concentrates in FR-positive cancer tissues. Pafolacianine assists optical imaging during surgery by absorbing light in the NIR region and emitting fluorescence.
Distribution: Vd: 17.1 ± 5.99 L; distributes into tissues.
Protein binding: 93.7%.
Half-life elimination: 0.44 ± 0.23 hours.
Excretion: Urine (~19%); feces (~16%).
Clearance: Plasma: 28.6 ± 4.97 L/hour.
