PACKAGING - PRINCIPAL DISPLAY PANEL

10 Vial Carton

NDC 81052-138-10

cytalux™
(pafolacianine) injection

3.2 mg / 1.6 mL (2 mg/mL)

10 x 1.6 mL Single-Dose Vials. Discard Unused Portion
For Intravenous Infusion After Dilution

Store vials in original carton to protect from light. Store frozen at
-25° to -15°C (-13° to 5°F) until expiration date. Once thawed, vials

may be stored refrigerated at 2° to 8°C (36° to 46°F) up to 30 days

or at room temperature at 20° to 25°C (68° to 77°F) up to 24 hours.

Rx only

ON TARGET LABORATORIES

Single Vial Carton Label

NDC 81052-138-01

cytalux™
(pafolacianine) injection

3.2 mg / 1.6 mL
(2 mg/mL)

For Intravenous Infusion After Dilution

Store vials in original carton to
protect from light.Store frozen at
** -25° to -15°C (-13° to 5°F) until**
** expiration date.**Once thawed, vials
may be stored refrigerated at 2° to 8°C
(36° to 46°F) up to 30 days or at room
temperature at 20° to 25°C (68° to
77°F) up to 24 hours.

Rx only

ON TARGET LABORATORIES 

Vial Label

NDC 81052-138-10

Sterile

cytalux™
(pafolacianine) injection

3.2 mg / 1.6 mL
(2 mg/mL)

For Intravenous Infusion After Dilution

Discard Unused Portion

Single-Dose Vial

Rx only

ON TARGET LABORATORIES

14372

LOT:
EXP: YYYY/MM

17 PATIENT COUNSELING INFORMATION

Embryo-Fetal Toxicity
Advise females of reproductive potential of the potential risk to a fetus and to contact their healthcare
provider with a known or suspected pregnancy
[ see Warnings and Precautions ( 5.3) and Use In Specific Populations ( 8.1) ].

Folate Supplements Usage
Inform patients that folic acid may reduce the detection of cancer tissue with CYTALUX. Advise the
patient to stop taking folate, folic acid, or folate-containing supplements 48 hours before
administration of CYTALUX [ see Dosage and Administration ( 2.1) and Drug Interactions ( 7) ].

RECENT MAJOR CHANGES

Dosage and Administration, 7/2025

Preparation and Storage Instructions ( 2.3)

FULL PRESCRIBING INFORMATION: CONTENTS*

RECENT MAJOR CHANGES

1. INDICATIONS AND USAGE

2 DOSAGE AND ADMINISTRATION

2.1 Recommended Testing, Evaluations and Premedications Prior to

Administration of
CYTALUX

2.2 Recommended Dosage and Administration

2.3 Preparation and Storage Instructions

2.4 Management of Infusion-Related Reactions

2.5 Imaging

3 DOSAGE FORMS AND STRENGTHS

4 CONTRAINDICATIONS

5 WARNINGS AND PRECAUTIONS

5.1 Infusion-Related Reactions

5.2 Risk of Misinterpretation

5.3 Embryo-Fetal Toxicity

5.4 Risk of Pafolacianine Aggregation and Infusion Reactions

6 ADVERSE REACTIONS

6.1 Clinical Trials Experience

7 DRUG INTERACTIONS

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

8.2 Lactation

8.3 Females and Males of Reproductive Potential

8.4 Pediatric Use

8.5 Geriatric Use

11 DESCRIPTION

12 CLINICAL PHARMACOLOGY

12.1 Mechanism of Action

12.2 Pharmacodynamics

12.3 Pharmacokinetics

13 NONCLINICAL TOXICOLOGY

13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

14 CLINICAL STUDIES

14.1 Patients with Known or Suspected Ovarian Cancer

14.2 Patients with Known or Suspected Cancer in the Lung

16 HOW SUPPLIED/STORAGE AND HANDLING

10 Vial Carton

Single Vial Carton Label

Vial Label

• Sections or subsections omitted from the full prescribing information are not listed.

2 DOSAGE AND ADMINISTRATION

2.1 Recommended Testing, Evaluations and Premedications Prior to

Administration of
CYTALUX

Obtain a pregnancy test in females of reproductive potential and verify the absence of pregnancy
prior to administration of CYTALUX [ see Warnings and Precautions (5.3) and Use in Specific Populations ( 8.1, 8.3) ].
Discontinue folate, folic acid, or folate containing supplements 48 hours before administration of
CYTALUX [ see Drug Interactions (7)].
Consider administering antihistamines and/or anti-nausea medication for prophylaxis against infusion related
reactions [ see Warnings and Precautions (5.1)].

2.2 Recommended Dosage and Administration

Adult Patients with Ovarian Cancer

The recommended dose of CYTALUX is a single intravenous infusion of 0.025 mg/kg diluted in 250 mL of 5% Dextrose Injection, administered over 60 minutes using a dedicated infusion line, 1 hour to 9 hours prior to surgery.

Adult Patients with Known or Suspected Cancer in the Lung

The recommended dose of CYTALUX is a single intravenous infusion of 0.025 mg/kg diluted in 250 mL of 5% Dextrose Injection, administered over 60 minutes using a dedicated infusion line, 1 hour to 24 hours prior to surgery.

2.3 Preparation and Storage Instructions

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.

1. Use aseptic technique for the preparation of CYTALUX infusion solution.

2. Only use 5% Dextrose Injection for dilution. Do not use other diluents due to incompatibility [see Warnings and Precautions ( 5.4)] .

3. CYTALUX vials should be stored and thawed in the original carton protected from light.

1. Remove carton containing one single vial of CYTALUX from freezer and record the date, time and thawing condition on the carton.
2. Thaw at room temperature between 20°C to 25°C (68°F to 77°F) for at least 60 minutes or under refrigerated conditions between 2°C to 8°C (36°F to 46°F) for at least 6 hours. When thawed under refrigerated conditions, allow the vial to stand at room temperature for 15 minutes before dilution.
3. Once thawed, an individual CYTALUX vial may be stored at room temperature between 20°C to 25°C (68°F to 77°F) for a maximum single period of 24 hours or under refrigerated conditions between 2°C to 8°C (36°F to 46°F) for a maximum single period of up to 30 days, prior to preparation for infusion.
4. If CYTALUX vial is not used within the maximum single period at either room temperature or under refrigerated conditions, the vial may be refrozen up to three times.
5. If the vial has been thawed after the third refreeze, it must be used. If not used after the third refreeze, do not use and discard the vial.
6. Each vial of CYTALUX may be penetrated only once at the time of preparation of infusion solution. Once penetrated, the vial may not be refrozen.

4. Hand shake or vortex the thawed CYTALUX vial for 60 seconds.

5. Withdraw the calculated volume of CYTALUX for a dose of 0.025 mg/kg. Discard any unused portion in the vial.

6. Add into a 250 mL of 5% Dextrose Injection, USP bag.

7. Gently swirl the bag by hand for 1 minute to mix the solution.

8. Visually inspect the infusion bag. The solution should be light blue/green to clear in color and should not contain any visible particulate matter.

9. Protect the infusion bag from light using a light-blocking cover during infusion and storage.

10. If not immediately used, store the diluted CYTALUX infusion solution in a refrigerator at 2°C to 8°C (36°F to 46°F) for not more than 24 hours. Once the bag is removed from refrigeration, infusion must be completed within 3 hours.

2.4 Management of Infusion-Related Reactions

If the patient develops an infusion reaction during administration, interrupt the infusion and treat with
antihistamines and/or anti-nausea medication as necessary, based on clinical decision. Complete the
infusion within 3 hours of the start of the initial administration [ see Warnings and Precautions (5.1)].

2.5 Imaging

• Clinical data demonstrate that near infrared (NIR) imaging devices that excite at 760 nm to 785 nm and detect emission at 790 nm to 815 nm are suitable for use with CYTALUX.
• CYTALUX is to be used with an NIR imaging system cleared by the FDA for specific use with pafolacianine.
• CYTALUX should only be used 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.

11 DESCRIPTION

CYTALUX contains pafolacianine, an optical imaging agent, as a tetrasodium salt referred to as
pafolacianine sodium. Chemically, pafolacianine sodium is (S)-2-(4-(((2-amino-4-oxo-3,4-
dihydropteridin-6-yl)methyl)amino)benzamido)-3-(4-(((E)-2-((E)-2-(3,3-dimethyl-5-sulfonato-1-(4-
sulfonatobutyl)-3H-indol-1-ium-2-yl)vinyl)-6-((E)-2-(3,3-dimethyl-5-sulfonato-1-(4-
sulfonatobutyl)indolin-2-ylidene)ethylidene)cyclohex-1-en-1-yl)oxy)phenyl)propanoate hydrate
tetrasodium. Pafolacianine sodium has a molecular formula of C 61H 63N 9Na 4O 17S 4, a molecular mass
of 1414.42 g/mol and has the following structure:

CYTALUX (pafolacianine) injection is a sterile, non-pyrogenic, dark bluish green, clear aqueous
solution for intravenous use. Each vial contains 3.2 mg (2 mg/mL) pafolacianine (equivalent to 3.4 mg
pafolacianine sodium),14.4 mg sodium chloride, 0.23 mg potassium phosphate monobasic, 1.27 mg
sodium phosphate dibasic heptahydrate in 1.6 mL volume. The pH is adjusted with sodium hydroxide
and/or hydrochloric acid and is between 7.1 to 7.8.

12 CLINICAL PHARMACOLOGY

12.1 Mechanism of Action

Pafolacianine binds to alpha and beta folate receptors (FR) on cells, is internalized via receptor-mediated endocytosis, and accumulates intracellularly.

Pafolacianine enhances lesion visualization through the differential level of expression and accessibility of folate receptors within lesions relative to normal tissue.

Pafolacianine absorbs light in the near-infrared (NIR) region within a range of 760 nm to 785 nm with peak absorption of 776 nm and emits fluorescence within a range of 790 nm to 815 nm with peak emission of 796 nm.

12.2 Pharmacodynamics

Tumor to background ratios of fluorescence intensity changed with different mass doses studied in patients with ovarian cancer. High tumor to background ratio was observed with 0.025 mg/kg dose. CYTALUX exposure-response relationships and the time course of pharmacodynamic responses are unknown.

12.3 Pharmacokinetics

The mean C max of pafolacianine was 59.1 ± 5.94 ng/mL and AUC inf was 63.6 ± 12.6 ng.hr/mL.
Distribution
The mean volume of distribution (V z) is 17.1 ± 5.99 L, indicating distribution into tissues.
Plasma protein binding of pafolacianine is 93.7%. No notable partitioning into red blood cells has
been observed.
Elimination
The elimination half-life of pafolacianine is 0.44 ± 0.23 hours and mean plasma clearance is 28.6 ±
4.97 L/hr.
Metabolism
Pafolacianine sodium is not metabolized by cytochrome P450 (CYP) enzymes.
Excretion
Following a single IV infusion of radiolabeled pafolacianine sodium, approximately 35% of the dose
was recovered in urine (19.1%) and in feces (15.8%) after approximately 3-5 weeks.
Specific Populations
No clinically significant differences in pharmacokinetics of pafolacianine were identified based on age
18 to 89 years, weight 41.6 to 133.6 kg, mild to moderate renal impairment (CLcr 30 to 89 mL/min),
mild to moderate hepatic impairment (total bilirubin < 3 ULN and AST > ULN). The effect of severe
renal impairment (CLcr < 30 mL/min) and severe hepatic impairment (total bilirubin > 3 ULN and any
AST value) on the pharmacokinetics of pafolacianine have not been studied.
Drug Interaction Studies
No clinical studies evaluating the drug interaction potential of pafolacianine have been conducted.
In Vitro Studies
CYP Enzymes: Pafolacianine is not an inhibitor of CYPs 1A2, 2B6, 2C8, 2C9, 2C19 2D6, 3A4/5.
UDP-glucuronosyltransferase (UGT) Enzymes: Pafolacianine is not an inhibitor of UGT1A1.
Transporter Systems: Pafolacianine is a substrate for OATP1B1, OATP1B3, and OAT1. Pafolacianine
is not an inhibitor of OATP1B1, OATP1B3, OAT1, OAT3, OCT2, MATE1, MATE2-K, P-gp, or BCRP

16 HOW SUPPLIED/STORAGE AND HANDLING

How Supplied
CYTALUX (pafolacianine) injection, 3.2 mg /1.6 mL (2 mg/mL), is a dark bluish green, clear aqueous
solution packaged in a sealed amber glass single-dose vial. It is supplied in a carton containing 10
vials (NDC 81052-138-10) individually packaged.

Storage and Handling
Store vials in their original cartons to protect from light.

CYTALUX may be stored according to the table below. If CYTALUX vial is not used within the maximum single period at either room temperature or under refrigerated conditions the vial may be refrozen up to three time.​

Storage Condition​	Condition Temperature Range​	Maximum Single Period	Permissible Freeze-Thaw Cycles​
Frozen	-25°C to -15°C (-13°F to 5°F)	Until Expiration Date	Not applicable
Refrigeration	2°C to 8°C (36°F to 46°F)	Up to 30 days	Three
Room Temperature	20°C to 25°C (68°F to 77°F)	Up to 24 hours	Three

Do not use the product past the expiration date

Manufactured by:

Grand River Aseptic Manufacturing

140 Front Ave SW

Grand Rapids, MI 49504

Manufactured for:

On Target Laboratories

1281 Win Hentschel Blvd

West Lafayette, IN 47906