Cytalux Pafolacianine injection 3.2 mg/1.6mL Injection
🆔 Identity & classification
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🏭 Manufacturer & labeler
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🩺 Clinical
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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UNII QTT17582CB
A strong acid used to adjust and maintain the proper pH level in liquid medicines, ensuring stability and preventing breakdown of active ingredients.
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UNII 4J9FJ0HL51
Potassium phosphate, monobasic is a salt compound used in medicines as a pH buffer and electrolyte source. It helps stabilize the acidity level of liquid and powdered formulations.
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UNII 451W47IQ8X
Sodium chloride is common table salt. It's used in medicines as a buffer to maintain proper pH, as a filler to add bulk, or to adjust the osmotic balance in liquid formulations.
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UNII 55X04QC32I
A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
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UNII 70WT22SF4B
A mineral salt that acts as a buffer to maintain the pH balance of the medication. It helps stabilize the drug's potency and prevents unwanted chemical changes during storage.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
6 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Cytalux 3.2 mg/1.6mLthis 81052-0138-10 | On | 1 vial | — | — | FDA listed | — |
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⏳ Availability & generic status
We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.
Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.
🛈 What do these terms mean?
- Patent
- Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
- Substance patent
- Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
- Formulation (product) patent
- Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
- Method-of-use patent
- A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
- Skinny label
- A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
- Exclusivity
- FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
- Paragraph IV
- A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
- RLD / RS
- Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
- TE / AB rating
- FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
- LOE (loss of exclusivity)
- The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.
Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.
| Patent | Type | Use code | Expires |
|---|---|---|---|
| US 9333270 ↗ | Drug substance | U-3291 | Aug 26, 2033 |
| US 9061057 ↗ | Drug substance | U-3291 | Nov 29, 2035 |
| US 10881747 ↗ | Drug substance | U-3291 | Aug 26, 2033 |
| US 9789208 ↗ | Drug substance | U-3291 | Aug 26, 2033 |
| US 9254341 ↗ | Drug substance | — | Oct 4, 2033 |
| US 9341629 ↗ | Drug substance | — | Aug 26, 2033 |
| Code | What it grants | Expires |
|---|---|---|
| NCE | New Chemical Entity (5-year) | Nov 29, 2026 |
| ODE-390 | Orphan Drug Exclusivity (7-year) | Nov 29, 2028 |
Is there a generic version of CYTALUX 3.2 MG /1.6 ML VIAL?
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 81052-0138-10 You're viewing this | 10 CARTON in 1 CARTON (81052-138-10) / 1 VIAL, SINGLE-DOSE in 1 CARTON / 1.6 mL in 1 VIAL, SINGLE-DOSE | 2021-11-29 | Active |
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1. INDICATIONS AND USAGE CYTALUX is indicated as an adjunct for intraoperative identification of: Malignant lesions in adult patients with ovarian cancer. Malignant and non-malignant pulmonary lesions in adult patients with known or suspected cancer in the lung.
CYTALUX is an optical imaging agent indicated as an adjunct for intraoperative identification of: Malignant lesions in adult patients with ovarian cancer. Malignant and non-malignant pulmonary lesions in adult patients with known or suspected cancer in the lung. ( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION For recommended testing, evaluations, and premedications, see Full Prescribing Information. ( 2.1 ) Recommended intravenous dosage of CYTALUX is: Adult Patients with Ovarian Cancer: 0.025 mg/kg over 60 minutes, 1 hour to 9 hours prior to surgery Adult Patients with Known or Suspected Cancer in the Lung: 0.025 mg/kg over 60 minutes, 1 hour to 24 hours prior to surgery. ( 2.2 ) For preparation, management of infusion-related reactions, and imaging information see Full Prescribing Information.
CYTALUX should only be used by trained surgeons using FDA cleared imaging systems. ( 2.3 , 2.4 , 2.5 )
2.1Recommended 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) ].
2.2Recommended 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.
2.3Preparation 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. Remove carton containing one single vial of CYTALUX from freezer and record the date, time and thawing condition on the carton.
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. 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.
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. 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.
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 c…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Injection: 3.2 mg/1.6 mL (2 mg/mL) pafolacianine (equivalent to 3.4 mg/1.6 mL pafolacianine sodium) supplied as a dark bluish green, clear aqueous solution in a single-dose vial. Injection: 3.2 mg/1.6 mL (2 mg/mL) of pafolacianine in a single-dose vial. (3)
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None. (4)
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Infusion-Related Reactions: Interrupt the infusion and treat as necessary with antihistamines and/or nausea medications. ( 5.1 ) Risk of misinterpretation: Non-fluorescing tissue in the surgical field does not rule out the presence of tumor. Fluorescence may be seen in non-cancerous tissues.
( 5.2 ) Embryo-Fetal Toxicity: CYTALUX may cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus. ( 5.3 , 8.1 , 8.3 ) Risk of Pafolacianine Aggregation and Infusion Reactions: Use only 5% Dextrose Injection for dilution.
Do not use other diluents. ( 5.4 )
5.1Infusion-Related Reactions Adverse reactions including nausea, vomiting, abdominal pain, flushing, hypersensitivity, elevation in blood pressure, dyspepsia, and chest discomfort were reported in patients receiving CYTALUX in clinical studies. A total of 17% of patients experienced reactions during the administration of CYTALUX [see Adverse Reactions ( 6.1 )] . Reactions typically occurred within 15 minutes of the start of infusion.
CYTALUX infusion interruption or discontinuation due to adverse reactions occurred in 11% of all patients. Treatment with antihistamines and/or anti-nausea medication may be used. If an adverse reaction occurs during administration, the infusion can be interrupted and resumed after treatment of the reaction [see Dosage and Administration ( 2.1 , 2.4 )] .
5.2Risk of Misinterpretation Errors may occur with the use of CYTALUX during intraoperative fluorescence imaging to detect ovarian cancer and lesions in the lung, including false negatives and false positives. Non-fluorescing tissue in the surgical field does not rule out the presence of ovarian cancer or lesions in the lung [see Clinical Studies ( 14 )] . Fluorescence may be seen in normal tissues including bowel, kidneys, lymph nodes, and lungs as well as in inflamed tissues.
5.3Embryo-Fetal Toxicity Based on its mechanism of action, CYTALUX may cause fetal harm when administered to a pregnant woman. Advise females of reproductive potential of the potential risk to a fetus. Verify pregnancy status of females of reproductive potential prior to initiating CYTALUX treatment. [ see Use in Specific Populations ( 8.1 , 8.3 ), Clinical Pharmacology ( 12.1 ) ].
5.4Risk of Pafolacianine Aggregation and Infusion Reactions Use of the incorrect diluent to prepare the CYTALUX infusion solution can cause the aggregation of pafolacianine; aggregation may induce infusion reactions, such as nausea, vomiting, abdominal pain or rash. Use only 5% Dextrose Injection to prepare the CYTALUX infusion solution. Do not use other diluents. [see Dosage and Administration ( 2.3 )].
5.1Infusion-Related Reactions Adverse reactions including nausea, vomiting, abdominal pain, flushing, hypersensitivity, elevation in blood pressure, dyspepsia, and chest discomfort were reported in patients receiving CYTALUX in clinical studies. A total of 17% of patients experienced reactions during the administration of CYTALUX [see Adverse Reactions ( 6.1 )] . Reactions typically occurred within 15 minutes of the start of infusion.
CYTALUX infusion interruption or discontinuation due to adverse reactions occurred in 11% of all patients. Treatment with antihistamines and/or anti-nausea medication may be used. If an adverse reaction occurs during administration, the infusion can be interrupted and resumed after treatment of the reaction [see Dosage and Administration ( 2.1 , 2.4 )] .
5.2Risk of Misinterpretation Errors may occur with the use of CYTALUX during intraoperative fluorescence imaging to detect ovarian cancer and lesions in the lung, including false negatives and false positives. Non-fluorescing tissue in the surgical field does not rule out the presence of ovarian cancer or lesions in the lung [see Clinical Studies ( 14 )] . Fluorescence may be seen in normal tissues including bowel, kidneys, lymph nodes, and lungs as well as in inflamed tissues.
5.3 Embryo-Fetal Toxicity…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reaction is described elsewhere in the labeling: • Infusion-Related Reactions [ see Warnings and Precautions ( 5.1 ) ] Most common adverse reactions (incidence ≥1%; ovarian and lung combined) included nausea, vomiting, abdominal pain, flushing, other infusion-related reactions, hypersensitivity, elevation in blood pressure, dyspepsia, and chest discomfort. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact On Target Laboratories at 1-844-434-9333 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of CYTALUX was evaluated in four open label clinical studies, two studies (N = 44 and N = 150) in patients with ovarian cancer and two studies (N = 100 and N = 112) in patients with known or suspected cancer in the lung.
A total of 406 patients received 0.025 mg/kg of CYTALUX via intravenous administration. The demographic characteristics of the study population were 82% female (66% female in lung studies), mean age 64 years (range 26 to 89 years), 85% White, 6% Black or African American, 5% Asian, and 4% other race, 5% Hispanic or Latino, 92% Not Hispanic or Latino, and 3% unreported ethnicity. Adverse reactions that occurred in > 1% of patients are presented in Table 1.
Table 1. Adverse Reactions from Clinical Studies Reported in ≥ 1% of CYTALUX Treated Patients with Ovarian Cancer or Known or Suspected Cancer in the Lung Adverse Reaction CYTALUX 0.025 mg/kg (N = 406) % Nausea 13 Vomiting 5 Abdominal pain 2 Flushing 2 Other infusion-related reactions 2 Hypersensitivity 2 Elevation in blood pressure 1 Dyspepsia 1 Chest discomfort 1 Adverse reactions occurred during the administration of CYTALUX in 17% of patients. Overall, the safety profile observed in patients treated with CYTALUX 0.025 mg/kg was similar between patients with ovarian cancer and patients with known or suspected cancer in the lung.
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of CYTALUX was evaluated in four open label clinical studies, two studies (N = 44 and N = 150) in patients with ovarian cancer and two studies (N = 100 and N = 112) in patients with known or suspected cancer in the lung.
A total of 406 patients received 0.025 mg/kg of CYTALUX via intravenous administration. The demographic characteristics of the study population were 82% female (66% female in lung studies), mean age 64 years (range 26 to 89 years), 85% White, 6% Black or African American, 5% Asian, and 4% other race, 5% Hispanic or Latino, 92% Not Hispanic or Latino, and 3% unreported ethnicity. Adverse reactions that occurred in > 1% of patients are presented in Table 1.
Table 1. Adverse Reactions from Clinical Studies Reported in ≥ 1% of CYTALUX Treated Patients with Ovarian Cancer or Known or Suspected Cancer in the Lung Adverse Reaction CYTALUX 0.025 mg/kg (N = 406) % Nausea 13 Vomiting 5 Abdominal pain 2 Flushing 2 Other infusion-related reactions 2 Hypersensitivity 2 Elevation in blood pressure 1 Dyspepsia 1 Chest discomfort 1 Adverse reactions occurred during the administration of CYTALUX in 17% of patients. Overall, the safety profile observed in patients treated with CYTALUX 0.025 mg/kg was similar between patients with ovarian cancer and patients with known or suspected cancer in the lung.
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Use of folate, folic acid, or folate-containing supplements may reduce binding of pafolacianine to folate receptors and could reduce the detection of lesions with CYTALUX. Avoid administration of folate, folic acid, or folate-containing supplements within 48 hours before administration of CYTALUX [see Dosage and Administration (2.1) and Clinical Pharmacology (12.1) ]. Folate Supplements: Avoid folate, folic acid, or folate-containing supplements within 48 hours before administration of CYTALUX.
(7) See 17 for PATIENT COUNSELING INFORMATION.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary Based on its mechanism of action, pafolacianine may cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no available human data to evaluate for a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. No adverse developmental effects were observed in rats and rabbits with intravenous administration of pafolacianine during organogenesis (embryofetal development) at doses up to 158-fold (rat) and 570-fold (rabbit) the recommended human dose of 0.025 mg/kg based on AUC, otherwise 9.6 and 38.4-fold based on human equivalent dose (HED) ( see Data ).
The estimated background risk of major birth defects and miscarriage for the indicated populations are unknown. All pregnancies have a background risk of birth defects, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
Data Animal Data In the definitive embryo-fetal development (EFD) studies, pafolacianine was intravenously administered during the period of organogenesis as follows: 0.015, 0.15, and 1.5 mg/kg/day from gestational day (GD) 6 to GD17 in rats (HEDs of 0.002, 0.024 and 0.242 mg/kg/day), and 0.3, 1, and 3 mg/kg/day from GD7 to GD20 in rabbits (HEDs of 0.097, 0.323 and 0.968 mg/kg/day). No significant drug-related maternal toxicity and embryo-fetal development toxicity were observed. NOAELs were 1.5 mg/kg/day in rats and 3 mg/kg/day in rabbits.
Estimated systemic exposures were 158 times (rat) and 570 times (rabbit) the human exposure at a human dose of 0.025 mg/kg based on plasma AUC comparison.
8.2Lactation Risk Summary There are no data on the presence of pafolacianine in either human or animal milk, the effects on the breastfed infant, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for CYTALUX and any potential adverse effects on the breastfed infant from CYTALUX or from the underlying maternal condition.
8.3Females and Males of Reproductive Potential CYTALUX may cause fetal harm if administered to a pregnant woman [see Warnings And Precautions ( 5.3 ) and Use in Specific Populations ( 8.1 )] . Pregnancy Testing Obtain a pregnancy test in females of reproductive potential and verify the absence of pregnancy prior to administration of CYTALUX [see Dosage and Administration ( 2.1 )] .
8.4Pediatric Use Safety and effectiveness of CYTALUX in pediatric patients have not been established.
8.5Geriatric Use Of the total number of patients in clinical studies of CYTALUX, 221 patients (54%) were 65 years of age and older: 153 (38%) were 65 to 74 years of age, 66 (16%) were 75 to 84 years of age, and 2 (0.5%) were 85 years of age and older. No overall differences in safety, effectiveness, or pharmacokinetics were observed between patients 65 years of age and older and younger adult patients.
8.1Pregnancy Risk Summary Based on its mechanism of action, pafolacianine may cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no available human data to evaluate for a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. No adverse developmental effects were observed in rats and rabbits with intravenous administration of pafolacianine during organogenesis (embryofetal development) at doses up to 158-fold (rat) and 570-fold (rabbit) the recommended human dose of 0.025 mg/kg based on AUC, otherwise 9.6 and 38.4-fold based on human equivalent dose (HED) ( see Data ).
The estimated background risk of major birth defects and miscarriage for the indicated populations are unknown. All pregnancies have a background risk of birth defects, loss, or other adverse outcomes. In the U.…
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism 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.
12.2Pharmacodynamics 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.
12.3Pharmacokinetics 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 ±
5.99L, 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 ±
4.97L/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
12.1Mechanism 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.
12.2Pharmacodynamics 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.
12.3Pharmacokinetics 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 ±
5.99L, 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 ±
4.97L/hr. Metaboli…
📦 How Supplied / Storage and Handling ▾
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
📋 Description ▾
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 61 H 63 N 9 Na 4 O 17 S 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. 214907s000lbl.jpg