CYTALUX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CYTALUX (CYTALUX).
CYTALUX (pafolacianine) is a folate receptor-targeted optical imaging agent. It binds to folate receptors (FRα) overexpressed on cancer cells and, upon activation by light, produces fluorescence for intraoperative imaging.
| Metabolism | Pafolacianine is metabolized primarily via reduction and conjugation. The exact metabolic enzymes are not fully characterized; however, in vitro studies suggest involvement of aldehyde oxidase and NADPH-dependent reductases. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 27% of the administered dose. Fecal excretion (primarily via biliary elimination) accounts for about 43%. |
| Half-life | Terminal elimination half-life is approximately 3.0 hours. This short half-life supports its use as a photodynamic therapy agent requiring rapid clearance to minimize prolonged photosensitivity. |
| Protein binding | 99.6% bound to plasma proteins, primarily to albumin and high-density lipoproteins. |
| Volume of Distribution | Volume of distribution is 0.61 L/kg, indicating distribution primarily within the vascular and interstitial spaces. |
| Bioavailability | Not applicable for intravenous administration. Oral bioavailability has not been studied; the drug is only approved for IV use. |
| Onset of Action | Following intravenous administration and light activation, the photodynamic effect begins within minutes. Clinical response is typically observed within 4-6 hours post-treatment. |
| Duration of Action | Duration of photosensitivity is approximately 40 hours post-infusion if no light activation occurs. After light activation, the therapeutic effect is localized and persists for several days. |
CYTALUX (pafolacianine) is administered intravenously at a dose of 0.025 mg/kg (based on actual body weight) over 60 minutes (±10 minutes) once between 1 to 9 hours prior to surgery.
| Dosage form | SOLUTION |
| Renal impairment | No specific dose adjustment is recommended based on renal impairment. However, the effect of severe renal impairment (eGFR <30 mL/min/1.73 m²) or end-stage renal disease on the pharmacokinetics of pafolacianine has not been evaluated. Monitor for adverse reactions. |
| Liver impairment | No specific dose adjustment is recommended based on hepatic impairment. The pharmacokinetics of pafolacianine have not been evaluated in patients with moderate (Child-Pugh B) or severe (Child-Pugh C) hepatic impairment. Use with caution. |
| Pediatric use | Safety and effectiveness in pediatric patients have not been established. No dosing recommendations are available for patients less than 18 years of age. |
| Geriatric use | Of the 276 patients in clinical studies who received CYTALUX, 42% were aged 65 and over, and 11% were aged 75 and over. No overall differences in safety or effectiveness were observed between these patients and younger patients, and no dose adjustment is recommended based on age. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CYTALUX (CYTALUX).
| Breastfeeding | No data on presence in human milk, effects on breastfed infant, or milk production. Caution should be exercised due to potential for serious adverse reactions. Consider developmental and health benefits of breastfeeding along with mother's clinical need for Cytalux and potential adverse effects on the infant. |
| Teratogenic Risk | Pregnancy Category X. Cytalux (pafolacianine) is a folate receptor-targeted fluorescent imaging agent. No human data available; animal studies show no teratogenic effects at clinically relevant doses. However, due to the mechanism of action, fetal risk cannot be excluded. Avoid use in pregnant women unless potential benefit outweighs risk. Use effective contraception during treatment and for at least 3 months after last dose. |
■ FDA Black Box Warning
None
| Serious Effects |
["Known hypersensitivity to pafolacianine or any component of CYTALUX"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis have been reported","Injection site reactions (e.g., pain, erythema, swelling)","Risk of false-negative or false-positive fluorescence; imaging should supplement visual inspection and palpation","Pregnancy: May cause fetal harm due to folate receptor expression in developing tissues; verify pregnancy status in women of reproductive potential"] |
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| Fetal Monitoring | Monitor for hypersensitivity reactions (including anaphylaxis, bronchospasm, hypotension) during and after infusion. Monitor for injection site reactions, nausea, vomiting, headache, and abdominal pain. No specific fetal monitoring recommended; if Cytalux is used during pregnancy, consider fetal monitoring per standard obstetric care. |
| Fertility Effects | No human data on fertility. In animal studies, there were no effects on male or female fertility at doses up to 10 times the recommended human dose based on body surface area. However, potential effects on fertility cannot be ruled out. |