PHOTOFRIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PHOTOFRIN (PHOTOFRIN).
Porfimer sodium is a photosensitizing agent that, upon activation by light of a specific wavelength (630 nm), produces reactive oxygen species (primarily singlet oxygen) causing cellular damage and tumor cell death. It selectively accumulates in malignant tissue due to increased lipid content and reduced lymphatic drainage.
| Metabolism | Porfimer sodium is not metabolized to a significant extent; it is eliminated primarily via the reticuloendothelial system and excreted in feces. Small amounts may be excreted in urine. |
| Excretion | Primarily excreted via the biliary/fecal route (>90%), with renal excretion accounting for <2% of the administered dose. |
| Half-life | Terminal elimination half-life approximately 15-20 hours for the porfimer sodium component; clinically, photosensitivity persists for up to 90 days due to prolonged skin retention. |
| Protein binding | Highly protein-bound (~90%), primarily to albumin and lipoproteins. |
| Volume of Distribution | Approximately 0.4 L/kg; indicates extensive distribution into tissues, particularly retention in tumor and skin. |
| Bioavailability | Not applicable; administered exclusively as intravenous infusion; oral bioavailability is negligible (<1%). |
| Onset of Action | Photodynamic therapy: onset of photoactivation occurs immediately upon laser light application (typically 40-50 hours after intravenous administration to allow tumor selectivity). |
| Duration of Action | Photodynamic effect lasts for the duration of light exposure (usually 10-30 minutes per treatment); residual drug in skin causes photosensitivity for up to 90 days, requiring patient precautions. |
2 mg/kg IV over 3-5 minutes, followed by laser light activation at 48-72 hours post-infusion. The drug-light interval may be extended up to 96 hours for esophageal cancer.
| Dosage form | Injectable |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min). Insufficient data for severe impairment or dialysis; use with caution. |
| Liver impairment | No specific Child-Pugh based adjustments. Use caution in severe hepatic impairment due to potential increased photosensitivity risk. |
| Pediatric use | Safety and efficacy not established in pediatric patients (<18 years). No dosing guidelines available. |
| Geriatric use | No specific dose adjustment recommended. Monitor for photosensitivity and renal function as elderly may have reduced organ function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PHOTOFRIN (PHOTOFRIN).
| Breastfeeding | It is unknown whether porfimer sodium is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. M/P ratio not available. |
| Teratogenic Risk | PHOTOFRIN (porfimer sodium) is a photosensitizer used in photodynamic therapy. Due to its mechanism of action involving light activation and production of reactive oxygen species, there is potential for fetal harm. Animal studies have shown fetal toxicity and teratogenicity at doses similar to human doses. In the first trimester, risk of major malformations is unknown but theoretical. In second and third trimesters, there is risk of fetal photosensitivity and possible effects on developing tissues. Use during pregnancy is contraindicated unless potential benefit justifies risk. |
■ FDA Black Box Warning
No black box warnings.
| Serious Effects |
["Porphyria or known hypersensitivity to porfimer sodium or porphyrins.","Existing tracheoesophageal or bronchoesophageal fistula (for esophageal PDT).","Tumors eroding into a major blood vessel.","Pregnancy (Category C) and lactation."]
| Precautions | ["Photosensitivity: Patients remain photosensitive for at least 30 days; avoid exposure to sunlight or bright indoor light.","Ocular sensitivity: Protect eyes from direct sunlight or bright light for 30 days.","Chest pain, dysphagia, esophageal stricture, and perforation risk in esophageal PDT.","Hemoptysis and respiratory distress in endobronchial PDT.","Anaphylactic reactions (rare).","Hepatic impairment may alter clearance."] |
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| Fetal Monitoring | Monitor maternal hepatic and renal function, as porfimer is eliminated via the liver and photoactivation can cause oxidative stress. Assess fetal growth and well-being via ultrasound if used during pregnancy. Monitor for maternal skin photosensitivity reactions. No specific fetal monitoring required beyond standard obstetric care. |
| Fertility Effects | Effects on human fertility are unknown. In animal studies, no significant effects on male or female fertility were observed at clinically relevant doses. However, due to the drug's mechanism, potential ovarian or testicular toxicity cannot be excluded. |