Porfimer

Medically reviewed by Drugs.com. Last updated on Sep 4, 2023.

Pronunciation

(POR fi mer)

Index Terms

CL-184116
Dihematoporphyrin Ester
Dihematoporphyrin Ether
Porfimer Sodium

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous, as sodium [preservative free]:

Photofrin: 75 mg (1 ea)

Brand Names: U.S.

Photofrin

Pharmacologic Category

Antineoplastic Agent, Miscellaneous

Pharmacology

Porfimer's cytotoxic activity is dependent on light and oxygen. Following administration, the drug is selectively retained in neoplastic tissues. Exposure of the drug to laser light at wavelengths >630 nm results in the production of oxygen free-radicals. Release of thromboxane A₂, leading to vascular occlusion and ischemic necrosis, may also occur.

Distribution

Steady state V_d: 0.49 L/kg ± 0.28 L/kg (Pereira 2010)

Half-Life Elimination

First dose: ~17 days; Second dose: ~30 days.

Protein Binding

Plasma: ~90%

Use: Labeled Indications

Barrett esophagus dysplasia (photodynamic therapy): Ablation of high-grade dysplasia in Barrett esophagus (in patients who do not undergo esophagectomy)

Endobronchial cancer (photodynamic therapy): Treatment of microinvasive endobronchial non-small cell lung cancer (NSCLC) in patients for whom surgery and radiation therapy are not indicated; reduction of obstruction and symptom palliation in patients with obstructing (partial or complete) endobronchial NSCLC

Esophageal cancer (photodynamic therapy): Palliation of completely obstructing esophageal cancer, or partially obstructing esophageal cancer in patients who cannot be treated satisfactorily with Nd:YAG laser therapy.

Off Label Uses

Cholangiocarcinoma (unresectable)

Data from a small, randomized, controlled study suggest that porfimer (as a component of photodynamic therapy) in addition to best supportive care may have benefit in the treatment of nonresectable cholangiocarcinoma (Bismuth types II to IV; TNM stage III to IV), based on the primary end point of survival time as well as quality of life measures ^{[Ortner 2003]}.

Contraindications

Porphyria; photodynamic therapy (PDT) is contraindicated in patients with existing tracheoesophageal or bronchoesophageal fistula, tumors eroding into a major blood vessel, emergency treatment of severe acute respiratory distress when caused by an obstructing endobronchial lesion, esophageal or gastric varices, esophageal ulcers >1 cm in diameter.

Canadian labeling: Additional contraindications (not in the US labeling): Hypersensitivity to porphyrins; PDT is contraindicated in patients with papillary bladder cancer who have received prior total bladder radiation or whose functional bladder capacity is <200 mL and in patients with coexisting bladder tumors of stage greater than stage 1 (T1) who have invasive cancer.

Dosing: Adult

Barrett esophagus dysplasia (photodynamic therapy): IV: 2 mg/kg, followed by endoscopic exposure to the appropriate laser light; repeat courses must be separated by at least 90 days (delay subsequent treatment for insufficient healing) for a maximum of 3 courses.

Cholangiocarcinoma, unresectable (photodynamic therapy) (off-label use): IV: 2 mg/kg, followed 48 hours later by light activation (Ortner 2003).

Endobronchial non-small cell lung cancer (photodynamic therapy): IV: 2 mg/kg, followed by endoscopic exposure to the appropriate laser light and debridement; repeat courses must be separated by at least 30 days (delay subsequent treatment for insufficient healing) for a maximum of 3 courses.

Esophageal cancer (photodynamic therapy): IV: 2 mg/kg, followed by endoscopic exposure to the appropriate laser light and debridement; repeat courses must be separated by at least 30 days (delay subsequent treatment for insufficient healing) for a maximum of 3 courses.

Dosing: Geriatric

Refer to adult dosing.

Reconstitution

Due to the potential for photosensitivity reactions, wear rubber gloves and eye protection and avoid skin and eye contact during preparation and administration. Spills should be wiped with a damp cloth and contaminated material should be disposed of properly. Protect from bright light if overexposure occurs.

Reconstitute each 75 mg vial with 31.8 mL of either D5W or NS injection resulting in a final concentration of 2.5 mg/mL. Shake well until dissolved. Protect the reconstituted product from bright light and use immediately. Use appropriate precautions for handling and disposal.

Administration

IV: Administer slow IV injection over 3 to 5 minutes. Avoid extravasation (if extravasation occurs, protect area from light and sunlight).

Due to the potential for photosensitivity reactions, wear rubber gloves and eye protection and avoid skin and eye contact during administration; if overexposure occurs, protect from bright light. Spills should be wiped with a damp cloth and contaminated material should be disposed of properly.

Storage

Store intact vials at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Reconstituted solutions should be protected from bright light and used immediately after preparation.

Drug Interactions

Aminolevulinic Acid (Systemic): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Systemic). Avoid combination

Aminolevulinic Acid (Topical): Photosensitizing Agents may enhance the photosensitizing effect of Aminolevulinic Acid (Topical). Monitor therapy

Photosensitizing Agents: May enhance the photosensitizing effect of Porfimer. Monitor therapy

Verteporfin: Photosensitizing Agents may enhance the photosensitizing effect of Verteporfin. Monitor therapy

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Cardiovascular: Chest pain (8% to 22%), edema (5% to 18%)

Dermatologic: Skin photosensitivity (19% to 69%)

Gastrointestinal: Esophageal stenosis (6% to 38%), nausea (24%), constipation (5% to 24%), abdominal pain (20%), vomiting (17%), dysphagia (10%)

Hematologic & oncologic: Anemia (esophageal cancer: 32%)

Nervous system: Pain (5% to 22%), insomnia (5% to 14%)

Neuromuscular & skeletal: Back pain (3% to 11%)

Respiratory: Pleural effusion (5% to 32%), dyspnea (7% to 30%), bronchial obstruction (≤21%), bronchial plugs (≤21%), pneumonia (12% to 18%), hemoptysis (16%), cough (7% to 15%), bronchoconstriction (bronchostenosis: 11%), pharyngitis (11%)

Miscellaneous: Fever (16% to 31%), serous drainage (22%)

1% to 10%:

Cardiovascular: Atrial fibrillation (10%), hypotension (7%), peripheral edema (5% to 7%), cardiac failure (≤7%), hypertension (6%), tachycardia (6%), substernal pain (5%), acute myocardial infarction (<5%), angina pectoris (<5%), bradycardia (<5%), pulmonary embolism (<5%), sick sinus syndrome (<5%), supraventricular tachycardia (<5%)

Endocrine & metabolic: Weight loss (9%), dehydration (7%)

Gastrointestinal: Anorexia (8%), disease of esophagus (esophageal edema: 8%), hematemesis (8%), tracheoesophageal fistula (6%), dyspepsia (2% to 6%), diarrhea (5%), eructation (5%), esophagitis (5%), melena (5%), esophageal perforation (<5%), gastric ulcer (<5%), intestinal obstruction (<5%), peritonitis (<5%)

Genitourinary: Urinary tract infection (7%)

Hematologic & oncologic: Tumor hemorrhage (8%), pulmonary hemorrhage (<5%)

Hepatic: Jaundice (<5%)

Infection: Candidiasis (9%), abscess (lung: <5%)

Nervous system: Confusion (8%), anxiety (6% to 7%), voice disorder (5%)

Neuromuscular & skeletal: Asthenia (6%)

Ophthalmic: Diplopia (<5%), eye pain (<5%), photophobia (<5%), visual disturbance (<5%)

Respiratory: Bronchitis (≤10%), respiratory insufficiency (6% to 10%), bronchospasm (<5%), laryngeal edema (<5%), pneumonitis (<5%), productive cough (8%), pulmonary edema (<5%), respiratory failure (<5%), stridor (<5%)

Miscellaneous: Ulcer (bronchial: 9%), postoperative complication (5%)

<1%, postmarketing, and/or case reports: Cataract, cerebrovascular accident, cutaneous nodule, fluid volume disorder, fragile skin, gastrointestinal necrosis, gastrointestinal perforation, hemorrhage, hypertrichosis, infusion related reaction (including dizziness and urticaria), local tissue necrosis (esophageal), pseudoporphyria, sepsis, skin discoloration, thromboembolism, wrinkling of skin

Warnings/Precautions

Concerns related to adverse effects:

• Airway obstruction: Treatment-induced inflammation may obstruct airway. Use with caution in patients with endobronchial tumors, especially if in areas where main airway may be obstructed (long or surrounding tumors). Necrotic debris or mucositis may also cause airway obstruction. Monitor closely between laser therapy and debridement for respiratory distress; may require urgent bronchoscopy to remove secretions or debris.

• Chest pain: Inflammatory responses within the treatment area may result in substernal chest pain.

• Esophageal strictures: Esophageal strictures may occur, usually within 6 months of treatment. May require multiple dilations to resolve. The risk is increased with nodule pretreatment or with re-treatment of the same area.

• Extravasation: Avoid extravasation. If extravasation occurs, protect affected area from light; use of antidotes is of unknown benefit.

• Gastroesophageal fistula/perforation: Serious and potentially fatal gastrointestinal and esophageal necrosis and perforation may occur following treatment. Due to the high risk for fistula, do not use in patients with esophageal tumors eroding into the trachea or bronchial tree/wall. Use is contraindicated in patients with existing tracheoesophageal or bronchoesophageal fistula.

• Hemorrhage: Patients with esophageal varices or tumors eroding into pulmonary blood vessels are at increased risk for hemorrhage, including fatal massive pulmonary hemoptysis (FMH). Do not administer light directly to an area with esophageal varices due to the potential for hemorrhage. Other risk factors for FMH include large, centrally located tumors, cavitating tumors, or extensive tumor extrinsic to the bronchus.

• Ocular photosensitivity: Ocular discomfort has been reported with sun or bright light exposure (or car headlights). For at least 30 days (and until ocular sensitivity resolves), when outdoors, patients should wear dark sunglasses that have an average white light transmittance of <4%.

• Photosensitivity: Photosensitivity reactions are common in patients who are exposed to direct sunlight or bright indoor light (eg fluorescent lights, unshaded light bulbs, examination/operating lights). Conventional UV sunscreens are not protective against photosensitivity reactions caused by visible light. Photosensitivity may last 30 to 90 days or more. Encourage exposure to ambient indoor light (aids in gradually inactivating residual porfimer). Patients should be educated to test for residual photosensitivity before resuming exposure to sunlight. Re-exposure to general sunlight should be gradual (expose small area of skin [not the face] for 10 minutes), if no photosensitivity (eg, edema, erythema, blistering) occurs after 24 hours, may gradually resume normal outdoor activities; if photosensitivity occurs then wait 2 weeks and retest.

• Thromboembolism: Thromboembolic events may occur, generally in patients with additional risk factors for thromboembolism (eg, advanced cancer, prolonged immobilization, cardiovascular disease, following major surgery).

Disease-related concerns:

• Barrett esophagus: In patients with Barrett esophagus, conduct rigorous surveillance (endoscopic biopsy every 3 months until 4 consecutive negative results for high-grade dysplasia followed by further follow-up per physician judgment). The long-term effects of photodynamic therapy in patients with Barrett esophagus are not known. Esophageal strictures are common adverse events associated with photodynamic therapy of Barrett esophagus; esophageal dilation may be required.

• Esophageal/gastric varices: Not suited for treatment of patients with esophageal or gastric varices (due to the high risk for hemorrhage).

• Hepatic impairment: Elimination may be prolonged in hepatic impairment; toxicities may be increased. Photosensitivity may persist beyond 90 days in patients with mild to severe hepatic impairment.

• Renal impairment: Elimination may be prolonged in renal impairment; toxicities may be increased. Photosensitivity may persist beyond 90 days in patients with severe renal impairment.

Concurrent drug therapy issues:

• Photosensitizing drugs: Concurrent use with other photosensitizing agents may increase the risk for photosensitivity reactions.

Special populations:

• Radiation therapy recipients: Allow 2 to 4 weeks to elapse after phototherapy prior to initiating radiation therapy; 4 weeks should elapse after radiation therapy prior to initiating phototherapy.

Monitoring Parameters

Evaluate pregnancy status prior to use in females of reproductive potential. Monitor injection site during infusion (for extravasation); monitor in between laser and debridement for evidence of respiratory distress in patients with endobronchial tumors; monitor for signs/symptoms of photosensitivity, hemorrhage, thromboembolic events, gastroesophageal fistulas/perforation, esophageal strictures.

Reproductive Considerations

Evaluate pregnancy status prior to use in females of reproductive potential. Females of reproductive potential should use effective contraception during treatment and for 5 months after the last porfimer dose. Males with female partners of reproductive potential should use condoms during treatment and for 5 months after the last porfimer dose.

Pregnancy Considerations

Based on the mechanism of action and data from animal reproduction studies, in utero exposure to porfimer may cause fetal harm.

Patient Education

What is this drug used for?

• It is used to treat cancer.

• It is used to treat changes in the swallowing tube called Barrett's esophagus.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Hair growth

• Nausea

• Vomiting

• Abdominal pain

• Constipation

• Diarrhea

• Weight loss

• Lack of appetite

• Anxiety

• Skin discoloration

• Skin changes

• Trouble sleeping

• Back pain

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Urinary tract infection like blood in the urine, burning or painful urination, passing a lot of urine, fever, lower abdominal pain, or pelvic pain

• Dehydration like dry skin, dry mouth, dry eyes, increased thirst, fast heartbeat, dizziness, fast breathing, or confusion

• Severe headache

• Severe dizziness

• Passing out

• Vision changes

• Mouth irritation

• Mouth sores

• Throat irritation

• Confusion

• Shortness of breath

• Swelling of arms or legs

• Excessive weight gain

• Fast heartbeat

• Abnormal heartbeat

• Vaginal pain, itching, and discharge

• Trouble swallowing

• Persistent cough

• Severe or persistent skin reaction

• Severe loss of strength and energy

• Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight

• Bowel problems like black, tarry, or bloody stools; fever; mucus in stools; vomiting; vomiting blood; severe abdominal pain; constipation; or diarrhea

• Blood clots like numbness or weakness on one side of the body; pain, redness, tenderness, warmth, or swelling in the arms or legs; change in color of an arm or leg; chest pain; shortness of breath; fast heartbeat; or coughing up blood

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.