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Description

Porfimer is a photosensitizing agent used in the photodynamic therapy (PDT) of tumors. Porfimer sodium was approved under the brand name PHOTOFRIN for the palliation of patients with completely obstructing esophageal cancer, or of patients with partially obstructing esophageal cancer who, in the opinion of their physician, cannot be satisfactorily treated with Nd:YAG laser therapy. For the reduction of obstruction and palliation of symptoms in patients with completely or partially obstructing endobronchial nonsmall cell lung cancer (NSCLC). For the treatment of microinvasive endobronchial NSCLC in patients for whom surgery and radiotherapy are not indicated. In addition, for the ablation of high-grade dysplasia in Barrett’s esophagus patients who do not undergo esophagectomy. The cytotoxic and antitumor actions of PHOTOFRIN® are light and oxygen dependent. Photodynamic therapy with Porfimer sodium is a two-stage process. The first stage is the intravenous injection of the drug, which mainly is concentrated in the tumor tissues for a longer period. Illumination with 630 nm wavelength laser light constitutes the second stage of therapy. Cellular damage is a consequence of the propagation of radical reactions. Radical initiation may occur after porfimer absorbs light to form a porphyrin excited state. Tumor death also occurs through ischemic necrosis secondary to vascular occlusion that appears to be partly mediated by thromboxane A2 release. The laser treatment induces a photochemical, not a thermal, effect. The necrotic reaction and associated inflammatory responses may evolve over several days.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
PHOTOFRIN
Palliative
PHOTOFRIN
Primary
PHOTOFRIN
Primary
PHOTOFRIN

Cmax

ValueDoseCo-administeredAnalytePopulation
43.1 μg/mL
2 mg/kg single, intravenous
PORFIMER plasma
Homo sapiens
15.3 μg/mL
2 mg/kg single, intravenous
PORFIMER plasma
Homo sapiens
43105.6 ng/mL
2 mg/kg 1 times / 5 weeks multiple, intravenous
PORFIMER serum
Homo sapiens
41307.1 ng/mL
2 mg/kg 1 times / 5 weeks multiple, intravenous
PORFIMER serum
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
2937 μg × h/mL
2 mg/kg single, intravenous
PORFIMER plasma
Homo sapiens
974 μg × h/mL
2 mg/kg single, intravenous
PORFIMER plasma
Homo sapiens
2937444.7 ng × h/mL
2 mg/kg 1 times / 5 weeks multiple, intravenous
PORFIMER serum
Homo sapiens
3937582.7 ng × h/mL
2 mg/kg 1 times / 5 weeks multiple, intravenous
PORFIMER serum
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
410 h
2 mg/kg single, intravenous
PORFIMER plasma
Homo sapiens
250 h
2 mg/kg single, intravenous
PORFIMER plasma
Homo sapiens
409.9 h
2 mg/kg 1 times / 5 weeks multiple, intravenous
PORFIMER serum
Homo sapiens
725 h
2 mg/kg 1 times / 5 weeks multiple, intravenous
PORFIMER serum
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
10%
PORFIMER serum
Homo sapiens

Doses

AEs

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
Photodynamic therapy (PTD) with PHOTOFRIN (porfimer sodium)) is a two-stage process requiring administration of both drug and light. The first stage of PDT is the intravenous injection of PHOTOFRIN at 2 mg/kg. Illumination with laser light 40–50 hours following injection with PHOTOFRIN constitutes the second stage of therapy. A second laser light application may be given 96-120 hours after injection, preceded by gentle debridement of residual tumor (see Administration of Laser Light).
Route of Administration: Intravenous
In Vitro Use Guide
Photofrin (porfimer sodium) was evaluated through in vitro processes with human malignant melanoma cells (MMCs). MMCs incubated with Photofrin at a concentration of about 3.5 microg/ml and exposed to laser light at 630 nm with a power density of 100 mW/cm2, showed 50% cell killing. An electron microscopic study demonstrated significant destruction of the target after photodynamic therapy (PDT).
Substance Class Polymer
Record UNII
Y3834SIK5F
Record Status Validated (UNII)
Record Version

Structural Modifications