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 Porfimer Sodium

porfimer sodium is the sodium salt of a mixture of oligomers formed by ether and ester linkages of up to eight porphyrin units with photodynamic activity. Absorbed selectively by tumor cells, porfimer produces oxygen radicals after activation by 630 nm wavelength laser light, resulting in tumor cell cytotoxicity. In addition, tumor cell death may occur due to ischemic necrosis secondary to vascular occlusion that appears to be partly mediated by the release of thromboxane A2. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Porfimer sodium, sold as Photofrin, is a photosensitizer used in photodynamic therapy and radiation therapy and for palliative treatment of obstructing endobronchial non-small cell lung carcinoma and obstructing esophageal cancer. Porfimer is a mixture of oligomers formed by ether and ester linkages of up to eight porphyrin units. It absorbs red light at 630nm. It was approved in Canada in 1993 for the treatment of bladder cancer. It was approved in Japan in 1994. It was approved by the U.S. FDA in December 1995 esophageal cancer, and in 1998, it was approved for the treatment of early non-small cell lung cancer. In August 2003 the FDA approved its use for Barrett's esophagus. (source: http://en.wikipedia.org/wiki/Porfimer_sodium).

DRUG DESCRIPTION

PHOTOFRIN (porfimer sodium) for Injection is a photosensitizing agent used in the photodynamic therapy (PDT) of tumors and of high-grade dysplasia (HGD) in Barrett's esophagus (BE). Following reconstitution of the freeze-dried product with 5% Dextrose Injection (USP) or 0.9% Sodium Chloride Injection (USP), it is injected intravenously. This is followed 40–50 hours later by illumination of the tumor or the esophageal segment with HGD in BE with laser light (630 nm wavelength). PHOTOFRIN is not a single chemical entity; it is a mixture of oligomers formed by ether and ester linkages of up to eight porphyrin units. It is a dark red to reddish brown cake or powder. Each vial of PHOTOFRIN contains 75 mg of porfimer sodium as a sterile freeze-dried cake or powder. Hydrochloric Acid and/or Sodium Hydroxide may be added during manufacture to adjust the pH to within 7.2-7.9. There are no preservatives or other additives.

Mechanism of Action

Cellular damage caused by photodynamic therapy (PDT) with PHOTOFRIN is a consequence of the propagation of radical reactions. Radical initiation may occur after porfimer sodium absorbs light to form a porphyrin excited state. Spin transfer from porfimer sodium to molecular oxygen may then generate singlet oxygen. Subsequent radical reactions can form superoxide and hydroxyl radicals. Tumor death also occurs through ischemic necrosis secondary to vascular occlusion that appears to be partly mediated by thromboxane A2 release. As opposed to a thermal effect, the laser treatment with porfimer sodium induces a photochemical effect. The necrotic reaction and associated inflammatory responses may evolve over several days.

INDICATIONS

Esophageal Cancer: PHOTOFRIN® is indicated 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.

Endobronchial Cancer: PHOTOFRIN is indicated for the treatment of microinvasive endobronchial non-small-cell lung cancer (NSCLC) in patients for whom surgery and radiotherapy are not indicated. PHOTOFRIN is indicated for the reduction of obstruction and palliation of symptoms in patients with completely or partially obstructing endobronchial NSCLC.

High-Grade Dysplasia: PHOTOFRIN is indicated for the ablation of high-grade dysplasia in Barrett'spatients who do not undergo esophagectomy.
 

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