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 Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: cancer tissue |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Palliative | PHOTOFRIN Approved UsePHOTOFRIN is a photodynamic therapy drug indicated for: Esophageal Cancer (1.1) 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 (1.2) Treatment of microinvasive endobronchial non-small-cell lung cancer (NSCLC) in patients for whom surgery and radiotherapy are not indicated Reduction of obstruction and palliation of symptoms in patients with completely or partially obstructing endobronchial NSCLC High-Grade Dysplasia in Barrett's Esophagus (1.3) Ablation of high-grade dysplasia (HGD) in Barrett's esophagus (BE) patients who do not undergo esophagectomy 1.1 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. 1.2 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. 1.3 High-Grade Dysplasia in Barrett's Esophagus PHOTOFRIN is indicated for the ablation of high-grade dysplasia in Barrett's esophagus patients who do not undergo esophagectomy. Launch Date1995 |
|||
| Palliative | PHOTOFRIN Approved UsePHOTOFRIN is a photodynamic therapy drug indicated for: Esophageal Cancer (1.1) 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 (1.2) Treatment of microinvasive endobronchial non-small-cell lung cancer (NSCLC) in patients for whom surgery and radiotherapy are not indicated Reduction of obstruction and palliation of symptoms in patients with completely or partially obstructing endobronchial NSCLC High-Grade Dysplasia in Barrett's Esophagus (1.3) Ablation of high-grade dysplasia (HGD) in Barrett's esophagus (BE) patients who do not undergo esophagectomy 1.1 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. 1.2 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. 1.3 High-Grade Dysplasia in Barrett's Esophagus PHOTOFRIN is indicated for the ablation of high-grade dysplasia in Barrett's esophagus patients who do not undergo esophagectomy. Launch Date1995 |
|||
| Primary | PHOTOFRIN Approved UsePHOTOFRIN is a photodynamic therapy drug indicated for: Esophageal Cancer (1.1) 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 (1.2) Treatment of microinvasive endobronchial non-small-cell lung cancer (NSCLC) in patients for whom surgery and radiotherapy are not indicated Reduction of obstruction and palliation of symptoms in patients with completely or partially obstructing endobronchial NSCLC High-Grade Dysplasia in Barrett's Esophagus (1.3) Ablation of high-grade dysplasia (HGD) in Barrett's esophagus (BE) patients who do not undergo esophagectomy 1.1 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. 1.2 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. 1.3 High-Grade Dysplasia in Barrett's Esophagus PHOTOFRIN is indicated for the ablation of high-grade dysplasia in Barrett's esophagus patients who do not undergo esophagectomy. Launch Date1995 |
|||
| Primary | PHOTOFRIN Approved UsePHOTOFRIN is a photodynamic therapy drug indicated for: Esophageal Cancer (1.1) 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 (1.2) Treatment of microinvasive endobronchial non-small-cell lung cancer (NSCLC) in patients for whom surgery and radiotherapy are not indicated Reduction of obstruction and palliation of symptoms in patients with completely or partially obstructing endobronchial NSCLC High-Grade Dysplasia in Barrett's Esophagus (1.3) Ablation of high-grade dysplasia (HGD) in Barrett's esophagus (BE) patients who do not undergo esophagectomy 1.1 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. 1.2 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. 1.3 High-Grade Dysplasia in Barrett's Esophagus PHOTOFRIN is indicated for the ablation of high-grade dysplasia in Barrett's esophagus patients who do not undergo esophagectomy. Launch Date1995 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
43.1 μg/mL |
2 mg/kg single, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
PORFIMER plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
15.3 μg/mL |
2 mg/kg single, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
PORFIMER plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
43105.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20629974/ |
2 mg/kg 1 times / 5 weeks multiple, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PORFIMER serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
41307.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20629974/ |
2 mg/kg 1 times / 5 weeks multiple, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PORFIMER serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2937 μg × h/mL |
2 mg/kg single, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
PORFIMER plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
974 μg × h/mL |
2 mg/kg single, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
PORFIMER plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2937444.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20629974/ |
2 mg/kg 1 times / 5 weeks multiple, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PORFIMER serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
3937582.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20629974/ |
2 mg/kg 1 times / 5 weeks multiple, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PORFIMER serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
410 h |
2 mg/kg single, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
PORFIMER plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
250 h |
2 mg/kg single, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
PORFIMER plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
409.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20629974/ |
2 mg/kg 1 times / 5 weeks multiple, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PORFIMER serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
725 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20629974/ |
2 mg/kg 1 times / 5 weeks multiple, intravenous dose: 2 mg/kg route of administration: Intravenous experiment type: MULTIPLE co-administered: |
PORFIMER serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
10% |
PORFIMER serum | Homo sapiens |
Doses
| Dose | Population | Adverse events |
|---|---|---|
2 mg/kg 1 times / month multiple, intravenous Studied dose Dose: 2 mg/kg, 1 times / month Route: intravenous Route: multiple Dose: 2 mg/kg, 1 times / month Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: photosensitivity... AEs leading to discontinuation/dose reduction: photosensitivity (3 patients) Sources: |
2 mg/kg single, intravenous Studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| photosensitivity | 3 patients Disc. AE |
2 mg/kg 1 times / month multiple, intravenous Studied dose Dose: 2 mg/kg, 1 times / month Route: intravenous Route: multiple Dose: 2 mg/kg, 1 times / month Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Heme oxygenase-1 protects tumor cells against photodynamic therapy-mediated cytotoxicity. | 2006-06-08 |
|
| Celecoxib and NS-398 enhance photodynamic therapy by increasing in vitro apoptosis and decreasing in vivo inflammatory and angiogenic factors. | 2005-10-15 |
|
| Erythropoietin restores the antitumor effectiveness of photodynamic therapy in mice with chemotherapy-induced anemia. | 2002-05 |
|
| Phototherapy of bladder cancer: dose/effect relationships. | 1986-08 |
Patents
Sample Use Guides
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18782948
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
Created
by
admin
on
Edited
Mon Mar 31 22:25:15 GMT 2025
by
admin
on
Mon Mar 31 22:25:15 GMT 2025
|
| Record UNII |
Y3834SIK5F
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Preferred Name | English | ||
|
Official Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
WHO-ATC |
L01XD01
Created by
admin on Mon Mar 31 22:25:15 GMT 2025 , Edited by admin on Mon Mar 31 22:25:15 GMT 2025
|
||
|
FDA ORPHAN DRUG |
35589
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
||
|
WHO-VATC |
QL01XD01
Created by
admin on Mon Mar 31 22:25:15 GMT 2025 , Edited by admin on Mon Mar 31 22:25:15 GMT 2025
|
||
|
FDA ORPHAN DRUG |
191904
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
||
|
EU-Orphan Drug |
EU/3/02/086
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
||
|
FDA ORPHAN DRUG |
39489
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
||
|
NCI_THESAURUS |
C1420
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
||
|
EMA ASSESSMENT REPORTS |
PHOTOBARR (WITHDRAWN: BARRETT ESOPHAGUS)
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
||
|
FDA ORPHAN DRUG |
357011
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
m8988
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | Merck Index | ||
|
SUB03955MIG
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | |||
|
Y3834SIK5F
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | |||
|
BB-28
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | |||
|
C1071
Created by
admin on Mon Mar 31 22:25:15 GMT 2025 , Edited by admin on Mon Mar 31 22:25:15 GMT 2025
|
PRIMARY | |||
|
DB00707
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | |||
|
100000089426
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | |||
|
60773
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | |||
|
CHEMBL1201481
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | |||
|
6670
Created by
admin on Mon Mar 31 22:25:15 GMT 2025 , Edited by admin on Mon Mar 31 22:25:15 GMT 2025
|
PRIMARY | |||
|
333848
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | RxNorm | ||
|
Y3834SIK5F
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | |||
|
DTXSID101021967
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | |||
|
Porfimer sodium
Created by
admin on Mon Mar 31 22:25:16 GMT 2025 , Edited by admin on Mon Mar 31 22:25:16 GMT 2025
|
PRIMARY | |||
|
87806-31-3
Created by
admin on Mon Mar 31 22:25:15 GMT 2025 , Edited by admin on Mon Mar 31 22:25:15 GMT 2025
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
|
Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| MOIETY | Sodium cation | LYR4M0NH37 |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT | CHEMICAL |
|