药品详细

Porfimer(卟吩姆)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

卟吩姆

英文名

Porfimer

分子式

C₉₉H₁₁₀N₁₂O₁₃

化学名

3-{14-[1-({3-[14-(1-{1-[10,14-bis(2-carboxyethyl)-5,9,15,19,20-pentamethyl-21,22,23,24-tetraazapentacyclo[16.2.1.1^{3,6}.1^{8,11}.1^{13,16}]tetracosa-3,5,7,9,11(23),12,14,16,18(21),19-decaen-4-yl]ethoxy}ethyl)-20-(2-carboxyethyl)-5,9,10,15,19-pentamethyl-21,22,23,24-tetraazapentacyclo[16.2.1.1^{3,6}.1^{8,11}.1^{13,16}]tetracosa-1(21),2,4,6,8(23),9,13,15,17,19-decaen-4-yl]propanoyl}oxy)ethyl]-20-(2-carboxyethyl)-5,9,10,15,19-pentamethyl-21,22,23,24-tetraazapentacyclo[16.2.1.1^{3,6}.1^{8,11}.1^{13,16}]tetracosa-1(21),2,4,6,8(23),9,13,15,17,19-decaen-4-yl}propanoic acid

分子量

Average: 1676.0053
Monoisotopic: 1674.831531666

CAS号

87806-31-3

ATC分类

L01X 其它抗肿瘤药

药物类型

small molecule

阶段

approved

商品名

Photofrin;

同义名

DHE;DHP ether;Dihematoporphyrin ether;Porfimer sodium;

基本介绍

The purified component of hematoporphyrin derivative, it consists of a mixture of oligomeric porphyrins. It is used in photodynamic therapy (hematoporphyrin photoradiation); to treat malignant lesions with visible light and experimentally as an antiviral agent. It is the first drug to be approved in the use of photodynamic therapy in the United States. [PubChem]

生产厂家

Axcan pharma us inc

封装厂家

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Not Available

Substructures

Not Available

适应症

Cancer 癌症;

药理

Indication	Indicated in the treatment of esophageal cancer.
Pharmacodynamics	Porfimer is a photosensitizing agent used in the photodynamic therapy (PDT) of tumors. Porfimer is indicated for the palliation of patients with completely obstructing esophageal cancer, or of patients with partially obstructing esophageal cancer who cannot be satisfactorily treated with Nd:YAG laser therapy, reduction of obstruction and palliation of symptoms in patients with completely or partially obstructing endobronchial nonsmall cell lung cancer (NSCLC), and the treatment of microinvasive endobronchial NSCLC in patients for whom surgery and radiotherapy are not indicated. The cytotoxic and antitumor actions of porfimer are light and oxygen dependent. Tumor selectivity in treatment occurs through a combination of selective retention of porfimer and selective delivery of light.
Mechanism of action	Cellular damage caused by porfimer is a consequence of the propagation of radical reactions. Radical initiation may occur after porfimer absorbs light to form a porphyrin excited state. Spin transfer from porfimer 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.
Absorption	Not Available
Volume of distribution	0.49 ± 0.28 L/kg [2 mg/kg dose of porfimer sodium to 4 male cancer patients]
Protein binding	~90%
Metabolism	Not Available
Route of elimination	Not Available
Half life	10-452 hours
Clearance	Renal cl=199.7 +/- 56.9 mL/min [Healthy subjects receiving a single 300-mg oral dose]
Toxicity	Not Available
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
logP	2.8	Not Available

Predicted Properties

Property	Value	Source
logP	5.55	ChemAxon
hydrogen acceptor count	21	ChemAxon
hydrogen donor count	11	ChemAxon
polar surface area	379.65	ChemAxon
rotatable bond count	25	ChemAxon
refractivity	496.6	ChemAxon
polarizability	199.95	ChemAxon

药物相互作用

食物相互作用

Not Available

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