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Identification
- Summary
Verteporfin is a benzoporphyrin derivative used to treat pathological myopia, ocular histoplasmosis, and choroidal neovascularization in macular degeneration.
- Brand Names
- Visudyne
- Generic Name
- Verteporfin
- DrugBank Accession Number
- DB00460
- Background
Verteporfin, marketed as Visudyne, is a benzoporphyrin derivative comprising a 50:50 mixture of two isomers: CL-315555 and CL-315585. It is used as a photosensitizer in photodynamic therapy to eliminate abnormal blood vessels in wet form macular degeneration. Verteporfin accumulates in these abnormal blood vessels and, when stimulated by nonthermal red light with a wavelength of 693 nm in the presence of oxygen, produces highly reactive short-lived singlet oxygen and other reactive oxygen radicals, resulting in local damage to the endothelium and blockage of the vessels.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Synonyms
- Verteporfin
- Verteporfina
- Vertéporfine
- Verteporfinum
- External IDs
- BPD
- BPD-MA
- CL 318952
- FF 18
Pharmacology
- Indication
For the treatment of patients with predominantly classic subfoveal choroidal neovascularization due to age-related macular degeneration, pathologic myopia or presumed ocular histoplasmosis syndrome. Verteporfin can also be used to destroy tumors.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Subfoveal choroidal neovascularization •••••••••••• Management of Subfoveal choroidal neovascularization ••• ••••• Management of Subfoveal choroidal neovascularization ••• ••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Verteporfin, otherwise known as benzoporphyrin derivative, is a medication used in conjunction with laser treatment to eliminate the abnormal blood vessels in the eye associated with conditions such as the wet form of macular degeneration. Verteporfin accumulates in these abnormal blood vessels and, when stimulated by nonthermal red light with a wavelength of 693 nm in the presence of oxygen, produces highly reactive short-lived singlet oxygen and other reactive oxygen radicals, resulting in local damage to the endothelium and blockage of the vessels.
- Mechanism of action
Verteporfin is transported in the plasma primarily by lipoproteins. Once verteporfin is activated by light in the presence of oxygen, highly reactive, short-lived singlet oxygen and reactive oxygen radicals are generated. Light activation of verteporfin results in local damage to neovascular endothelium, resulting in vessel occlusion. Damaged endothelium is known to release procoagulant and vasoactive factors through the lipo-oxygenase (leukotriene) and cyclo-oxygenase (eicosanoids such as thromboxane) pathways, resulting in platelet aggregation, fibrin clot formation and vasoconstriction. Verteporfin appears to somewhat preferentially accumulate in neovasculature, including choroidal neovasculature. However, animal models indicate that the drug is also present in the retina. As singlet oxygen and reactive oxygen radicals are cytotoxic, Verteporfin can also be used to destroy tumor cells.
- Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Metabolized to a small extent to its diacid metabolite by liver and plasma esterases. NADPH-dependent liver enzyme systems (including the cytochrome P450 isozymes) do not appear to play a role in the metabolism of verteporfin.
- Route of elimination
Elimination is by the fecal route, with less than 0.01% of the dose recovered in urine.
- Half-life
Following intravenous infusion, verteporfin exhibits a bi-exponential elimination with a terminal elimination half-life of approximately 5-6 hours. Mild hepatic insufficiency increases half-life by approximately 20%.
- Clearance
Not Available
- Adverse Effects
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Overdose of drug and/or light in the treated eye may result in nonperfusion of normal retinal vessels with the possibility of severe decrease in vision that could be permanent. An overdose of drug will also result in the prolongation of the period during which the patient remains photosensitive to bright light.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAminolevulinic acid Aminolevulinic acid may increase the photosensitizing activities of Verteporfin. Carprofen Carprofen may increase the photosensitizing activities of Verteporfin. Celecoxib Celecoxib may increase the photosensitizing activities of Verteporfin. Clofazimine Clofazimine may increase the photosensitizing activities of Verteporfin. Cyproheptadine Cyproheptadine may increase the photosensitizing activities of Verteporfin. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Active Moieties
Name Kind UNII CAS InChI Key CL-315555 mixture WU713D62N9 133513-12-9 YTZALCGQUPRCGW-MXVXOLGGSA-N CL-315585 mixture 54JVX48G8K 142878-05-5 CABKTHJNHVBKCC-MXVXOLGGSA-N - International/Other Brands
- Visudine (Novartis)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Visudyne Injection, powder, lyophilized, for solution 2 mg/1mL Intravenous Novartis 2000-04-14 2012-09-01 US 
Visudyne Powder, for solution 15 mg / vial Intravenous Cheplapharm Arzneimittel Gmbh 2000-06-26 Not applicable Canada 
Visudyne Injection, powder, lyophilized, for solution 15 mg/1 Intravenous QLT Ophthalmics, Inc. 2000-04-12 Not applicable US Visudyne Injection, powder, for solution 15 mg Intravenous Cheplapharm Arzneimittel Gmb H 2020-12-16 Not applicable EU 
Visudyne Injection, powder, lyophilized, for solution 15 mg/1 Intravenous Bausch Health US LLC 2000-04-12 Not applicable US
Categories
- ATC Codes
- S01LA01 — Verteporfin
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 0X9PA28K43
- CAS number
- 129497-78-5
References
- General References
- Chan WM, Lim TH, Pece A, Silva R, Yoshimura N: Verteporfin PDT for non-standard indications--a review of current literature. Graefes Arch Clin Exp Ophthalmol. 2010 May;248(5):613-26. doi: 10.1007/s00417-010-1307-z. Epub 2010 Feb 17. [Article]
- Nowak-Sliwinska P, Karocki A, Elas M, Pawlak A, Stochel G, Urbanska K: Verteporfin, photofrin II, and merocyanine 540 as PDT photosensitizers against melanoma cells. Biochem Biophys Res Commun. 2006 Oct 20;349(2):549-55. Epub 2006 Aug 22. [Article]
- External Links
- Human Metabolome Database
- HMDB0014603
- KEGG Drug
- D01162
- PubChem Compound
- 5362420
- PubChem Substance
- 46506236
- ChemSpider
- 4515032
- 118886
- ChEMBL
- CHEMBL2052016
- PharmGKB
- PA451871
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Verteporfin
- FDA label
- Download (39.2 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data4 Completed Treatment Age - Related Macular Degeneration (AMD) 2 somestatus stop reason just information to hide 4 Completed Treatment Age - Related Macular Degeneration (AMD) / Polypoidal Choroidal Vasculopathy (PCV) 1 somestatus stop reason just information to hide 4 Completed Treatment Maculopathy, Age Related / Subfoveal Choroidal Neovascularization (CNV) 1 somestatus stop reason just information to hide 4 Completed Treatment Polypoidal Choroidal Vasculopathy (PCV) 1 somestatus stop reason just information to hide 4 Terminated Treatment Age - Related Macular Degeneration (AMD) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Qlt inc
- Packagers
- Hollister-Stier Laboratories LLC
- JHP Pharmaceuticals LLC
- Novartis AG
- QLT Inc.
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous 15 mg/1vial Injection, powder, lyophilized, for solution Intravenous 15 mg/1 Injection, powder, lyophilized, for solution Intravenous 2 mg/1mL Powder, for solution Intravenous 15 mg / vial Powder, for solution Intravenous; Parenteral 15 MG Injection Intravenous 15 mg Injection, powder, for solution Intravenous 15 mg - Prices
Unit description Cost Unit Visudyne 15 mg vial 1702.64USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5214036 No 1993-05-25 2010-05-25 US CA2536069 No 2008-06-03 2014-03-14 Canada CA1339927 No 1998-06-23 2015-06-23 Canada US5756541 No 1998-05-26 2016-03-11 US US5798349 No 1998-08-25 2015-08-25 US US5707608 No 1998-01-13 2015-08-02 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 2.1 Not Available - Predicted Properties
- Not Available
- Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.5377 Blood Brain Barrier + 0.6313 Caco-2 permeable - 0.6425 P-glycoprotein substrate Substrate 0.7738 P-glycoprotein inhibitor I Non-inhibitor 0.577 P-glycoprotein inhibitor II Non-inhibitor 0.5444 Renal organic cation transporter Non-inhibitor 0.7681 CYP450 2C9 substrate Non-substrate 0.8178 CYP450 2D6 substrate Non-substrate 0.822 CYP450 3A4 substrate Substrate 0.6429 CYP450 1A2 substrate Inhibitor 0.7915 CYP450 2C9 inhibitor Inhibitor 0.7158 CYP450 2D6 inhibitor Non-inhibitor 0.754 CYP450 2C19 inhibitor Non-inhibitor 0.7057 CYP450 3A4 inhibitor Non-inhibitor 0.5157 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.652 Ames test Non AMES toxic 0.6596 Carcinogenicity Non-carcinogens 0.9368 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.6756 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9884 hERG inhibition (predictor II) Non-inhibitor 0.9038
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Drug created at June 13, 2005 13:24 / Updated at June 14, 2024 18:55