Verteporfin
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Verteporfin (trade name Visudyne), a
benzoporphyrin Porphyrins ( ) are a group of heterocyclic macrocycle organic compounds, composed of four modified pyrrole subunits interconnected at their α carbon atoms via methine bridges (=CH−). The parent of porphyrin is porphine, a rare chemical compo ...
derivative, is a
medication A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy (pharmacotherapy) is an important part of the medical field and re ...
used as a
photosensitizer Photosensitizers produce a physicochemical change in a neighboring molecule by either donating an electron to the substrate or by abstracting a hydrogen atom from the substrate. At the end of this process, the photosensitizer eventually returns to ...
for
photodynamic therapy Photodynamic therapy (PDT) is a form of phototherapy involving light and a photosensitizing chemical substance, used in conjunction with molecular oxygen to elicit cell death (phototoxicity). PDT is popularly used in treating acne. It is used cl ...
to eliminate the abnormal
blood vessel The blood vessels are the components of the circulatory system that transport blood throughout the human body. These vessels transport blood cells, nutrients, and oxygen to the tissues of the body. They also take waste and carbon dioxide away ...
s in the eye associated with conditions such as the wet form of
macular degeneration Macular degeneration, also known as age-related macular degeneration (AMD or ARMD), is a medical condition which may result in blurred or no vision in the center of the visual field. Early on there are often no symptoms. Over time, however, som ...
. Verteporfin accumulates in these abnormal blood vessels and, when stimulated by nonthermal red light with a
wavelength In physics, the wavelength is the spatial period of a periodic wave—the distance over which the wave's shape repeats. It is the distance between consecutive corresponding points of the same phase on the wave, such as two adjacent crests, tro ...
of 689 nm in the presence of
oxygen Oxygen is the chemical element with the symbol O and atomic number 8. It is a member of the chalcogen group in the periodic table, a highly reactive nonmetal, and an oxidizing agent that readily forms oxides with most elements as wel ...
, produces highly reactive short-lived singlet oxygen and other reactive oxygen radicals, resulting in local damage to the
endothelium The endothelium is a single layer of squamous endothelial cells that line the interior surface of blood vessels and lymphatic vessels. The endothelium forms an interface between circulating blood or lymph in the lumen and the rest of the vessel ...
and blockage of the vessels.Verteporfin Verteporfin is also used
off-label Off-label use is the use of pharmaceutical drugs for an unapproved indication or in an unapproved age group, dosage, or route of administration. Both prescription drugs and over-the-counter drugs (OTCs) can be used in off-label ways, although m ...
for the treatment of
central serous retinopathy Central serous chorioretinopathy (CSC or CSCR), also known as central serous retinopathy (CSR), is an eye disease that causes visual impairment, often temporary, usually in one eye. When the disorder is active it is characterized by leakage of f ...
.


Administration

Verteporfin is usually injected
intravenous Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutrie ...
ly into the largest arm vein. It is injected at a dose of 6 mg/m2 and light-activated. It is usually is given 15 minutes before laser treatment. This dose can be repeated 4 times per year.


Contraindications

Porphyria Porphyria is a group of liver disorders in which substances called porphyrins build up in the body, negatively affecting the skin or nervous system. The types that affect the nervous system are also known as acute porphyria, as symptoms are ra ...
.


Side effects

Most common side effects are blurred vision, headache, and local effects at the injection site. Also,
photosensitivity Photosensitivity is the amount to which an object reacts upon receiving photons, especially visible light. In medicine, the term is principally used for abnormal reactions of the skin, and two types are distinguished, photoallergy and phototoxicity. ...
; it is strictly advised to avoid exposure to sunlight and unscreened lighting until 48 hours after verteporfin administration. Dogs and rats have been treated with inactivated daily doses 32–70 times higher than the dose advised for humans. The 4 weeks of treatment resulted in mild extravascular hemolysis and hematopoiesis in the animals.


Interactions

Verteporfin is known to interact with the herbal remedy
feverfew ''Tanacetum parthenium'', known as feverfew, is a flowering plant in the daisy family, Asteraceae. It may be grown as an ornamental plant, ornament, and may be identified by its synonyms, ''Chrysanthemum parthenium'' and ''Pyrethrum parthenium' ...
(''Tanacetum parthenium''), the latter of which seems to act as an antagonist to verteporfin for unknown reasons. Taking the two substances simultaneously is inadvisable. Verteporfin does not appear to be metabolized by
Cytochrome P450 Cytochromes P450 (CYPs) are a Protein superfamily, superfamily of enzymes containing heme as a cofactor (biochemistry), cofactor that functions as monooxygenases. In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are ...
enzymes, therefore not affecting
Cytochrome P450 Cytochromes P450 (CYPs) are a Protein superfamily, superfamily of enzymes containing heme as a cofactor (biochemistry), cofactor that functions as monooxygenases. In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are ...
metabolism of other drugs.


Shortages

In May 2020, a low manufacturing capacity caused disruption. This affected the usage of verteporfin among providers and patients in Europe. The EMA expected normal manufacturing to return by the first quarter 2022.


Potential against scarring

Verteporfin is FDA approved. Verteporfin is a YAP pathway inhibitor. Verteporfin displays a wide spectrum of anti-fibrotic properties. Verteporfin prevents fibrosis in several human organs. Verteporfin was first noted as a drug that blocked cell proliferation in the liver. It is an inhibitor of fibrosis in patients with persistent
cholestasis Cholestasis is a condition where bile cannot flow from the liver to the duodenum. The two basic distinctions are an obstructive type of cholestasis where there is a mechanical blockage in the duct system that can occur from a gallstone or malignan ...
. Research has highlighted that verteporfin decreased expression of fibrotic genes in fibroblasts collected from nodules of patients suffering from
Dupuytren's contracture Dupuytren's contracture (also called Dupuytren's disease, Morbus Dupuytren, Viking disease, palmar fibromatosis and Celtic hand) is a condition in which one or more fingers become progressively bent in a flexed position. It is named after Guilla ...
. In 2018 information revealed verteporfin stopped fibrosis in the lung. Verteporfin is a marketed drug with a good safety profile. Physicians use verteporfin off-label. In 2018, physicians described the off-label usage for Peyronie's disease as an interesting step. In 2021, scientists tested verteporfin to reveal if the drug would prevent scar tissue in skin.Molteni, Megan,
In mouse experiments, scientists unlock the key to scar-free skin healing
', STAT News, April 22, 2021
The testing of verteporfin on humans cleft lips was due to occur in late 2021.


References


External links

* {{Intracellular chemotherapeutic agents Photosensitizing agents Ophthalmology drugs Novartis brands