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Biological Chemistry

Patent Picks: Scleroderma Treatments

A look at recent patenting activity in scleroderma treatments, brought to you by C&EN and CAS

by Science, Technology & Education Department
September 28, 2015 | A version of this story appeared in Volume 93, Issue 38

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Credit: Walt Fletcher
A common symptom of scleroderma sufferers is reduced blood flow to the fingertips.
An image of the arm of a scleroderma sufferer.
Credit: Walt Fletcher
A common symptom of scleroderma sufferers is reduced blood flow to the fingertips.

Limited scleroderma is a chronic autoimmune disease characterized by hardening of the hand’s skin and vasculature. The disease is rare—only about 77,000 Americans have it—and it afflicts women three times as often as is does men. The exact cause of these painful cutaneous manifestations is not known, but viruses and oxidative stress are possible suspects. The disease first presents itself as a dysfunction in the lining of the hand’s blood vessels resulting in inflammation, collagen deposition, and impairment in the ability to create new blood vessels. There is no cure for scleroderma, only treatments to relieve symptoms, such as pain from ulceration and stiffness due to vasoconstriction. Here, we highlight three advances in scleroderma treatment from the databases of Chemical Abstracts Service (CAS).

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Using Fat Cells To Mitigate Pain

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Credit: Cytori Therapeutics
Cytori Therapeutic’s adipose cell therapy treatment is injected on both sides of each finger in the hand.
Image of Cytori Therapeutics adipose cell therapy treatment in action.
Credit: Cytori Therapeutics
Cytori Therapeutic’s adipose cell therapy treatment is injected on both sides of each finger in the hand.

Researchers at Cytori Therapeutics use a patient’s own adipose, or fat, cells to treat some of the worse symptoms of the disease (WO 2015042182). The process involves using a liposuction device to remove fat from the patient, an amount roughly equal to a volume of half-a-can of soda, says John Fraser, the chief scientist at Cytori. With a proprietary enzymatic digestion, Cytori’s system can remove fat cells from the sample, leaving other adipose cell types that can contribute to healing, such as stem cells, mesenchymal and endothelial progenitor cells, lymphatic cells, and pericytes. Clinicians can then inject these fat-free adipose cells at the site of a patient’s scleroderma lesions. The injected cells stimulate production of factors that promote blood vessel growth, such as VEGF and PIGF. In a pilot study, researchers tested the therapy on 12 scleroderma patients who had functional disability in their hands. One year after treatment, the patients regained significant function in their hands and had significantly less pain, Fraser tells C&EN.

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Topical Scleroderma Treatment

Tyrosine kinases are responsible for the activation of multitudes of signaling pathways in cells, including those that initiate inflammation and eventual hardening of the hand’s skin and vasculature in scleroderma patients. A team from PreCision Dermatology formulated a cream that incorporates a tyrosine kinase inhibitor (TKI) as a topical treatment for scleroderma (WO 2015005985). The cream consists of imatinib mesylate, a TKI approved by FDA to treat chronic myeloid leukemia, dissolved in a mixture of phosphate-buffered saline, benzyl alcohol, ethanol, and hydroxypropyl cellulose. When given to mice with scleroderma, the TKI cream decreased inflammation and kinase receptor gene expression. In 2014, PreCision was bought by Valeant Pharmaceuticals for $450 million.

Structure of imatinib mesylate.

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Blue Light Special For Pain

People who suffer from scleroderma often experience pain caused by the constriction of blood vessels in their hands. Dan Berkowitz and Gautam Sikka from Johns Hopkins University may have a way to relieve that pain through a light-based treatment. The method takes advantage of a little known phenomenon in which blood vessels relax when stimulated with blue light. The mechanism behind the relaxation is thought to involve melanopsin receptors, which play an important role in regulating the body’s circadian rhythms. The protein probably resides in the smooth muscle layer of blood vessels, Berkowitz says. However, blood vessels become desensitized from chronic light exposure. Berkowitz says that he and Sikka next want to identify melanopsin receptor kinase inhibitors to pair with the photorelaxation therapy to block the desensitization effect. So far the team has studied the phenomenon only in isolated blood vessels and in the tail arteries of live mice but plans to test in animal models of scleroderma.

Mitch Garcia wrote this month’s PatentPicks in collaboration with CAS. This feature reports on trends CAS scientists observe from patents in CAS databases. Please send comments and suggestions to patentpicks@acs.org.

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